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THE USE FOR MALARIA

This treatment for malaria was, however, lost over time. It was only
rediscovered in an archeological dig in the 1970s where its medicinal use was
found in a recipe inside a tomb. The formula was dated back to 168 B.C.
where the Chinese chemist isolated the primary active ingredient from the
leafy portion of plant called A. annua L.

In 1972, scientists in the West called this crystalline compound "qinghaosu" or


"artemisinin". Since then, studies in China and Vietnam have confirmed that
artemisinin is a highly effective compound with close to 100 percent
response rate for treating malaria. It has the ability to destroy the
malaria parasite by releasing high doses of free radicals that attack the cell
membrane of the parasite in the presence of high iron concentration. In fact,
over one million malaria patients have been cured via this method. Their
symptoms also subsided in a matter of days.

However, the treatment using this herb to treat malaria is not approved for use
in the U.S.A due to the concern that it has a 21 percent recrudescent rate.
Scientists believe that this is more likely due to patients not taking the
compound for a long period. Many of them actually stop taking it as soon
as their symptoms subside.

Artemisinin comes in a few derivatives, including the oil soluble artemether,


which has been found to induce neurotoxic symptoms in animals in high dose
(but not reported in humans). For those who are technically inclined, the
activities of all artemisinin derivatives are dependent on their internal
endoperoxide bridge. It is therefore a close relative of hydrogen peroxide
therapy. While the exact mechanism is still under intense research, it has
been shown that this herb works via highly reactive oxygen-based free
radicals that becomes activated in the presence of iron. Iron is an oxidant, and
our body tries to protect us from excessive iron moving it to a binded state
such as hemoglobin and enzymes. The malaria parasite accumulates iron by
infecting iron-rich red blood cell. Excessive iron that is spilled onto the
surrounding tissues will activate the artemisinin to generate a burst of free
radicals that attack the iron rich cells, killing the parasite in the process.

In other words, this compound works well in an iron rich


environment (remember that malaria lives in the red blood cell
rich in iron) through the release of free radicals that serve to
damage the malaria organism. It is also interesting to note that drugs
known to work by enhancing oxygen radical effects such as doxorubicin can
enhance the effects of artemisinin.

For malaria, there is no resistance nor toxicity at the dosage of 3 grams,


(about 50mg/kg) administered over a 3 to 5 day period. It is especially useful
in the treatment of drug resistant malaria.
Outside of the United States, artemisinin is the number one natural herb used
for malaria treatment.

THE USE FOR CANCER


So far, the most extensive study on the use of Artemisinin as an anti-cancer
agent was carried out by bioengineering scientists Drs Narenda Singh and
Henry Lai of the University of Washington. This study was reported in the
Journal Life Science (70 (2001): 49-56).

Iron is required for cell division, and it is well known that many cancer cell
types selectively accumulate iron for this purpose. Most cancers have large
number of iron attracting transferring receptors on their cell surface compared
to normal cells. In laboratory studies of radiation, resistant breast cancer cells
that has high propensity for accumulating iron revealed that
artemisinin has 75 percent cancer cell killing properties in a 8
hours and almost 100 percent killing properties within 24 hours
when these cancer cells are "pre-loaded" with iron after incubation
with holotransferrin. On the other hand, the normal cells remained virtually
unharmed. Another study showing the effectiveness of artesunate in treatment
of cancer was also published in Oncology (April 2001: 18(4): 767-73).

The fact that iron content of cancer cells is high has also been used in another
anti-cancer therapy called Zoetron therapy, where iron containing cancer cells
are induced into motion using a magnetic device to induce resonance.
Resonance generate heat. Cancer cells are more sensitive to heat compared
to normal healthy cells. When cancer cells are heated to a certain
temperature, they die while normal cells still survive.

