rexresearch.com
Euphorbia
peplus [ Milkwood ] vs Cancer
http://www.dailymail.co.uk/health/article-1350454/Milkweed-miracle-Applying-sap-common-garden-weed-cure-skin-cancer.html
26th January 2011
Common
garden weed 'cures skin cancer', say scientists
by
Jenny Hope
A common weed could help cure skin cancers, claim researchers.
The sap from a plant known as
petty
spurge or milkweed [ * a typo -- actually, it's " milkw
ood " ] - found by
roadsides and in woodland - can 'kill' certain types of cancer cells
when applied to the skin.
It works on non-melanoma skin cancers, which affect hundreds of
thousands of Britons each year.
They are triggered by sun damage and, although not usually fatal, can
be disfiguring without treatment.
The plant has been used for centuries as a traditional folk medicine to
treat conditions such as warts, asthma and several types of cancer.
But for the first time a team of scientists in Australia has carried
out a clinical study of sap from
Euphorbia
peplus, which is related to
Euphorbia plants grown in gardens in the UK.
The study of 36 patients with a total of 48 non-melanoma lesions
included basal cell carcinomas (BCC), squamous cell carcinomas (SCC)
and intraepidermal carcinomas (IEC), a growth of cancerous cells
confined to the outer layer of the skin.
Patients had failed to respond to conventional treatment including
surgery, or they refused or were unsuitable for surgery because of
their age.
The patients were treated once a day for three consecutive days by an
oncologist using a cotton bud to apply enough of the E.peplus sap to
cover the surface of each lesion.
The initial results were impressive, says findings to be released this
week in the British Journal of Dermatology.
After only one month 41 of the 48 cancers had completely gone.
Patients who had some of the lesions remaining were offered a second
course of treatment.
After an average of 15 months following treatment, two thirds of the 48
skin cancer lesions were still showing a complete response.
Of the three types of skin cancer tested,
the final outcome was a 75
per cent complete response for IEC lesions, 57 per cent for BCC and 50
per cent for SCC lesions.
Side-effects were low, with 43 per cent of patients in no pain as a
result of the treatment and only 14 per cent reporting moderate pain,
and only one patient encountered severe short-term pain.
In all cases of successful treatment the skin was left with a good
cosmetic appearance.
The researchers, from a number of medical institutions in Brisbane,
attribute the benefit to the active ingredient ingenol mebutate which
has been shown to destroy tumour cells.
British experts said further studies were needed and people should not
try this at home as the weed sap can be harmful to the eyes and should
not be eaten.
More than 76,500 people are diagnosed with non-melanoma skin cancer in
the UK each year, with 90 per cent caused by ultraviolet light exposure.
Lesions usually appear on the areas most exposed to the sun, such as
the head, neck, ears, and back of the hands.
Kimberley Carter of the British Association of Dermatologists said:
'This is a very small test group so it will be interesting to see what
larger studies and the development of the active ingredient in E.
peplus sap will reveal.
'Whilst it would not provide an alternative to surgery for the more
invasive skin cancers or melanoma, in the future it might become a
useful addition to the treatments available to patients for
superficial, non-melanoma skin cancers.
'Any advances that could lead to new therapies for patients where
surgery is not an option are definitely worth investigating.
'It is also very important to note that this is definitely not a
treatment people should be trying out at home.
'Exposure of the sap to mucous producing surfaces, such as the eyes,
results in extreme inflammation and can lead to hospitalisation.
'The concentration of the active ingredients in the sap also varies
between different plants, with high doses able to cause very severe and
excessive inflammatory responses.'
Euphorbia
peplus : Petty Spurge, Milkwood
www.gardenorganic.org.uk
PETTY
SPURGE, OR MILKWOOD
Latin name: Euphorbia peplus
Occurrence: Petty spurge is a small, branched annual, plentiful in
gardens and arable fields.
It is native and common throughout the UK, in any kind of soil. The
plant exudes a milky sap when damaged, which is a severe irritant if
applied to the skin.
Biology: Petty spurge flowers from April to November. The seed number
per plant ranges from 260 to 1,200.
Petty spurge may be found in fruit for eight months of the year.
Seedlings emerge throughout the year except for in winter but the main
flush is from April to May. Most seed germinates within a year of
shedding.
Just a few seedlings emerge in the following 5 years. Germination
occurs at 5 to 10 mm depth in soil.
Persistence and Spread: Seed recovered from house demolitions and
archaeological digs and dated at 20, 25, 30 and 100 years old has been
reported to germinate.
www.wikipedia.org
Euphorbia
peplus
Not to be confused with Euphorbia peplis, Purple spurge, a relatively
rare plant of coastal sand and shingle.
Scientific classification
Kingdom: Plantae
Division: Magnoliophyta
Class: Magnoliopsida
Order: Malpighiales
Family: Euphorbiaceae
Genus: Euphorbia
Species: E. peplus
Binomial name : Euphorbia peplus L.
Euphorbia peplus (Petty spurge, Radium weed[1] or Cancer weed[2]) is a
species of Euphorbia, native to most of Europe, northern Africa, and
western Asia, where it typically grows in cultivated arable land,
gardens, and other disturbed land.[3][4][5]
It is an annual plant growing to between 5–30 cm tall (most plants
growing as weeds of cultivation tend towards the smaller end), with
smooth hairless stems. The leaves are oval-acute, 1–3 cm long, with a
smooth margin. It has green flowers in three-rayed umbels. The glands,
typical of the Euphorbiacae, are kidney-shaped with long thin horns.[5]
The milky latex sap is toxic, and used as a therapeutic agent for the
removal of warts and sunspots on the skin.[1] Recent work also suggests
that it may also be effective in treating superficial basal cell
carcinomas.[6][7]
Outside of its native range it is very widely naturalised and often
invasive, including in Australia, New Zealand, North America, and other
countries in temperate and sub-tropical regions.[3]
References
1. http://www.beautanicals.com.au/Petty%20spurge.html
2.
http://www.environmentalweedsactionnetwork.org.au/images/pdf/EterracinaWorkshopText.pdf
3. Germplasm Resources Information Network: Euphorbia peplus
4. Flora Europaea: Euphorbia peplus
5. Blamey, M. & Grey-Wilson, C. (1989). Flora of Britain and
Northern Europe. ISBN 0-340-40170-2
6. Goliath:Skin and Allergy News Sep 07: Plant-based compound shows
efficacy against basal cell cs
7. The Age May 06: Peplin cancer gel shows promise
http://plantmed.blogspot.com/2004_02_01_archive.html
February 24, 2004
Other
alternative skin cancer treatments
The white sap of petty spurge (Euphorbia peplus), also called cancer
weed or radium weed, is excellent on skin cancers and insensitive
external tumors. Skin cancers may also be destroyed by repeatedly
applying a drop of 35% hydrogen peroxide, preferably protecting the
surrounding skin with a barrier cream.
