Research Progress on Pharmacological Activities and Mechanism of Triptonide / 中国实验方剂学杂志

The root of Tripterygium wilfordii has the effect in dispelling wind and eliminating dampness. Now it is mostly used in the treatment of systemic lupus erythematosus and other diseases. Triptonide is a diterpene small molecule compound extracted from T. wilfordii. In the early years， it was studied as a potential drug with anti-inflammatory and anti-reproductive effects. Recently， researchers found that its anti-tumor effect was particularly prominent because triptonide could inhibit the growth of a variety of tumors with different mechanisms at the nanomole dose， with a potential to be used as a broad-spectrum anti-cancer drug. In addition， due to the low yield from T. wilfordii， low bioavailability due to poor water solubility and anti-reproductive side effect as an antitumor drug， it will become study hotspots to exploring its synthesis and preparation and modifying its structure to reduce cost， improve bioavailability and reduce side effect， while maintaining its pharmacological activity. The authors reviewed domestic and foreign studies and patents on triptonide， and summarized its pharmacological activity and mechanism. It is found that although current studies on triptonide are still in the preliminary stage， there have been increasingly more studies on its anti-tumor mechanism year by year since 2014. This paper mainly introduces the antitumor pharmacological activity and mechanism of triptonide. In addition， it reviews anti-inflammatory， immunosuppression and anti-reproductive pharmacological effect of triptonide， as well as the existing studies on its toxicity， synthesis and structural modification. The authors put forward some personal ideas on its future study direction， in the hope to provide thinking and inspirations for other researchers and provide references for further development and research.

Effect of Triptonide on Proliferation and Apoptosis of SHI-1 Cells / 中国实验方剂学杂志

Objective:This study aims to investigate the effect of triptonide （TN） on proliferation， cell cycle， apoptosis and expressions of apoptosis-related proteins of human acute monocytic leukemia（AML） cell line SHI-1， and to explore its possible mechanism of action. Method:The thiazolyl blue （MTT） colorimetric assay was applied to detect the inhibitory effect of 20，40，80，160，320 nmol·L^-1 triptonide on the proliferation of SHI-1 cells for 48， 72 h. Changes in SHI-1 cell cycle before and after triptonide treatment were detected by flow cytometry propidium iodide （PI） simple staining， and changes in SHI-1 cell apoptosis before and after triptonide treatment were detected by flow cytometry with AnnexinV/PI double staining. Western blot was applied to detect the protein expression of cysteine protease （Caspase）-3， Caspase-8 and nuclear transcription factor kappaB（NF-<italic>κ</italic>B） in SHI-1 cells before and after treatment with 80， 160 nmol·L^-1triptonide. Result:Compared with the blank group， 40，80，160，320 nmol·L^-1 triptonide significantly inhibited the proliferation of SHI-1 cells（<italic>P</italic><0.01） in a dose-dependent manner for 48， 72 h， while 160， 320 nmol·L^-1 triptonide induced apoptosis of SHI-1 cells（<italic>P</italic><0.01） for 48， 72 h， and 160 nmol·L^-1 triptonide could decrease the S phase ratio of SHI-1 cells（<italic>P</italic><0.01）. In addition， compared with the blank group， 80，160 nmol·L^-1 triptonide induced the downregulation of NF-<italic>κ</italic>B significantly（<italic>P</italic><0.01）， 160 nmol·L^-1 triptonide induced the downregulation of Caspase-3， Caspase-8 significantly（<italic>P</italic><0.01）. Conclusion:Triptonide can inhibit the proliferation and induce apoptosis <italic>in vitro</italic> of SHI-1 cells， which may be related to the reduction of the cells in S phase proportion by triptonide， and the downregulation of the expression levels of Caspase-3， Caspase-8 and NF-<italic>κ</italic>B proteins.

Preparation and characterization of solid dispersion in vitro from extract of Tripterygium wilfordii based on multi-component evaluation / 中草药

Objective To improve the dissolution in vitro, thereby to prepare the solid dispersion (SD) from the extract of Tripterygium wilfordii (ETW). Methods Polyethylene glycol 6000 (PEG 6000) and poloxamer 188 (F68) were used as carrier to prepare ETW-SD by solvent-melting method. The triptolide, triptonide, wilforine, tripterine and wilforlide were used as the evaluation indexes to characterize the optimal prescription of ETW-SD by dissolution in vitro, scanning electron microscopy (SEM), differential scanning calorimetry (DSC), and X-ray diffraction (XRD). Results The optimal formulation for ETW-SD composed of ETW-PEG 6000-F68 (1∶2∶1). Compared with the raw materials, the dissolution of triptonide, triptolide and wilforine increased by a factor of 3.32, and wilforine by 2 times, while the dissolution of tripterine and wilforlide reached more than 83% within 60 min.

Determination of Triptolide and Triptonide in plasma by HPLC / 中国法医学杂志

Objective To establish a method for quantitative determination of triptolide and triptonide in human plasma samples by HPLC.Methods The samples were extracted with Oasis HLB solid phase extraction cartridge and analyzed with reserved phase HPLC coupled with diode array detection.Results Recoveries rates obtained from spiked plasma for the two diterpenoid were higher than 80%.The linearity ranged from 10 ng/ml to 1 000 ng/ml.Detection limits of the method were 3.0ng/ml for triptolide and 4.5ng/ml for triptonide.Conclusion The method is fast and accurate,which is applicable to determination of diterpenoid in cases of suspected poisoning of Triptergium wilfordii Hook.f. in forensic practice.