Artemisinin is effective against a wide variety of cancers as


shown in a series of successful experiments. The most effective
is leukemia and colon cancer. Intermediate activities were also
shown against melanoma, breast, ovarian, prostate, CNS and
renal cancer. Although artemisinin is insoluble in water, it is able to cross
the blood brain barrier (the water soluble artesunate is the weakness among
the derivates) and may be particularly suitable for curing brain tumors,
together with Poly-MVA (an metalo-vitamin)

In laboratory studies, iron needs to be added to enhance the


effects of artemisinin. Within the human body, no such addition
is necessary, as iron already exist in the body. It can also be taken
orally and therefore high doses are not required. Some people believe that as
nitrogen (tertiary amine) is absent in ART, cancer cells cannot get rid of it once
it enters into the cancer cell. As a result, ART stays in the cell much longer.
In addition to the high affinity for iron in aggressive cancer
cell types, most cancer cells also lack the enzyme catalayse
and gutathione peroxidase. Catalayse breaks down
hydrogen peroxide. A low catalayse content means a higher
hydrogen peroxide load, which can release superoxide free
radicals when properly stimulated to do so. This is in fact
one common mechanism among chemotherapeutic agents
as well as vitamin C. These traits make cancer cells more susceptible to
oxidative damage as compare to normal cells in the presences of hydrogen
peroxide. For this reason, administration of vitamin C in high dose is
acceptable, although a gap of 2-3 hours is preferred.

According to Dr Rowen , a naturally oriented medical doctor and editor of the


medical newsletter " Second Opinion" , the Hoang family of physicians in
Vietnam had used arteminisin in the treatment of cancer for years. They have
reported that, over a 10-year period, more than 400 patients were treated with
artemisinin in conjunction with a comprehensive anti-cancer program with 50
to 60 percent long-term remission rate. The safety record of artemisinin has
well been studied for over 25 years. No significant toxicity in short-term use
for malaria at high dose of up to 70 mg/kg per day has been reported.

Artemisinin is not a stand-alone chemotherapeutic agent. A


combination of nutritional supplements (such as green tea, CoQ10 and
pancreatic enzyme) as well as a good anti-cancer diet is required.

ART may be administered orally, with a 32 percent bioavailability as


compared to injections. It is highly bound to membranes. Laboratory
measurement of its serum level is therefore not exact.

Forms of Artesminin
There are three common forms of artemsinin. The water soluble form is called
artesunate . It is the most active and the least toxic. It also has the shortest
life within the body Artemether is the lipid soluble form. It has the longest life
but also the most toxic in high dosage which is seldom needed. The biggest
advantage of artemether is that it can cross the blood brain barrier.
Artemisinin is the active parent compound of the plant. It's half-life is
intermediate. It is also very safe, and can cross the blood-brain barrier. Some
clinicians prefer to use a combination of all three forms, while others tend to
favor the use of artemisinin alone with great success.

TOXICITY AND SIDE EFFECTS


High doses of artemisinin can produce neurotoxicity such as gait
disturbances, loss of spinal and pain response, respiratory depression, and
ultimately cardiopulmonary arrest in large animals.

In human beings, there are very few reports of adverse effects except for one
case of first-degree heart block. According to Robert Rowen, MD, there is a
dose related decrease in reticulocyte count for 4 days after artesunate
or artemether at doses of 4 mg/kg per day for 3 days. However, the
count returns to normal by day 14. When artemisinin suppositories are
used, doses as high as 40 mg/kg per day have no effects on the
reticulocyte count. In a study, it was reported that up to 35 percent of the
volunteers had some form of transient drug induced fever.

When ART is tested with monkeys, they showed no toxicity when they
received up to 292 mg/kg of artemether over 1 to 3 months. This is equal
to a human dose of 20,000 mg for a 70 kg male (Journal of
Traditional Chinese Medicine 2(1):31-36 1982). In another study, there was
also no sign of toxicity in over 4000 patients. This does not exclude possible
cases of long-term cumulative toxicity which is unknown at this time.

CAUTIONS
a. No artesminin should be taken within 30 days of radiation therapy because
of possible free iron leaks to the surrounding tissues after radiation therapy.

b. Preliminary laboratory studies include: CBC, reticulocyte count, liver


function test, ferritin, TIBC, ESR, C reactive protein, and appropriate tumor
markers. If the iron load is low, supplementing iron for a few days can be
considered prior to starting artemisinin.

c. Tumor markers may increase during the initial stages as the tumor starts
breaking down.

d. Vitamin E may work against the effectiveness of ART in vitro. However, this
has not been shown to be a concern in human clinical cases.