However, the most effective way to remove skin cancer, melanoma and
tumors close to the skin, possibly including breast tumors, is to apply
an 'Escharotic'. These are caustic remedies, commonly with zinc
chloride and the herb bloodroot as main ingredients. These may be
available from some health shops or naturopaths. Skin cancers may
become inflamed for a few days and then form dry pus (an eschar) and
fall out after about 10 days.
Before you rush out to buy the stuff, read this abstract on [negative]
Consequences of using escharotic agents as primary treatment for
nonmelanoma skin cancer.
http://www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=PubMed&list_uids=12472348&dopt=Abstract
Instructions for using Euphorbia peplus (petty spurge) - more from
Australia
Do not get in eye
from email: [it has] different effects on different areas of the
body... ...usually apply Betadine (Iodine) if any infection appears
present. Typically (on the face eg) the spot will become "angry"
looking, and break out into a weeping type sore. You may also see a
line or "lines" moving out from the spot. These also may breakout
through the skin. Both areas of reaction may take 2-3 weeks to settle,
and scab over, and it can look quite messy for a while. Past this
point, the area should start to heal and return to normal without the
cancer. Applying the sap daily for 3-4 days followed by every 2nd-3rd
day may be a better approach for some people. Certainly, reactions can
vary from person to person but the biggest risk is from secondary
infection and it is surprising how many people miss this point.
United States Patent Application
20090292017
THERAPEUTIC COMPOSITIONS
Brown; Marc Barry ; et al. November 26,
2009
Abstract
Ingenol angelate is a potent
anticancer agent, and can be stabilised by dissolving it in an aprotic
solvent in the presence of an acidic buffer.
Inventors: Brown; Marc Barry; (Watford, GB) ;
Crowthers; Michael Edward Donald; (Hillsborough, GB) ; Nazir; Tahir;
(Isleworth, GB)
Current U.S. Class: 514/511
Class at Publication: 514/511
International Class: A61K 31/25 20060101 A61K031/25;
A61P 35/00 20060101 A61P035/00
Description
[0001] The present invention relates to compositions of compounds
obtainable from Euphorbia species and which are useful in the treatment
of skin cancers.
[0002] The compound ingenol angelate can be isolated from various
Euphorbia species, and particularly from Euphorbia peplus and Euphorbia
drummondii. Ingenol angelate exists in three isoforms;
ingenol-3-angelate (isoform `b`), ingenol-5-angelate (isoform `a`) and
ingenol-20-angelate (isoform `c`). The first of these is also referred
to herein as I3A and has the following structure:
##STR00001##
[0003] Ingenol angelate has been found to be highly toxic for skin
cancer cells via rapid mitochondrial disruption and cell death by
primary necrosis, while leaving healthy cells unaffected.
[0004]
U.S. Pat. No. 6,432,452
discloses compounds present in an active principle derived from plants
of the species Euphorbia peplus, Euphorbia hirta and Euphorbia
drummondii, which show selective cytotoxicity against several different
cancer cell lines. The compounds are useful in effective treatment of
cancers, particularly malignant melanomas and squamous cell carcinomas
(SCCs). The compounds are selected from jatrophanes, pepluanes,
paralianes and ingenanes. The preferred compound is an
angeloyl-substituted ingenane obtained from the sap of Euphorbia peplus.
[0005] Microgram quantities of ingenol angelate are typically
therapeutically effective. However, the tendency for isoform `b` to
undergo rearrangement to isoform `a` and subsequently to isoform `c`
presents a formulation problem, where it is desired to restrict the
formulation to either a specific isoform or to a ratio of isoforms.
This is particularly a problem with I3A, as the different isoforms have
different solubilities.
[0006] There is a need for an effective, topical treatment for skin
cancer, as systemic treatments involving other drugs necessarily result
in exposure of susceptible healthy cells, in non-target parts of the
body, to cytotoxic chemicals. In addition, systemic anti-cancer
treatments, whether administered orally or by injection, have lower
patient acceptance.
[0007] There is a need to provide a stable formulation of ingenol
angelate, preferably for topical administration.
[0008] It has now, surprisingly, been found that ingenol angelate can
be solubilised, substantially without rearrangement between isoforms,
in an acceptable, aprotic solvent in the presence of an acceptable,
miscible acidic buffer.
[0009] Thus, in a first aspect, the present invention provides a
formulation of ingenol angelate for use in therapy, wherein the ingenol
angelate has been dissolved in a pharmaceutically acceptable, aprotic
solvent, said formulation further comprising a pharmaceutically
acceptable acidifying agent which is at least partially compatible with
the solvent and which provides the formulation with an apparent pH of
no greater than 4.5.
[0010] The present invention envisages formulations of any of the
isoforms of ingenol angelate, or mixtures thereof. At present, the
preferred isoform is isoform `b`, also referred to herein as I3A. It
will be understood that references to `ingenol angelate` and `I3A`
include reference to other isoforms and mixtures thereof, unless
otherwise apparent.
[0011] Ingenol angelate can be dissolved in many solvents, and various
solvents are illustrated in accompanying Example 1. However, ingenol
angelate is generally susceptible to rearrangement in protic solvents,
and any substantial degree of rearrangement, typically beyond about 1%
for plant derived products, but more preferably about 0.5%, is
undesirable in a pharmaceutical formulation.
[0012] In aprotic solvents, which are generally solvents that do not
contribute protons to a solution, such as polyethylene glycol,
dissolution can take some considerable time and this, together with the
temperatures required, can also lead to rearrangement to an extent
above acceptable levels.
[0013] Substances such as acetone and acetonitrile are capable of
dissolving I3A, but are not generally pharmaceutically acceptable, and
may not be suitable for long term storage. More acceptable may be
substances such as methyl ethyl ketone, ethyl acetate, or diethyl
ether, but benzyl alcohol is generally most preferred.
[0014] A number of substances are suitable to dissolve I3A, but
stability is not guaranteed, and generally unacceptable rearrangement
levels may be observed after periods ranging between as little as 12
hours and as much as six months or a year.
[0015] In the absence of water, or other protic solvent, there will not
be a measurable pH. Under such conditions, and especially at elevated
temperatures, rearrangement is likely. Thus, it has been found that it
is generally possible to inhibit rearrangement by the presence of a
suitable acid.
[0016] Suitable acids are generally organic acids, as it has been
established that I3A can decompose much below about a pH of 3, while
rearrangement is likely to occur at above a pH of about 4.5. Where it
is intended to store the formulation for periods of any length, such as
a month or more, then it is preferred that the acid be in the form of a
buffer. Suitable buffers include citrate buffer, phosphate buffer,
acetate buffer and citrate-phosphate buffer, although other buffers
will be apparent to those skilled in the art. In particular, it is
preferred that the buffer provides an apparent pH to the formulation of
no greater than 4.5 and no less than 2.5. A formulation pH of less than
4 is more preferred, and it is particularly preferred that the apparent
formulation pH be 3.8 or less, preferably around 3.5, or less. An
apparent pH of around 3 is useful. A buffer having a pH of 2.75 has
been found to be particularly advantageous, conferring an apparent pH
of about pH 3.5 to the final formulation when used in quantities as
illustrated in the accompanying Examples. A preferred pH range of the
buffer is between 2.6 and 2.85, preferably pH 2.7-pH 2.8, and is
preferably a citrate buffer. It will be appreciated that the acid will
generally be in the form of an aqueous solution, preferably in
deionised water, unless otherwise indicated. Citrate buffer is
preferred. Where acetate buffer is used, this may typically have a pH
range of 3.5 to 5.5, while citrate-phosphate buffer may typically have
a pH range of 2.75 to 7.0.
