Triptolide is a diterpene triepoxide, immunosuppresive agent extracted from the Chinese herb Tripterygium wilfordii. It has immunosuppressive, anti-inflammatory, antiproliferative and antitumour effects. Triptolide is an NF-κB activation inhibitor.
NSC 163062; PG490; Trisoxireno[4b,5:6,7:8a,9]phenanthro[1,2-c]furan-1(3H)-one, 3b,4,4a,6,6a,7a,7b,8b,9,10-decahydro-6-hydroxy-8b-methyl-6a-(1-methylethyl)-, (3bS,4aS,5aS,6R,6aR,7aS,7bS,8aS,8bS)-; (3bS,4aS,5aS,6R,6aR,7aS,7bS,8aS,8bS)-3b,4,4a,6,6a,7a,7b,8b,9,10-Decahydro-6-hydroxy-8b-methyl-6a-(1-methylethyl)-trisoxireno[4b,5:6,7:8a,9]phenanthro[1,2-c]furan-1(3H)-one; (-)-Triptolide; PG 490; Triptolide
Soluble in Dichloromethane (Slightly), DMSO (Slightly), Ethyl Acetate (Slightly), Methanol
The triptolide-loaded microemulsions showed an enhanced in vitro permeation through mouse skins compared to an aqueous solution of 20% propylene glycol containing 0.025% triptolide. The permeation of microemulsions accorded with the Fick's first diffusion law. No obvious skin irritation was observed for the studied microemulsion ME6, but the aqueous solution of 20% propylene glycol containing 0.025% triptolide revealed the significant skin irritation. Cell growth was significantly inhibited by triptolide as observed by an inverted phase contrast microscope; the results of MTT assay indicated that triptolide inhibits HEC-1B cell proliferation in a dose and time-dependent manner.
Flow cytometry showed that low concentration (5 ng/ml) of triptolide induces cell cycle arrest of HEC-1B cells mainly at S phase, while higher concentration (40 or 80 ng/ml) induced cell cycle arrest of HEC-1B cells mainly at G2/M phase, and apoptosis of the cells was also induced. High-dose triptolide showed a similar tumor-inhibitory effect as cisplatin (-50%); high-dose triptolide significantly inhibited Bcl-2 and VEGF expression in the xenograft model compared to normal saline control (P<0.05). The in vivo anti-osteosarcoma effects of triptolide were verified in osteosarcoma nude mice. The in vivo associated protein expressions were detected using immunohistochemistry (IHC). The results indicated that Triptolide could significantly inhibit the proliferation of various osteosarcoma cells. Besides, it could induce their apoptosis. Triptolide triggered the mitochondrial dependent apoptotic pathway, significantly inhibited the in vivo growth of osteosarcoma cells, and caused in vivo apoptosis.
Clinical Trial Information
|NCT Number||Condition Or Disease||Phase||Start Date||Sponsor||Status|
|NCT00801268||Polycystic Kidney||Not Applicable||2015-03-30||Zhi-Hong Liu, M.D.||Terminated (high rate of drop-out)|
|NCT02115659||Autosomal Dominant Polycystic Kidney Disease (ADPKD)||Phase 3||2014-04-17||Shanghai Changzheng Hospital||Unknown Verified April 2014 by Mei changlin, Shanghai Changzheng Hospital. Recruitment status was Recruiting|
|NCT02219672||AIDS/HIV PROBLEM||Phase 3||2014-08-19||Peking Union Medical College||Unknown Verified August 2014 by LI Taisheng, Peking Union Medical College. Recruitment status was Recruiting|
|NCT04896073||Adenosquamous Carcinoma of the Pancreas||Phase 2||2021-11-29||National Cancer Institute (NCI)||Recruiting|
|NCT01817283||HIV||Phase 1, Phase 2||2013-03-25||LI Taisheng||Unknown Verified March 2013 by LI Taisheng, Peking Union Medical College. Recruitment status was Recruiting|
White to Off-white Powder
Room temperature, or blue ice upon request.
Store at -20°C under inert atmosphere
Acute Toxic; Health Hazard
601.7±55.0°C at 760 mmHg