DOSAGE
The therapeutic dose ranges from 200 mg a day up to 1,000 a
day (in divided doses ) depending on cancer types and the
source of the herb. In laboratory studies, significant cell toxicity is shown
to have been effected at dosage as little as 1-2 mg/kg body weight .

The exact dosage is highly controversial. In addition to the lack of clinical trials
and individual variations, the dosage is highly dependent on the purity and
potency of the herb itself. The same 100 mg capsules from one manufacturer
may have different and varied effect from another manufacturer.

Artemisinin should always be taken with food. Cod liver oil , cottage
cheese, or fish oil may be administered at the same time to enhance
absorption. Generally, 400 to 800 mg per day can be used for at least 6 to
12 months. After that, it can be tapered off slowly.

Always take artesminin 2-3 hours aside from other antioxidants such as
Vitamin C.

Artemisinin is a "cooling herb" in the traditional Chinese medicine perspective,


and some may find it too "cooling" with symptoms such as tingling. If this
occurs, then the dosage should be reduced.

Despite its seemingly high degree of effectiveness, it is important to note that


artemisinin is not a stand-alone compound. Concurrent use of
high dose pancreatic enzyme , daily enema, liver detoxification,
and periodic laboratory measurement should also be
considered as part of an overall aggressive anti-cancer
program.

PRODUCT CONCERNS
Due to the increasing popularity of this product, the consumer should exercise
extreme caution and buy only from the most reputable supplier. Only
genuine and pure artemisinin should be used, and only buy
from sources you are familiar with. There is tremendous
variation in the potency of the herb. A 100 mg of artemisinin
from one source may be many times more potent than the same
100 mg from another source. Only buy from source you can
trust, and not be fooled by inexpensive "alternatives".

Since the herb comes from China and South-east Asia, proper quality
assurance on purity and standardization is of tremendous
importance. High-grade artemisinin must always be confirmed
by independent laboratory analysis on a batch by batch basis to
ensure consistence and purity.

Lastly, always check with your health care professional prior to


starting this herb.

Read also: Artemisinin Research Study

About The Author


Michael Lam, M.D., M.P.H., A.B.A.A.M. is a specialist in Preventive and Anti-Aging Medicine.
He is currently the Director of Medical Education at the Academy of Anti-Aging Research,
U.S.A. He received his Bachelor of Science degree from Oregon State University, and his
Doctor of Medicine degree from Loma Linda University School of Medicine, California. He
also holds a Masters of Public Health degree and is Board Certification in Anti-aging
Medicine by the American Board of Anti-Aging Medicine. Dr. Lam pioneered the formulation of
the three clinical phases of aging as well as the concept of diagnosis and treatment of sub-
clinical age related degenerative diseases to deter the aging process. Dr. Lam has been
published extensively in this field. He is the author of The Five Proven Secrets to Longevity
(available on-line). He also serves as editor of the Journal of Anti-Aging Research.

For More Information

For the latest anti-aging related health issues, visit Dr. Lam at www.LamMD.com. Feel free
to email Dr. Lam at dr@LamMD.com if you have any questions.

Reprint Information
This article may, in its unabridged, unaltered form and in its entirety only, be reprinted and
republished without permission provided that it is for personal and non commercial education
use only and further provided that credit be given to the author, with copyright notice and
www.LamMD.com clearly displayed as source. Written permission from Dr. Lam is
required for all other use.

ARTEMISININ STUDY
ABSTRACTS
The compound artemisinin was extracted from a plant called woodworm.
Thousands of years ago, the Chinese used it to combat Malaria. Today,
scientists have proven that this miraculous herb is just as effective in
combating cancer as well.

Let us review some of the scientific research papers published so far on this
herb.

A CANCER TREATMENT METHOD


All cancer cells need plenty of iron to multiply. In other words,
cancer cells have a much higher iron concentration than normal
cells. During the study, the researchers pumped cancer cells with maximum
iron concentrations and then injected artemisinin into them. The results
revealed that artemisinin had the properties of killing and
inhibiting cancer cells.
(US Patent Document 5,578,637, University of Washington, inventors Dr
H.Lai and Dr NP Singh, November 26 1996.)