[0017] It will be understood that a solution in which the solvent is
aprotic cannot have a pH, as this is a measurement of the H.sup.+ ion.
However, where such a solution is at least partially miscible with an
acid, or acidic buffer, and such is present, then attempts to measure
the pH will yield a result. Preferred formulations of the invention are
made up as topical administration forms, and will generally comprise a
majority of buffer, or ionic solution, but will always comprise aprotic
solvent, so that only an apparent, rather than an absolute, pH can be
measured, as the measured pH relates only to the ionic component. A
suitable means for measuring apparent pH is with the Jenway 3320 pH
meter. Accordingly, the result may not have the meaning normally
ascribed to an ionic solution, especially where the amount of acid or
buffer is small, but the significance is that, insofar as any ionic
environment is present, that environment is acidic. As the amount of
acid increases, so the apparent pH becomes more equivalent to pH. While
not being bound by theory, it is likely that ingenol angelate is
primarily dissolved in the aprotic solvent, as it has very low
solubility in water. Subsequent addition of the ingenol angelate
solution in solvent to an acidified ionic solution allows a suitable,
optionally aqueous, ionic solution of ingenol angelate to be prepared,
thereby avoiding dissolution of ingenol angelate directly in a protic
solvent, which is when the greatest amount of rearrangement appears to
take place. Thus, contact with a protic solvent can immediately result
in the formation of the other isoforms, but this can be minimised if a
small amount of acid or acidic buffer, which terms are used
synonymously herein unless otherwise apparent, is added. Even the act
of dissolution in protic solvents, given the length of time and
conditions necessary, can lead to undesirably high levels of isoforms
forming, such is the susceptibility of ingenol angelate to
rearrangement.
[0018] The aprotic solvent and the acid are at least partially
compatible, in that a stable preparation of the two can be formed. The
acid and solvent are preferably miscible, and are preferably miscible
at all ratios. In particular, it is generally preferred to add a small
amount of buffer to the solvent during, or shortly after,
solubilisation of the ingenol angelate, in order to keep the apparent
pH at a relatively low level. Subsequently, it may be desirable to make
up the solubilised ingenol angelate in an excess of the buffer that was
used during the initial solubilisation. Stable preparations made up
with an excess of buffer are illustrated in Example 9, below.
[0019] It will be appreciated that it is preferred that the acid and
solvent be sufficiently miscible to be able to form a single phase,
although immiscible, or less miscible, solvents and acids may be
prepared in the form of emulsions or micro-emulsions. Such emulsions
can be stable, but the provision of a mixture of solvent and acid as a
single phase generally further minimises any risk of angelate
rearrangement.
[0020] Solvents that are particularly useful in the present invention
are those which exhibit both hydrophilic and lipophilic traits, such as
ring systems which are preferably homocyclic, and which have hydroxy
groups substituted thereon but separated by at least one carbon atom
from the ring structure. A particularly preferred example of such a
solvent is benzyl alcohol.
[0021] Although it is possible to use an acid rather than a buffer, it
is generally preferred to use an acidic buffer to minimise the
fluctuation in pH. As such, it will be appreciated that, whilst the
term `buffer` will generally be used herein, this term also encompasses
acids and acid preparations, where appropriate. A particularly
preferred buffer is citrate buffer, pH 3 or lower, preferably pH 2.75.
In benzyl alcohol, a 2.5% w/w quantity of pH 2.5 citrate buffer will
generally yield an unmeasurable apparent pH but, at higher quantities,
yields a pH of around pH 3. The relationship between pH of buffer and
apparent pH is explored in the accompanying Examples. At low quantities
of buffer when dissolving I3A in the solvent, it is simply preferred to
keep the environment acidic, and the nature of the preferred buffer at
these levels is similar to the nature of the preferred buffer when
subsequently diluting the formulation for use. It is generally
preferred to acidify the solvent, preferably benzyl alcohol, with an
amount of acidic buffer, preferably between 1 and 10% by weight, more
preferably between 2 and 5%, prior to addition of I3A.
[0022] While the formulation does not have to be diluted for use, it is
generally the case that I3A is a potent substance, and stock solutions
of I3A in solvent, preferably benzyl alcohol, may be made up for
storage, preferably at 8.degree. C. or below. Such stock solutions may
then be diluted, preferably with buffer, as desired, when making up any
final formulation or preparation.
[0023] The amount of buffer used when solubilising the ingenol angelate
can vary between about 0 and 100%. When the amount is 0, it is
preferred to add a quantity of buffer shortly after adding the ingenol
angelate to the solvent, in order to minimise the likelihood of any
rearrangement taking place. It is generally preferred to avoid using
amounts of buffer greater than 100% by weight of the solvent, as
dissolution directly into the buffer is generally not readily
achievable. It is preferred to employ the buffer as a means to keep the
apparent pH of the solvent at a low level, without providing any
substantial amount of protic solvent during dissolution of the ingenol
angelate. Once the ingenol angelate has been substantially dissolved,
then it is possible, and may even be desirable, to make up the
formulation with an excess of buffer comprising, if desired, other
optionally protic constituents, such as antibiotics, for example.
Preferred levels of buffer are in the region of 0.5%-10%, and
preferably between 1% and 5%, with about 2-3% being most preferred
during the dissolution phase. The dissolution phase comprises
dissolving at least a majority of the ingenol angelate in the solvent,
and preferably at least 95% w/w ingenol angelate in the solvent, more
preferably at least 99% w/w.
[0024] Formulations of the present invention may be used directly, or
may be stored for future use. In addition, formulations of the present
invention may provide a base formulation which can then be further
modified prior to use. For example, as described above, the formulation
may be made up in an excess of buffer or may be formulated into a gel,
for example.
[0025] It has also been found that formulations of the present
invention are generally more stable at lower temperatures. Particularly
preferred formulations of the present invention, such as those
comprising benzyl alcohol and citrate buffer, may exhibit substantial
stability at temperatures as high as 40.degree. C. but, in general,
increasing stability is observed at temperatures below room temperature
and pressure (RTP), and the greatest stability is observed at
temperatures below about 8.degree. C. Freezing does not appear to
enhance stability so that, in general, the greatest stability is
achieved simply by placing formulations of the invention in a
conventional refrigerator at a temperature of between about 2.degree.
C. and 8.degree. C.
[0026] The present invention further provides a process for preparing a
solution of ingenol angelate, comprising dissolving the ingenol
angelate in a pharmaceutically acceptable, aprotic solvent, said
formulation further comprising a pharmaceutically acceptable acidifying
agent which is at least partially compatible with the solvent and which
provides the formulation with an apparent pH of no greater than 4.5,
said acid being added with, before, or after the ingenol angelate.
