 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)
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