CELL OF A HUMAN LEUKEMIA CELL LINE


In another study, researcher Dr Lai noted even more amazing results
involving leukemia cells. He mentioned that the cancer cells were destroyed
very quickly within a few hours when exposed to holotransferrin (which binds
with transferring receptors to transport iron into cells) and dihydroartemisinin
(a more water-soluble form of artemisinin). He further explained that it might
be because of the high concentration of iron in the leukemia cells.

(H.Lai and NP Singh, Selective Cancer Cell Cytoxicity from Exposure in


Dihydroartemisinin and Holotransferrin, Cancer Letters, 91:41-46, 1995)

55 CANCER CELL LINES


This amazing herb was also examined for its activity against 55 cancer cell
lines. It was found to be the most active against leukemia and colon
cancer and active against melanomas, breast cancer, prostate
cancer, CNS and renal cancer. It was also reported that artemisinin's
effectiveness was comparable with other standard drugs used to combat
cancer. As such, these results and the low toxicity of artemisinin had made
this herb to be a potential for cancer chemotherapy.

(Efferth et al, Anti-Malaria Drug is Also active against cancer, Int'l Journal of
Oncology, 18;767-773,2001.)

BREAST CANCER CELLS


This herb becomes cytotoxic in the presence of ferrous iron. To accommodate
a rate of iron intake greater than normal cells, cancer cells surfaces feature
greater concentrations of transferrin receptors- cellular pathways that allow
iron into a cell. In breast cancer cells, they have 5 to 15 times more
transferrin receptors on their surface than normal breast cells.
During a recent study, both breast cancer cells as well as normal cells were
injected with artemisinin. The results showed that artemisinin
effectively killed radiation-resistant breast cancer cells in vitro.
However, the effects on the normal breast cells were minimal.
This simply goes to show that this herb might be a simple, effective and
economical treatment for cancer.

(NP Singh and H Lai, Selective toxicity of dihydroartemisinin and


holotransferrin toward human breast cancer cells. Life Sciences, 70:49-
56,2001)

SMALL-CELL LUNG CARCINOMA CELLS


(SCLC)
When artemisinin was tested on drug sensitive (H69) and multi-drug resistant
(H69VP) SCLC cells which were actually injected with transferrin to raise the
iron concentration levels, it was found that the cytotoxicity of artemisinin for
H69VP cells was ten times lower than for H69 cells. This concluded that
artemisinin was part of the drug resistance phenotype. This experiment also
indicated that pretreatment of H69 did not lower the iron concentration for
artemisinin whereas for H69 VP cells, the iron concentration was lowered to
near drug sensitive levels. The researchers therefore concluded that
artemisinin could be used together with transferin in drug
resistance SCLC.

(Sadava, D et al, Transferrin overcomes drug resistance to artemisinin in


human small cell lung carcinoma cells, Cancer Letter, 179,151-156, 2002)

ENHANCED EFFECTIVENESS OF
CHEMOTHERAPY
Various studies carried out separately in Germany and Australia, revealed the
activities of twenty drugs on leukemia CCRF-CEM cells lines, artemisinin,
artesuante, balcalein, baicalin, barberine, bufalin, cantharidin, cephalotaxine,
curcumin, daidzein, daidzin, diallyl, disulfide, ginsenoside, Rh2, glycirrhizic
acid, isonardosinon, homoharringtonine, nardosinon, nardofuran, puerarin,
quercetin, tannic acid and tetrahydronardosinon. The results showed that
artesunate increased daunorabicin accumulation in CEM/E1000
cells. As artesunate and bufalin both have abilities to combat
leukemia, whether it was applied alone or together with
daunonrubicin in multi-resistant cells, these two drugs might be
suitable for treating leukemia in the near future.

(Efferth et al, Blood Cells, Molecules, and Diseases 28(2) Mar/April; 160-168,
2002)

MODULATION OF MULTIDRUG RESISTANCE


FOR CHEMOTHERAPY
Arteminisin could prevent the spread of cancer cells and increase cytotoxicity
of perarubicin and doxorubicin in P-glycoprotein-overexpressing, and in MRP-
overexpressing, but not in their corresponding drug sensitive cell lines.