[0027] In an alternative, the present invention provides a process for
preparing a solution of ingenol angelate, comprising dissolving the
ingenol angelate in a pharmaceutically acceptable, aprotic solvent,
said process comprising the addition of a pharmaceutically acceptable
acidifying agent which is at least partially compatible with the
solvent and which provides the formulation with an apparent pH of no
greater than 4.5, said acidifying agent being added with, before, or
after the ingenol angelate. The acidifying agent is preferably a buffer.
[0028] It is preferred to add the acid, or buffer, sufficiently soon
after addition of the I3A to ensure that no more than about 1%, and
preferably no more than about 0.5%, of the `b` isoform rearranges into
the `a` isoform. Preferably, the acid or buffer is added to the solvent
before adding the I3A, although all three ingredients may be combined
at the same time. This latter is the least preferred option.
[0029] This process may also be used for the preparation of ingenol
angelate formulations using other compounds and solvents, such as
polyethylene glycol, where direct solubilisation may be associated with
an unacceptable level of rearrangement. Although I3A can dissolve in
PEG, it takes in the region of an hour at elevated temperature, which
generally leads to the generation of unacceptable levels of the `a`
isoform. If the I3A is dissolved in buffered benzyl alcohol first, this
can then be introduced directly into the PEG, without the prolonged
exposure to heat. As only enough benzyl alcohol is needed to solubilise
the I3A, then the total amount of benzyl alcohol in the final PEG
formulation need only be in the region of 1% w/w or less.
[0030] These formulations may be kept for sustained periods, especially
when kept at temperatures of 8.degree. C. or lower. Preferred
compositions see no more than about 1%, and preferably no more than
about 0.5%, rearrangement of the `b` isoform to the `a` isoform after 3
months, more preferably 6 months.
[0031] There is further provided the use of a formulation of the
invention in the treatment of a skin cancer.
[0032] The invention also provides the use of ingenol angelate in the
manufacture of a medicament for the treatment or prevention of a skin
cancer, wherein the ingenol angelate is dissolved in a pharmaceutically
acceptable, aprotic solvent, said formulation further comprising a
pharmaceutically acceptable acidifying agent which is at least
partially compatible with the solvent and which provides the
formulation with an apparent pH of no greater than 4.5.
[0033] Suitable cancers for treatment in accordance with the present
invention include squamous and basal cell cancers.
[0034] It will be appreciated that `treatment`, as used herein,
includes both therapy and prophylaxis.
[0035] The present invention also provides a method of treating a
subject suffering from a cancerous skin condition, comprising the
topical application of a therapeutically effective amount of a
composition of the invention to the area of the cancerous condition.
[0036] Suitable subjects for treatment are mammals, including humans,
primates, livestock animals (including cows, horses, sheep, pigs and
goats), companion animals (including dogs, cats, rabbits, guinea pigs),
captive wild animals, and laboratory animals, such as rabbits, mice,
rats, guinea pigs and hamsters. The compositions of the present
invention are particularly suitable for the treatment of human skin
cancers.
[0037] It will be appreciated that the formulations of the present
invention may be used in any suitable cancer prophylaxis or treatment.
Administration forms may be any suitable, and include creams, gels,
ointments, lotions, sprays, lacquers and paints for topical
application, powders, solutions and suspensions for the airways,
solutions and emulsions for injection, capsules, syrups and elixirs for
oral administration, and pessaries and suppositories. Other suitable
administration forms will be readily apparent to those skilled in the
art, and may include transdermal patches, for example. In a preferred
embodiment of the present invention, the ingenol angelate formulations
are formulated for topical administration.
[0038] In all cases, the initial formulation is as a formulation of the
invention. The formulation may be made up into the final form either
just before use as soon as desired after preparation of the
formulation, but will usually remain a formulation of the invention at
all times.
[0039] Formulations may comprise additional ingredients, as discussed
below. It is particularly preferred to employ antioxidants, as these
appear to provide enhanced stability to the formulations. Suitable
examples of antioxidants include retinol, ascorbic acid, lycopene,
butylated hydroxytoluene, and tocopherol.
[0040] The amount of ingenol angelate required for pharmaceutical
efficacy will be apparent to those skilled in the art, and may be
adapted according to physiological parameters, such as age, weight and
sex of the patient, as well as the size of any lesion. In general, an
amount of ingenol angelate suitable to provide between about 0.01 .mu.g
cm.sup.-2 to about 1 mg cm.sup.-2 may be employed, with a range of 0.1
mg cm.sup.-2 to about 100 .mu.g cm.sup.-2 being more preferred. In the
accompanying Examples, a formulation providing 15 .mu.g cm.sup.-2 was
used, but formulations of 1 .mu.g cm.sup.-2, or less, have been found
to be effective. In the alternative, formulations of the invention may
contain I3A in an amount of from 0.001% (w/w) to 0.15% (w/w), more
preferably up to about 0.1-0.12% (w/w).
[0041] Topical formulations are a preferred embodiment of the present
invention. In this regard, a heretofore unrecognised property of the
ingenol angelates is particularly useful, in that it has been found
that they have vasoconstrictive properties. Accordingly, systemic
distribution of the active ingredient is minimised, owing to the
reduced blood flow in the vicinity of treatment.
[0042] It will be appreciated that the nature of the formulation will
determine the rate of permeation across the skin. As such, it is
generally preferred that the formulation be prepared such that a rate
of permeation of at least about 11 ng cm.sup.-2 h.sup.-1 is achieved.
There is no special upper limit, although it is generally preferred
that this not exceed around 1 .mu.g cm.sup.-2 h.sup.-1.
[0043] Topical formulations may take any suitable form. In general, it
is preferred that they exhibit some level of viscosity, in order that
they can be targeted at the desired area without running off.
Accordingly, it is generally preferred to formulate ingenol angelate as
creams, gels, ointments, and paints. Given the potency of ingenol
angelate, paints may be employed, as they may be applied sparingly,
depending on levels of the active ingredient.
[0044] Poloxamers may be used in preferred formulations of the present
invention. They are co-polymers which consist of a hydrophobic
poloxypropylene (POP) molecule sandwiched between two hydrophilic
molecules of poloxyethylene (POE). Thus, they have the ability to
solubilise lipophilic drugs within the hydrophobic core. Furthermore,
poloxamer based aqueous gel formulations exhibit thermo-rheological
properties, which may be advantageous for localised, sustained delivery
of drugs. Above a certain temperature, known as the critical micelle
temperature (cmt), the viscosity of the poloxamer gel increases
dramatically. An increase in viscosity leads to a decrease in the
diffusion of any drugs dissolved in the gel which slows down the
release of drug from the gel and leads to sustained delivery. The
increase in viscosity may also provide a prolonged, localised `depot`
at the site of action.
[0045] The cmt is dependent on a number of variables such as
concentration of poloxamer and other additives such as propylene
glycol. Ideally, the cmt should be at a temperature such that the
formulation can be injected into the lesion as a liquid (ease of
administration) and upon contact with body temperature a gel is formed
with the aim of achieving a localised, sustained delivery of the drug.
