Artemisinin

[tucker_man]

Anyone have any experience, knowledge or opinion about the effectiveness of taking artemisinin? There is a lot of positive, but not conclusive information if you google "artemisinin prostate cancer".

[Graham49]

See encouraging in-vitro study abstract below.

Anticancer Drugs. 2017 Oct;28(9):1018-1031. doi: 10.1097/CAD.0000000000000547. Artemisinin disrupts androgen responsiveness of human prostate cancer cells by stimulating the 26S proteasome-mediated degradation of the androgen receptor protein. Steely AM1, Willoughby JA Sr, Sundar SN, Aivaliotis VI, Firestone GL. Androgen receptor (AR) expression and activity is highly linked to the development and progression of prostate cancer and is a target of therapeutic strategies for this disease. We investigated whether the antimalarial drug artemisinin, which is a sesquiterpene lactone isolated from the sweet wormwood plant Artemisia annua, could alter AR expression and responsiveness in cultured human prostate cancer cell lines. Artemisinin treatment induced the 26S proteasome-mediated degradation of the receptor protein, without altering AR transcript levels, in androgen-responsive LNCaP prostate cancer cells or PC-3 prostate cancer cells expressing exogenous wild-type AR. Furthermore, artemisinin stimulated AR ubiquitination and AR receptor interactions with the E3 ubiquitin ligase MDM2 in LNCaP cells. The artemisinin-induced loss of AR protein prevented androgen-responsive cell proliferation and ablated total AR transcriptional activity. The serine/threonine protein kinase AKT-1 was shown to be highly associated with artemisinin-induced proteasome-mediated degradation of AR protein. Artemisinin treatment activated AKT-1 enzymatic activity, enhanced receptor association with AKT-1, and induced AR serine phosphorylation. Treatment of LNCaP cells with the PI3-kinase inhibitor LY294002, which inhibits the PI3-kinase-dependent activation of AKT-1, prevented the artemisinin-induced AR degradation. Furthermore, in transfected receptor-negative PC-3 cells, artemisinin failed to stimulate the degradation of an altered receptor protein (S215A/S792A) with mutations in its two consensus AKT-1 serine phosphorylation sites. Taken together, our results indicate that artemisinin induces the degradation of AR protein and disrupts androgen responsiveness of human prostate cancer cells, suggesting that this natural compound represents a new potential therapeutic molecule that selectively targets AR levels. PMID: 28708672 DOI: 10.1097/CAD.0000000000000547

[jimbay]

Looks like kind of scary stuff. Excerpt from the NIH and CSC:

Case 1. Acute liver injury due to artemisinin exposure.

[Modified from: Centers for Disease Control and Prevention (CDC). Hepatitis temporally associated with an herbal supplement containing artemisinin – Washington, 2008. MMWR Morb Mortal Wkly Rep 2009; 58: 854-6. PubMed Citation]

A 52 year old man with irritable bowel syndrome was treated with an herbal powder that contained artemisinin and developed fatigue and dark urine 10 days later. He had no history of liver disease, alcohol abuse, recent travel or risk factors for viral hepatitis. His only other medication was an occasional acetaminophen tablet. Analysis of the powder indicated that he had been taking the equivalent of 600 mg of artemisinin daily. Physical examination revealed jaundice and mild abdominal tenderness without fever or rash. Laboratory testing suggested a mild hepatitis (Table). His serum enzymes had been normal on routine testing five months earlier.

Comment

Cases of artemisinin hepatotoxicity have been characterized by rapid onset within a few days to 3 weeks of starting therapy and a hepatocellular pattern of serum enzyme elevations, but without signs of hypersensitivity such as rash, fever or eosinophilia. The cause of the injury is unknown, but it has many features of hypersensitivity such as short latency and occurrence upon reexposure. Fatal instances have been reported. The current case was distinctive in that the patient was taking artemesinin not for malaria, but as a part of an herbal medication for gastrointestinal complaints.

[Ramp7]

Doing a brief check on this compound there are some interesting finds.

ncbi.nlm.nih.gov/pmc/articl...

Artemisinin Blocks Prostate Cancer Growth and Cell Cycle Progression by Disrupting Sp1 Interactions with the Cyclin-dependent Kinase-4 (CDK4) Promoter and Inhibiting CDK4 Gene Expression*

[tucker_man]

I took it and can’t say one way or another whether it helped. I know it didn’t have any negative side effects. I used it on my dog when he got a tumor and it didn’t shrink it like I’d hoped.