(Reungpatthanaphong, P et al Modulation of MDR by Artemisinin, artesunate


and DHA in K562, GLC4 Resistant cell lines, Biology Pharmocology Bull.
25(12) 1555-1561, 2002)

5 CANCER CELL LINES


When a triterpene and a sesquiterpene were isolated from separation of
artemisia stolonifera, both of them proved to be able to destroy cancer
cells in non-small cell lung adenocarcinorma, ovarian cancer, skin
melanoma, CNS and colon cancer.

(Kwon, Phytochemical constituents of Artemisia stolonifera, Arch.Pharm,


Research 24(4):312-315,2001)

ANTI-TUMOR EFFECT
When artemisinin's derivative, 9 C-10 was prepared as dimers using novel
chemistry, it proved to be able to kill malaria cells. Additionally, dimers 8,
10 and 12 were especially powerful and prevented cancer growth in the NCI
in vitro 60 cell line assay.

(Posner, GH et al, Antimalarial, antiproliferative and antitumor activities of


Artemisin Derived Dimers, J Medicinal Chemistry, 42(21), 178-181, Oct 1999)

LEUKEMIA AND NON SMALL-CELL LUNG


CARCINOMA CELL LINES
Researchers discovered a novel class of compounds that could destroy
cancer cells after modifying artemisinin in one of the experiments conducted
recently. This new derivative contained cyano and aryl groups and was very
effective in destroying leukemia and human lung carcinoma cells.

(Li, Ying, et al, Novel antitumor artemisinin derivatives targeting G1 phase of


the cell cycle, Bioorganic and Medicinal chemistry letters 11:5-8, 2001)

TUMOR CELLS
Some artemisinin related endoperoxides that were tested on their abilities
to destroy Ehrlich ascites tumor cells (EAT) were proven positive. Surprisingly,
its derivatives were even more powerful at destroying cancer cells. This test
also confirmed artemisinin and its derivaties abilities to kill EAT cells at higher
concentration than those needed for in vitro anti-malaria activities.

(Woerdenbag, HJ et al. Cytotoxicity of artemisinin-related endoperoxides to


EATcells, J Natural Products 56(6), 849-856, 1993)

BLOOD-BRAIN BARRIER & ALZELMER'S


DISEASE (AD)
Although artemisinin could not be dissolved in water, it was able to cross
the blood brain barrier. It might therefore be useful for curing brain
tumors and other brain diseases.

During a recent experiment, an alkaloid of artemisia asiatica was metabolized


to small molecules in the digestive tract and was passed through the blood
brain barrier. The results showed that it could act as an acetylcholinesterase
inhibitor with a blocker of neuroloxicity induced by a beta in human beings that
caused AD.

(Heo et al, Inhibitory effects of Artemesia alkaloids on acetylcholine sterase


activity from PC12 cells, molecule cells, Jun 30:10(3):253-262)

Clinical Trials Using Artemisinin


HUMAN LARYNX CANCER TREATMENT
In this case, the patient was given artesunate injections and tablets over a
period of nine months. His tumor was significantly reduced by about 70
percent just after two months of treatment. The patient also reported that he
benefited much from this treatment. It actually prolonged his life and improved
his quality of life. Once again, artemisinin had proven its amazing properties in
killing cancer cells.

(Singh and Verma, Case report of a laryngeal squamous cell carcinoma

treated with artesunate, Archive of Oncology, Vol 10(4), 279-80, 2002)

TOXICITY OF ARTEMISININ
LARGE ANIMALS
High doses of artemisinin could produce neurotixicity such as
ding gait disturbances, loss of spinal and pain response, respiratory
depression and ultimately cardiopulmonary arrest in large animals.
When artemisinin was given to monkey at 292 mg/kg over 1 to 3 months, they
showed no toxicity.

(Journal of Traditional Chinese Medicine 2(1) : 31-36, 1982)

HEALTHY VOLUNTEERS
In pharmacokinetic studies, 250 mg tablets of artemisin and
artesunate tablets were used. Both forms of tablets were well
tolerated and there were no negative side effects.