Five poloxamers are listed in the USP, and include poloxamer 188 and
poloxamer 407. Poloxamer 188 has been approved as an excipient for IV
formulations (http://www.accessdata.fda.gov).
[0046] Poloxamer gels have been used for subcutaneous delivery of
insulin (Barichello et al., 1999) and other drug delivery systems for
percutaneous use (Tobiyama et al., 1994). One particular copolymer,
poloxamer 407 has been administered subcutaneously for the slow release
of peptides and therapeutics proteins, which included interleukin-2 and
human growth hormone (Morikawa et al., 1987; Katakama et al., 1997).
Following administration, the gels slowly released the entrapped
protein molecules over a period of 1-2 days. Furthermore, a substantial
fraction of this poloxamer eventually underwent renal excretion.
[0047] Poloxamers are generally regarded as non-toxic and non-irritant
materials. Animal toxicity studies, with dogs and rabbits, have shown
poloxamers to be non-irritant and non-sensitising when applied, in 5%
w/v and 10% w/v concentration, to the eyes, gums and skin. In a 14-day
study of intravenous administration to rabbits, at concentrations up to
0.5 g/kg/day, no overt adverse effects were noted. A similar study with
dogs also showed no adverse effects at dosage levels up to 0.5
g/kg/day. Furthermore, no haemolysis of human blood cells was observed
over 18 hours at 25.degree. C., with 0.001-10% w/v poloxamer solutions
(Wade and Weller, 1994). However, hyperlipidemia in rats has been
reported when an intraperitoneal (IP) injection (1.0 g/kg) of poloxamer
407 was introduced (Wasan et al., 2003).
[0048] Oils may also be used in the present invention. The use of an
emulsion based intralesional formulation has been reported for the
treatment of psoriasis (Ho et al., 1990). Prior to administration, a
vehicle, such as polyoxyethylated castor oil, is normally diluted with
saline to form the emulsion. However, our studies have shown that
dilution of I3A with normal saline increases the conversion of isoform
`b` to `a`. This conversion may be minimised if the administration time
of the formulation is short.
[0049] There are a number of lipophilic products that are formulated as
oily solutions for intramuscular administrations (IM), for example
Prolixin Enanthate (Bristol Myers Squibb). The vehicle (oil) used
varies widely from vegetable oils such as arachis oil (used with benzyl
benzoate in Dimercaprol Injection B.P.) and sesame oil (used in depot
injections of Fluphenazine Enanthate Injection B.P). The use of
oleaginous vehicles may slow absorption due to delayed partitioning of
the drug from the oil to the aqueous body fluids (Ford, 1987). When
injected into an aqueous environment (such as muscle tissue) a
relatively lipophilic drug such as I3A, dissolved in an oil phase, will
have a tendency not to leave the oil and `instantaneously` partition
into the aqueous phase. In this way a sustained release effect can be
achieved.
[0050] Buccal formulations may also be employed. Transmucosal delivery
of therapeutic agents is a popular administration form, because mucous
membranes are relatively permeable, allowing for the rapid uptake of a
drug into the systemic circulation and avoiding first pass metabolism.
Transmucosal products can be designed to be administered via the nasal
route and oral/buccal route using mucoadhesives. In the development of
these drug delivery systems, mucoadhesion of the device/formulation is
a key element. The term `mucoadhesive` is commonly used for materials
that adhere to the mucin layer of a biological membrane. Mucoadhesive
polymers have been utilised in many different dosage forms in efforts
to achieve systemic and localised delivery of drugs through the
different mucosae. These dosage forms include tablets, patches, tapes,
films, semisolids and powders.
[0051] To serve as mucoadhesive polymers, the polymers should possess
physicochemical features such as being predominantly anionic with
numerous hydrogen bond-forming groups, suitable surface properties for
wetting mucus/mucosal tissue surfaces and sufficient flexibility and
length (molecular weight) to penetrate the mucus network or tissue
crevices. Diverse classes of polymers have been reported as potential
mucoadhesives such as carbomers (polyacrylic acids), hydroxypropyl
methylcellulose (HPMC) as well as naturally occurring polymers, such as
hyaluronic acid and chitosan.
[0052] Preparation of suitable formulations is within the skill of
those in the art, and suitable excipients for inclusion in any such
formulation include, for example, gellants, viscosifiers, penetration
enhancers, preservatives, such as antibiotics and antifungals, and
cosmetic ingredients, such as scents and colourings.
[0053] Suitable gelling agents include: water soluble cellulose derived
polymers, such as hydroxyalkyl cellulose polymers (e.g.
hydroxymethylcellulose, hydroxyethylcellulose, hydroxypropylcellulose
and hydroxypropylmethylcellulose), carboxymethyl cellulose,
methylhydroxyethyl cellulose and methyl cellulose, carbomer (e.g.
carbopol); and carrageenans. The gelling agent may be added in any
suitable amount, such as 1-5% (w/w). Preferred gelling agents are
cellulose derived, most preferably hydroxyalkylcellulose, particularly
hydroxyethylcellulose.
[0054] Suitable preservatives will be apparent to those skilled in the
art, and include the parabens (methyl, ethyl, propyl and butyl),
benzoic acid and benzyl alcohol. Preservatives employed solely for that
purpose will generally form 1% (w/w) or less of the final topical
formulation.
[0055] Suitable penetration enhancers include isopropyl alcohol,
sulphoxides (such as dimethylsulphoxide, DMSO), Azones (e.g.
laurocapram), pyrrolidones (for example 2-pyrrolidone), alkanols (e.g.
decanol), and glycols (for example propylene glycol).
[0056] Preferred compositions of the invention comprise:
a) I3A;
[0057] b) penetration enhancer;c) preservative;d) gelling agent; ande)
buffer;wherein the composition has an apparent pH of between 3 and 4,
inclusive.
[0058] A particularly preferred composition comprises:
a) 0.1% (w/w) I3A;b) 30% (w/w) isopropyl alcohol;c) 0.9% (w/w) benzyl
alcohol;d) 1.5% (w/w) hydroxy ethyl cellulose; ande) 67.5% (w/w)
citrate buffer pH 3, preferably pH 2.75.
PLANTS Profile for Euphorbia peplus (petty spurge) | USDA PLANTS
plants.usda.gov/java/profile?symbol=EUPE6
Euphorbia peplus | Wildflowers of the Pacific Northwest
Euphorbia peplus. Petty Spurge. Erect, hairless, yellow-green plant
with milky sap. Stem hairless, 4–14 in. tall. Leaves with short
petioles, smaller at top ...
www.pnwflowers.com/flower/euphorbia-peplus
Calflora: Euphorbia peplus
Euphorbia peplus, a dicot, is an annual herb that is not native to
California; it was introduced from elsewhere and naturalized in the
wild. ...
www.calflora.org/cgi-bin/species_query.cgi?where...3561
Euphorbia Family (Euphorbiaceae)
Petty spurge (Euphorbia peplus), an erect garden weed in southern
California with alternate leaves and milky sap. Originally native to
Europe, this prolific ...
waynesword.palomar.edu/trmar98b.htm
http://cancerfighter.wordpress.com/2008/06/03/radium-weed-euphorbia-peplus-for-skin-cancers/
Radium
weed (Euphorbia peplus) for skin cancers
Posted by cancerfighter on June 3, 2008
The Big Book:
Cancer: The Complete Recovery Guide
“This book tells me everything. Why didn’t my doctor tell me this?”-
Rev. Bill Newbern
RADIUM WEED
A story from the Australian Naturopathic Network notes the recent
announcement that Euphorbia peplus (commonly known as Radium Weed) has
been found “to cause sun spots, Basal Cell Carcinoma
(BCC) and Squamous Cell Carcinoma (SCC) to disappear, and drop off!”
