Preclinical Pharmacokinetics of Triptolide: A Potential Antitumor Drug.[Pubmed: 30112986]

Triptolide, a bioactive component in Tripterygium wilfordii extracts, possess strong anti-proliferative activity on all 60-national cancer institute (NCI) cancer cell lines. The antitumor property of triptolide has made it become a promising anti-cancer drug. However, the widespread use of triptolide in the clinical practice is greatly limited for its multi-organ toxicity and narrow therapeutic window. All the toxic characteristics of triptolide are associated with the pharmacokinetics especially its distribution and accumulation in the target organ. The article presents a comprehensive review of the preclinical pharmacokinetics of triptolide. Oral triptolide is rapidly and highly absorbed. Grapefruit juice affects oral absorption, increasing the area under the concentration-time curve (AUC) by 153 % and the maximum concentration (Cmax) by 141 %. The AUC and the Cmax are not dose proportional. Triptolide distributes into the liver, heart, spleen, lung and kidney. Biotransformation of triptolide in rats includes hydroxylation, sulfate, glucuronide, N-acetylcysteine (NAC) and glutathione (GSH) conjugation and combinations of these pathways. Less than 4 % of triptolide was recovered from the feces, bile and urine within 24 h. After repeating dosage, triptolide was eliminated quickly without accumulation in vivo. As a substrate of P-glycoprotein (P-gp) and CYP3A4, triptolide could have clinically significant pharmacokinetic interactions with those proteins substrates/inhibitors.

[Chemical Constituents of An Endophytic Fungus from Tripterygium wilfordii and Their Monoamine Oxidase Inhibitory Activity}[Pubmed: 30088877]

To study the chemical constituents and monoamine oxidase inhibitory activity of Talaromyces wortmannii,an endophytic fungus was isolated from Tripterygium wilfordii.