(Benakis et al. Pharmacokinetics of artemisinin and artesunate after oral


administration in healthy volunteers. American Journal of Tropical Medicine
Hyg, Jan;56(1): 17-23, 1997)

PHARMACOKINETICS
During a study, healthy volunteers were given 250 mg of tablets of artemisinin
and artesunate orally. The researchers reported that in the case of
artemisinin, the mean maximum drug concentration C= 0.36 microgram/ml,
appearance half life T= 0.62 hr, distribution half life t(12) a= 2.61 hr, decline
half life t(12) = 4.34 hr, total area under the concentration curve (AUC) = 1.10
microgram.hg/ml, its main metabolite, dihydroartemisinin was measurable in
plasma. On the other hand, half lives were much shorter in the case of
artesunate.

(Benakis, et al, Dept of Pharmacology, Geneva U Swiss, Am J Trop Med Hyg,


Jan; 56(1): 17-23, 1997)

Artemisinin is a herbal treatment for parasitic infections and malaria that also protects against particular types of
cancer

Extracted from the plant Artemesia Annua L (sweet wormwood, also known as the Chinese herbal Qinghao),
Artemisinin has been used for centuries to kill parasites, particularly worms and flukes. These parasites, which are
present in us all, create a burden for the body, sapping energy resources and creating by-products that need to be
excreted.

Anti-malaria

Artemisinin has also proven itself as a safe and effective treatment for malaria in over two million patients.

Anti-cancer

Now studies are also showing that Artemisinin is effective against a wide variety of cancers as shown in a series of
successful experiments. The most effective is leukemia and colon cancer. Intermediate activities were also shown
against melanoma, breast, ovarian, prostate, CNS and renal cancer.

Artemisinin’s method of action

Artemisinin contains two oxygen atoms linked together in what is known as an 'endoperoxide bridge', which react
with iron atoms to form free radicals. Artemisinin becomes toxic to malaria parasites when it reacts with the high iron
content of the parasites, generating free radicals, and leading to damage to the parasite.

By this same mechanism, Artemisinin becomes toxic to cancer cells which sequester relatively large amounts of iron
compared to normal, healthy human cells. According to the Gordon Research Institute, tests have been conducted
which show that Artemisinin causes rapid and extensive damage and death in cancer cells and yet has relatively low
toxicity to normal cells.

Dosage:
For general eradication of parasites, take one or two capsules (100 mg each) per day, ideally before a meal.

Those who are “at risk” from malaria, cancer or other serious parasite infection should consider at least 100 mg to
200mg three times a day.
ABOUT THE PROJECT 
A unique collaboration of representatives from academia, biotechnology, pharmaceutical, and the nonprofit sector
is pioneering a bold approach to make safe, effective antimalarial medicines accessible to people in poor
countries.
The partnership is applying a combination of synthetic biology, industrial fermentation, chemical synthesis, and
drug development expertise to a very specific need of the developing world. In doing so, the partnership sets an
example of how groups with critical knowledge and skills can pool talents to address a major global health
problem. A key element of this project is the application of basic research principles to a real-world issue.

Armed with a $42.6 million grant from the Bill & Melinda Gates Foundation, the Institute for OneWorld Health
formed a funded research and development collaboration, known as the Artemisinin Project, with Prof. Jay
Keasling at the University of California, Berkeley and Amyris to develop semisynthetic artemisinin. In 2008,
sanofi-aventis joined the collaborative effort to apply their expertise in process development and manufacturing
scale-up.

Malaria has become increasingly resistant to front-line medications, but combination drugs containing artemisinin
derivatives show nearly 100 percent effectiveness after a brief, three-day regimen. Yet, even at a price of
approximately $2.20 per adult course for artemisinin combination therapies (ACTs) approved by the World Health
Organization 1, these drugs are still beyond the reach of millions of the world's poorest people.

Over the course of the grant, the project aims to create, optimize, scale-up, and industrialize microbial production
systems to make bulk artemisinin available for incorporation into ACTs, at a low price with consistent high quality.
A second source of artemisinin, in addition to plant-derived material, is needed to ensure global supply needs can
be fulfilled due to current market volatility. If technical benchmarks are achieved, the project would progress to the
commercial manufacturing phase with the goal to facilitate integration of semisynthetic artemisinin into the supply
chain and ACTs.