Brian McDermott, the commentator presenting the story, said, “Our
grandmothers taught us this over half-a-century ago, and it was well-
known in the bush, where we grew up!” He predicts the so-called experts
will now be stumbling
over each other in the race to patent their “discovery.”
http://species.wikimedia.org/wiki/Euphorbia_peplus
Euphorbia
peplus
Classification System: APG III (down to family level)
Regnum: Plantae
Cladus: Angiosperms
Cladus: Eudicots
Cladus: Core eudicots
Cladus: Rosids
Cladus: Eurosids I
Ordo: Malpighiales
Familia: Euphorbiaceae
Subfamilia: Euphorbioideae
Tribus: Euphorbieae
Subtribus: Euphorbiinae
Genus: Euphorbia
Species: Euphorbia peplus
Patents
Anti-cancer compounds
US7410656
Inventor(s): AYLWARD JAMES HARRISON
Classification:- international: A61K31/225;
A61K36/47; A61K31/21; A61K36/185; (IPC1-7): A61K31/225; A61K35/78-
European: A61K31/225; A61K36/47
Abstract -- This invention
relates to a compound or group of compounds
present in an active principle derived from plants of species
Euphorbia
peplus, Euphorbia hirta and Euphorbia drummondii, and to
pharmaceutical
compositions comprising these compounds. Extracts from these plants
have been found to show selective cytotoxicity against several
different cancer cell lines. The compounds are useful in effective
treatment of cancers, particularly malignant melanomas and squamous
cell carcinomas (SCCs). In a preferred embodiment of the invention, the
compound is selected from the group consisting of jatrophanes,
pepluanes, paralianes and ingenanes, and pharmaceutically-acceptable
salts or esters thereof, and more particularly jatrophanes of
Conformation II.
Chinese medicinal preparation for
treating esophagus cancer
CN101590176
Abstract -- The invention
discloses a Chinese medicinal preparation for
treating esophagus cancer. The Chinese medicinal preparation adopts a
method of treating both primary and secondary symptoms to strengthen
body resistance and eliminate pathogenic factors so as to achieve the
aim of treating esophageal cancer by inhibiting the proliferation of
cancer cells and the killing cancer cells. The inventor takes ancestral
secret prescriptions and Chinese traditional medical theories as
foundation, and prepares the Chinese medicinal preparation according to
the monarch-minister-assistant-guide composition principle and
compatibility of Chinese prescriptions. By taking red sage roots,
scorpion, toad skin, airpotato yam and nidus vespae as monarch
medicines, taking arrowhead leaves, white stiff silkworms,
sun
euphorbia herbs, house lizards, kiwi roots, walnuts and
peperomia
dindygulensis as minister medicines, assisting the monarch medicines
and the minister medicines with Chinese olive, seaweed, disporum
leschenaultianum, gynura bicolor grass and rhizoma bolbostemmae, and
taking dried persimmon frost, magnolia officinalis, rhizoma
anemarrhenae, hippocampus, cordyceps sinensis and musk as guide
medicines, the Chinese medicinal preparation is prepared through
scientific compatibility and a preparation process.
Medicine for treating breast cancer
CN101780187
Abstract -- The invention
relates to a medicine for treating breast
cancer, which comprises the following components by weight ratio: 70-90
Euphorbia pallasie Steud, 20-30
rhizoma arisaematis, 20-30 pinellia
tuber, 5-15 golden thread, 3-7 rhubarb and 3-7 licorice. The invention
is prepared by Chinese herbal medicines, has low making cost, low cost
of treatment, calm nature, and no toxicity and side effects. At least
50g of liquid finished product or 3-4 capsules are taken once and taken
three times a day, the medicine can be safely and reliably taken by
patients, and the curative effect is obvious; and the clinical trial
results for more than 120 breast cancer patients show that the total
effective rate is 98%, and the cure rate is over 85%.
Extraction and preparation method of
total phenol of compound abnormal savda munziq
CN101757128 (A)
Abstract -- The invention
provides an extraction and preparation method
of total phenol of compound abnormal savda munziq, wherein the abnormal
savda munziq is prepared by the following steps of: mixing ten kinds of
medicines such as cordial fruits, bugloss, licorice, diantaceae,
euphorbia humifusa and the like
according to the proportion, decocting,
soaking, filtering, decompressing, condensing and drying the mixture to
obtain an extract solid; crushing the extract solid to obtain dry
powder; adding hot water into the dry powder and dissolving and
filtering; adding ethanol into filtrate to precipitate; stirring,
standing and filtering the precipitation; decompressing and condensing
the filtrate; treating the filtrate through a polyamide; sequentially
eluting the filter with water and dilute ethanol; discarding eluent;
eluting with high-concentration ethanol; and decompressing, condensing,
drying and crushing the eluent to obtain a total phenol product with
stronger in vitro anti-cancer activity, wherein the content of the
total phenol is over 30 percent and the content of total flavone is
over 13 percent. The extraction and preparation method has low cost,
simple process, practicability and safety; and the prepared total
phenol has excellent stability and can be prepared into tablets,
capsules, oral liquid, granules, decoction, syrups, pills and the like
for use.
Pharmaceutical composition with
effects of resisting cancer and alleviating pain
CN101745065
Abstract -- The invention
discloses a pharmaceutical composition with
effects of resisting cancer and alleviating pain, which is prepared
from 40 traditional Chinese medicines: toad venom, pangolin scales,
centipede, scorpion, honeycomb, leech, szechuan aconite, wild aconite,
arisaema tuber, tuber pinellia,
euphorbia
kansui, knoxia corymbosa,
rhizoma sparganii, rhizoma zedoariae, polyporus umbellatus, rhubarb,
amur corktree bark, baikal skullcap root and the like. The
pharmaceutical composition of the invention has obvious curative
effects on various cancers of early, middle and late stages, and has
the efficacies of resisting cancer and inhibiting tumor, promoting
blood circulation and removing stasis, removing the necrotic tissue and
promoting granulation, and promoting circulation of qi and relieving
pain. The pharmaceutical composition of the invention controls cancer
pain by resisting cancer and inhibiting tumor, draws out cancer poison,
enables the tumor to shrink and disappear to achieve the purposes of
improving living quality and prolonging life, and has convenient and
safe use and no toxic and side effect. The efficacies are better by
pasting the pharmaceutical composition of the invention on
corresponding points of a human body.
