Foods/Supplements-Vitamins: Artemisinin / {Prescription: Dihydroartemisinin}

New Dihydroartemisinin study below [4].

[1] Wikipedia.

"Artemisinin, also known as qinghao su (Chinese: 青蒿素), and its semi-synthetic derivatives are a group of drugs that possess the most rapid action of all current drugs against Plasmodium falciparum malaria. It was discovered by Tu Youyou, a Chinese scientist, who was awarded half of the 2015 Nobel Prize in Medicine for her discovery. Treatments containing an artemisinin derivative (artemisinin-combination therapies, ACTs) are now standard treatment worldwide for P. falciparum malaria. Artemisinin is isolated from the plant Artemisia annua, sweet wormwood, an herb employed in Chinese traditional medicine."

"Artemisinin is undergoing early research and testing for the treatment of cancer. Artemisinin has anticancer effects in experimental models of hepatocellular carcinoma. Artemisinin has a peroxide lactone group in its structure, and it is thought that when the peroxide comes into contact with high iron concentrations (common in cancerous cells), the molecule becomes unstable and releases reactive oxygen species. It has been shown to reduce angiogenesis and the expression of vascular endothelial growth factor in some tissue cultures. Recent pharmacological evidence demonstrates the artemisinin derivative dihydroartemisinin targets human metastatic melanoma cells in vitro with induction of phorbol-12-myristate-13-acetate-induced protein 1 dependent mitochondrial apoptosis that occurs downstream of iron-dependent generation of cytotoxic oxidative stress. A pilot study on the use of the artemisinin derivative artesunate yielded promising results for the treatment of colorectal cancer."

[2] Products.

I gave artemisinin a shot almost 10 years ago. The NutriCology product [2a] might have been the only product available back then. It was not expensive. Things have changed. More options - some of them cheap [2b].

Artemisinin is not for chronic use, I feel. I used it for the first 7 days of each month & limited it to 6 months.

Unfortunately, I was using something that probably reduced iron levels in my PCa cells. Artemisinin is drawn to iron & will only kill cells that have an excessive amount.

{"Intracellular iron uptake is regulated by the transferrin receptor (TfR), and the activity of artemisinin depends on the availability of iron. " [8]}

[3] Prescription Drugs.

[3a] Dihydroartemisinin.

"Dihydroartemisinin (also known as dihydroqinghaosu, artenimol or DHA) is a drug used to treat malaria. Dihydroartemisinin is the active metabolite of all artemisinin compounds (artemisinin, artesunate, artemether, etc.) and is also available as a drug in itself. It is a semi-synthetic derivative of artemisinin and is widely used as an intermediate in the preparation of other artemisinin-derived antimalarial drugs."

[4] (2017 - China / Canada)

"Dihydroartemisinin (DHA) has been proven to be a promising anticancer agent in vitro as well as in vivo in accumulating data. However, the detailed mechanisms of how DHA action in human prostate cancer PC-3 cells remain elusive."

"We showed that DHA induced the downregulation of UHRF1 and DNMT1, accompanied by an upregulation of p16 in PC-3 cells." ...

"Our results suggested that downregulation of UHRF1/DNMT1 is upstream to many cellular events, including G1 cell arrest, demethylation of p16, and apoptosis."

[5] (2008 - China)

"Artesunate induces prostate cancer cell line PC-3 differentiation and cell cycle arrest"

[6] (2008 - U.S.)

"Artemisinin, a natural product isolated from Artemisia annua, contains an endoperoxide group that can be activated by intracellular iron to generate toxic radical species. Cancer cells over-express transferrin receptors (TfR) for iron uptake while most normal cells express nearly undetectable levels of TfR. We prepared a series of artemisinin-tagged transferrins (ART-Tf) where different numbers of artemisinin units are attached to the N-glycoside chains of transferrin (Tf). The Tf bearing approximately 16 artemisinins retains the functionality of both Tf and artemisinin. Reduction of TfRs by TfR siRNA transfection significantly impaired the ability of ART-Tf, but not dihydroartemisinin, to kill cells. We also demonstrate that the ART-Tf conjugate kills the prostate carcinoma cell line DU 145 by the mitochondrial pathway of apoptosis."

[7] (2008 - U.S.)

"Artemisinin, a naturally occurring component of Artemisia annua, or sweet wormwood, is a potent anti-malaria compound that has recently been shown to have anti-proliferative effects on a number of human cancer cell types, although little is know about the molecular mechanisms of this response. We have observed that artemisinin treatment triggers a stringent G1 cell cycle arrest of LNCaP (lymph node carcinoma of the prostate) human prostate cancer cells that is accompanied by a rapid down-regulation of CDK2 and CDK4 protein and transcript levels."

"... our results demonstrate that a key event in the artemisinin anti-proliferative effects in prostate cancer cells is the transcriptional down-regulation of CDK4 expression by disruption of Sp1 interactions with the CDK4 promoter."

[8] (2010 - U.S.)

"Artemisinin is a plant-derived anti-malarial drug that has relatively low toxicity in humans and is activated by heme and/or intracellular iron leading to intracellular free radical formation. Interestingly, artemisinin has displayed anti-cancer activity, with artemisinin dimers being more potent than monomeric artemisinin."

This study looked at two such dimers.

[9] (2010 - U.S.)

"Dihydroartemisinin upregulates death receptor 5 expression and cooperates with TRAIL to induce apoptosis in human prostate cancer cells."

[10] (2012 - China)

"Dihydroartemisinin can significantly suppress the growth of PC-3M cells, promote their apoptosis and reduce the expressions of VEGF mRNA and protein, which may serve to explain its inhibitory effect on tumor and angiogenesis."

[11] (2015 - Germany)

"A patient with prostate carcinoma (pT3bN1M1, Gleason score 8 (4+4)) presented with a prostate specific antigen (PSA) level >800 µg/l. After short-term treatment with bacalitumide (50 mg/d for 14 days) and long-term oral treatment with A. annua {Artemisia annua L} capsules (continuously 5 × 50 mg/d), the PSA level dropped down to 0.98 µg/l. MRT, scintigraphy and SPECT/CT verified tumor remission. Seven months later, PSA and ostase levels increased, indicating tumor recurrence and skeletal metastases. Substituting A. annua capsules by artesunate injections (2 × 150 mg twice weekly i.v.) did not prohibit tumor recurrence."

"Long-term treatment with A. annua capsules combined with short-term bicalitumide treatment resulted in considerable regression of advanced metastasized prostate carcinoma."

[12] (2016 - China)

"DHA {Dihydroartemisinin} induced obvious apoptosis in PC3 cells. ... we found 86 differentially expressed proteins linked to the cytotoxicity of DHA in PC3 cells. ... one candidate protein, heat shock protein HSP70 (HSPA1A), was identified ..."

"Our results indicate that multiple mechanisms involved in the anticancer activity of DHA in PC3 cells. Decreased HSP70 expression may have an important role in DHA-induced apoptosis in PC3 cells."

[13] (2016 - China)

"In vitro and in vivo inhibition of tumor cell viability by combined dihydroartemisinin and doxorubicin treatment, and the underlying mechanism."

















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