Medicament for treating lung cancer
CN101703726
Abstract -- The invention
relates to a medicament, in particular to a
medicament for treating lung cancer, which solves the problem of
inapparent curative effect of the conventional medicaments for treating
the lung cancer. The medicament comprises is prepared from the
following raw materials by conventional method:; mongolian dandelion
herb, centipede, scorpion, rhizoma pleionis, black nightshade herb,
bittersweet herb,
sun euphorbia
herb, Indian mockstrawberry herb, toad
venom, sarcandra glabra, green tangerine peel, Indian buead, oriental
waterplantain rhizome, szechwon tangshen root, villous amomum fruit,
plantain seed, glossy ganoderma, honeysuckle flower, weeping forsythiae
capsule, chicken's gizzard-membrane, largehead atractylodes rhizome,
immature bitter orange, glossy privet fruit, radix astragali, Chinese
atractylodes rhizome, katsumade galangal seed, Chinese sage herb, radix
asparagi, blackberrykiky rhizome, cassia twig, Chinese magnoliavine
fruit, semen armeniacae amarum, radix scutellariae, common coltsfoot
flower, bulbus fritillariae thunbergii, radix glycyrrhizae preparata,
peach seed, danshen root, rosewood heart wood, szechuan lovage rhizome,
sessile stemona root,; pinellia tuber, tatarian aster root, snakegourd
fruit, red paeony root, perilla fruit, radish seed, pepperweed seed,
greenish lily bulb, scorch-fried crataegus, scorch-fried medicated
leaven, hordeum vulgare, longstamen onion bulb, eucommia bark, south
dodder seed, tangerine peel, costustoot, nutgrass galingale rhizome,
heartleaf houttuynia herb, indigowoad root, dwarf lilyturf tuber,
coastal glehnia root, virgate wormwood herb, hairyvein agrimonia herb
and bud and spreading hedyotis herb.
Traditional Chinese medicine for
treating hepatitis B, cirrhosis, liver cancer and liver ascites
CN101618172
Abstract -- The invention
relates to a traditional Chinese medicine for
treating cirrhosis, which is prepared by grinding traditional Chinese
medicines, i.e. cornu bubali, rhubarb, pariphyllin, melanterite, colla
corii asini, rhizoma zedoariae, turtle shell, radix morindae
officinalis, cordyceps sinensis, and the like, into powder to be
encapsulated, wherein if components, i.e. the large cornu bubali, the
pariphyllin and the melanterite, are added to the traditional Chinese
medicines, the traditional Chinese medicine for treating the cirrhosis
can be used for treating hepatitis B; if the melanterite is removed
from the traditional Chinese medicines, the traditional Chinese
medicine for treating the cirrhosis has good treatment effect on liver
cancer; ascites can be caused by the cirrhosis and the liver cancer,
and the traditional Chinese medicine for treating the ascites is
prepared from morning glory,
euphorbia
kansui, yam, matrimony vine,
cinnamon, and the like. The traditional Chinese medicines have the
advantages of least toxic side effect, tonification and purgation in
combination, long-term administration and high cure rate and effective
rate.
Chinese medicinal preparation for
treating esophagus cancer
CN101590176 (A)
Abstract -- The invention
discloses a Chinese medicinal preparation for
treating esophagus cancer. The Chinese medicinal preparation adopts a
method of treating both primary and secondary symptoms to strengthen
body resistance and eliminate pathogenic factors so as to achieve the
aim of treating esophageal cancer by inhibiting the proliferation of
cancer cells and the killing cancer cells. The inventor takes ancestral
secret prescriptions and Chinese traditional medical theories as
foundation, and prepares the Chinese medicinal preparation according to
the monarch-minister-assistant-guide composition principle and
compatibility of Chinese prescriptions. By taking red sage roots,
scorpion, toad skin, airpotato yam and nidus vespae as monarch
medicines, taking arrowhead leaves, white stiff silkworms,
sun
euphorbia herbs, house lizards, kiwi roots, walnuts and
peperomia
dindygulensis as minister medicines, assisting the monarch medicines
and the minister medicines with Chinese olive, seaweed, disporum
leschenaultianum, gynura bicolor grass and rhizoma bolbostemmae, and
taking dried persimmon frost, magnolia officinalis, rhizoma
anemarrhenae, hippocampus, cordyceps sinensis and musk as guide
medicines, the Chinese medicinal preparation is prepared through
scientific compatibility and a preparation process.
Medicated wine for treating cancer and
tumor and method for preparing same
CN1966008
Abstract -- The invention
discloses a Chinese medicinal liquor
preparation for treating cancer and its preparing process, wherein the
liquor is prepared from the following raw materials herbs:
dysosmapleiantha woods 10-15g, Rhodoendron lacteum 10-15g, Pediculus
melo 3-5g, hairy deerhorn 10-1.5g, barbat skullcap 20-30g, Japanese
felt fern leaf. 15-20g, seaweed 15-20g,
euphorbia helioscopia 40-60g,
wasp's nest 10-15g, Pygmy arrowhead 10-5g, airpotato yam 40-60g, walnut
kernel 40-60g, acanthopanax root 40-60g, ear of wheat 40-60g, toad
12-15g, buthus martensi kirsch 6-8g, Chinese date 15-20g, white-stiff
silkworm 9-15g, house lizard 6-10g, leech 6-10g, musk 9-15g, bat's
feces 30-40g, licorice root 6-10g, Chinese actinidia root 40-60g,
osmanthus flower wine 500-550ml, and white spirit 4500-5000ml.
Traditional Chinese medicine for
treating digestive cancer and its producing method
CN101057945
Abstract -- The invention
relates to a Chinese medicament for
preventing and treating digestive tract cancer and process for
preparation, wherein the medicament is prepared from astragalus root,
green tangerine orange peel, banksia rose, linaloe, clove, zedoary,
burred tuber, Ligusticum wallichii, pinellia tuber, white mustard seed,
euphorbia helioscopia, radical
lobelia, barbat skullcap, oldenlandia,
selfheal, dried body of ground beetle, leeches and water.
Medicine for treating cancer and
preparing method thereof
CN101143167
Abstract -- The invention
relates to a drug for remedying the cancer
and especially indicates a cancer-washing cure drug of Hunan He
pharmacy for remedying the cancer. The invention has good curative
effect within the following weight range of 7 to 15 portions of
duchesneas, 7 to 15 portions of
sun
euphorbia, 7 to 15 portions of
prepared pinellia tubers, 7 to 15 portions of alums, 5 to 15 portions
of rhubarbs and 450 to 550 grams of liquor. The preparation method of
active components of the drug of the invention is as follows that the
raw materials of the duchesnea, the
sun
euphorbia, the prepared
pinellia tuber, the alum and the rhubarb are washed cleanly for using;
the raw materials are dipped in the liquor of high quality in an urn;
the drug can be taken out for using after one month.
A Chinese traditional external use
medicine for treating medium term and late brain tumor
CN1943644
Abstract -- This invention
relates to a Chinese traditional external
use medicine for treating medium term and late brain tumor. It includes
the main medicine and excipient, the said main medicine is composed
with the flowing raw materials by the unit of weight: whole
scorpion(25-35), radix aconiti sinensis (16-20), radix aconiti
agrestis16-20), meretrix shell(16-20), putamen manidis (15-25), bombyx
batryticatus (10-20), dog button (4-8), gecko (3-7), argum groundsel
herb (3-8), knoxia root (3-7),
Euphorbia
kansui Liou (2-6), galla
sinensis (1-3), twotooth achyranthes root (1-3), borneol (0.5-1.5),
catharsius (0.5-1.5), blister beetle (0.5-1.5), camphor (5-15), musk
(6-10) and calculus bovis (10-14). The said excipient is prepared by
the following raw materials through using the unit of weight: safflower
(3.7), glycyrhiza(3.7), centipede (3.7), succus spissatus of Shanxi
vinegar(486 use size as its unit). After preparing the said main
medicine and excipient, externally apply to the affected part, the
medicine through penetration will make the hydrocephalus discharged,
epilepsia eliminated, so to cut off the existence of the cancer cell
and kill the target cell of the cancer cell, and at the same time make
the dead cancer cell excreted outside of the body, so to have the
organist immunity improved, and finally reach the aim of the recovery
of the brain tumor.
DITERPENES FROM EUPHORBIA KANSUI AND
THEIR USE
WO2006116897
Abstract -- Novel diterpenes
with antitumor activity of formula (I),
wherein R1 ~ R3 represent aliphatic group; or represent group of RCO-,
in which R represents aliphatic group, aryl, or heteroaryl. The
compounds of the present invention are prepared by extracting roots of
euphorbia kansui with organic
solvent (chloroform, ethyl acetate and
butanol) and treating the extract by conventional methods. The
compounds of the present invention have cell proliferation inhibiting
activity, and can inhibit the proliferation of specific cancer cell
lines via inhibition of topoisomerase. These compounds can be used for
preparing medicaments for treating malignant tumor.
DITERPENES FROM EUPHORBIA KANSUI AND
THEIR USE
WO2006116897
Abstract -- Novel diterpenes
with antitumor activity of formula (I),
wherein R1 ~ R3 represent aliphatic group; or represent group of RCO-,
in which R represents aliphatic group, aryl, or heteroaryl. The
compounds of the present invention are prepared by extracting roots of
euphorbia kansui with organic
solvent (chloroform, ethyl acetate and
butanol) and treating the extract by conventional methods. The
compounds of the present invention have cell proliferation inhibiting
activity, and can inhibit the proliferation of specific cancer cell
lines via inhibition of topoisomerase. These compounds can be used for
preparing medicaments for treating malignant tumor.
Chinese medicine for treating cancer
CN1698738
Abstract-- The invention
relates to a Chinese medicine for treating
cancer which is prepared from the following raw materials, scorpion,
house lizard, dysosmapleiantha woods,
creeping
euphorbia, hairy
deerhorn, black-tail snake, long-nosed pit viper, toad skin, centipede,
batryticated silkworm, leeches, earthworm, seaweed, wood louse,
pangolin scales, safflower, notoginseng, dry human placenta,
decapetalous daesalpinia and gadfly.
Anti-cancer compounds
US7410656
Abstract -- This invention
relates to a compound or group of compounds
present in an active principle derived from plants of species
Euphorbia
peplus, Euphorbia hirta and Euphorbia drummondii, and to
pharmaceutical
compositions comprising these compounds. Extracts from these plants
have been found to show selective cytotoxicity against several
different cancer cell lines. The compounds are useful in effective
treatment of cancers, particularly malignant melanomas and squamous
cell carcinomas (SCCs). In a preferred embodiment of the invention, the
compound is selected from the group consisting of jatrophanes,
pepluanes, paralianes and ingenanes, and pharmaceutically-acceptable
salts or esters thereof, and more particularly jatrophanes of
Conformation II.
COMBINATION OF ACTIVE FRACTIONS FROM
THE PLANTS EUPHORBIA TIRUCALLI L AND FICOS CARICA L. AND METHOD OF
TREATING CANCER AND AIDS
WO2006007676
Abstract -- The present
invention refers to the combination of active
fractions from the plants
Euphorbia
tirucalli L. e Fícus carica
L. more particularly the pharmaceutical compositions comprising the
said combinations, which are useful for treatment of cancer and
Acquired Immunodeficiency Syndrome (AIDS). The present invention also
relates to the process of manufacture of the active fractions from the
plants.
Methods of stimulating the immune
system
US6844013
Abstract -- This invention
relates to a compound or group of compounds
present in an active principle derived from plants of species
Euphorbia
peplus, Euphorbia hirta and Euphorbia drummondii, and to
pharmaceutical
compositions comprising these compounds. Extracts from these plants
have been found to show selective cytotoxicity against several
different cancer cell lines. The compounds are useful in effective
treatment of cancers, particularly malignant melanomas and squamous
cell carcinomas (SCCs). In a preferred embodiment of the invention, the
compound is selected from the group consisting of jatrophanes,
pepluanes, paralianes and ingenanes, and pharmaceutically-acceptable
salts or esters thereof, and more particularly jatrophanes of
Conformation II.
Cancer treating medicine
CN1256146
Abstract -- The medicine of the
present invention is injecta, tablet or
capsule prepared with Herba Hedyotis Diffusae, Rhizoma Zedoariae,
Euphorbia fisheriana, peach
kernel and other over ten Chinese medicinal
materials and through water or alcohol extraction and other steps. It
may be used to prevent and cure lung cancer, gastric cancer, esophagus
cancer, etc.
Anticancer Chinese medicine and its
preparation
CN1205890
Abstract -- The medicine is
prepared by using
euphorbia
hilioscopia
juice, selfheal, Euphorbia fisheriana, greater celandine, ginseng, etc.
as material. During the preparation, euphorbia hiliscopia juice is
treated through modern biotechnology. The medicine can control and
eliminate cancer cells, eliminate cancer source, and prevent the
generation of cancer cell and it has obvious curative effect and no
serious effect to health cell. As one product of combined traditional
Chinese medicine theory and modern biotechnology, the medicine is
widely used in treating esophagns cancer, liver cancer, lung
cancer,etc. and may be also used in treating lymphosarcoma,
osteonyclitis, obstinats sore, etc.
Powerful anticancer plaster and its
preparing method
CN1112011
Abstract -- The powerful
anticancer plaster suitable for different
stages of cancer is prepared through segmental decoction of edible
plant oil, blushred rabdosis herb, dry toad skin,
sun euphorbia herb,
etc. at 300-350 and 350-400 deg.C, cooling to 200 deg.C, mixing with
fine powder processed from 9 Chinese-medicinal materials such as
pinellia tuber, prepared aconite root, cloves, Chinese blistering
beetle, etc., and stirring, and features high effective rate (96% for
esophagus, cardia, stomach and large intestine cancers and 80% for
liver and uterus cancer).