Tripterygium hypoglaucum (Lévl.) Hutch and Its Main Bioactive Components: Recent Advances in Pharmacological Activity, Pharmacokinetics and Potential Toxicity

Abstract

Tripterygium hypoglaucum (Lévl.) Hutch (THH) is believed to play an important role in health care and disease treatment according to traditional Chinese medicine. Moreover, it is also the representative of medicine with both significant efficacy and potential toxicity. This characteristic causes THH hard for embracing and fearing. In order to verify its prospect for clinic, a wide variety of studies were carried out in the most recent years. However, there has not been any review about THH yet. Therefore, this review summarized its characteristic of components, pharmacological effect, pharmacokinetics and toxicity to comprehensively shed light on the potential clinical application. More than 120 secondary metabolites including terpenoids, alkaloids, glycosides, sugars, organic acids, oleanolic acid, polysaccharides and other components were found in THH based on phytochemical research. All these components might be the pharmacological bases for immunosuppression, anti-inflammatory and anti-tumour effect. In addition, recent studies found that THH and its bioactive compounds also demonstrated remarkable effect on obesity, insulin resistance, fertility and infection of virus. The main mechanism seemed to be closely related to regulation the balance of immune, inflammation, apoptosis and so on in various disease. Furthermore, the study of pharmacokinetics revealed quick elimination of the main component triptolide. The feature of celastrol was also investigated by several models. Finally, the side effect of THH was thought to be the key for its limitation in clinical application. A series of reports indicated that multiple organs or systems including liver, kidney and genital system were involved in the toxicity. Its potential serious problem in liver was paid specific attention in recent years. In summary, considering the significant effect and potential toxicity of THH as well as its components, the combined medication to inhibit the toxicity, maintain effect might be a promising method for clinical conversion. Modern advanced technology such as structure optimization might be another way to reach the efficacy and safety. Thus, THH is still a crucial plant which remains for further investigation.

Differences in Multicomponent Pharmacokinetics, Tissue Distribution, and Excretion of Tripterygium Glycosides Tablets in Normal and Adriamycin–Induced Nephrotic Syndrome Rat Models and Correlations With Efficacy and Hepatotoxicity

“…Previous studies on TGT pharmacokinetics have mainly focused on healthy animals, or animals with rheumatoid arthritis. Of note, the severity of rheumatoid arthritis was positively correlated with plasma exposure to WFG and WFR in rats after TGT administration ( Su et al, 2015a ; Lin et al, 2021 ; Zhao et al, 2021 ). Thus, it is rational to investigate the influence of NS on the key TGT components, as NS is another clinical indication for TGT.…”

Network Pharmacology and Experimental Validation to Explore That Celastrol Targeting PTEN is the Potential Mechanism of Tripterygium wilfordii (Lév.) Hutch Against IgA Nephropathy

“…40 Celastrol is considered one of the most active and widely studied components of THH. 8 This traditional medicinal component was listed by Cell in 2007 as most likely to be developed as modern drugs. 41 Celastrol has recently been proven to restrain cancers, obesity, and inflammation.…”

“…6,7 However, their composition and toxicity are slightly different, some scholars believe that the toxicity and side effects of THH are less than TwHF. 8,9 Due to its striking immunosuppressive and resist-inflammatory effects, THH is applied extensively in many kinds of immune system diseases such as rheumatoid arthritis, psoriasis, and diabetic kidney disease, which can exert its pharmacological effects through multiple targets and multiple pathways. [10][11][12] As preparations of dried root extract of THH, Colquhounia Root Tablet and Kunxian Capsule have been used for treating kinds of kidney disease in China for over 30 years because of their favorable clinical effects and medicinal value.…”

ROS Responsive Nanoparticles Encapsulated with Natural Medicine Remodel Autophagy Homeostasis in Breast Cancer

“…Triptolide (TP), a main active component of the traditional Chinese medicine Tripterygium wilfordii Hook F , , is well-known for its immunomodulatory and antitumor pharmacological effects. − It shows preclinical antitumor effects by inducing tumor cell apoptosis, suppressing tumor invasion and metastasis, inhibiting drug resistance, and regulating cell autophagy. − Utmost, as a natural regulator of cell autophagy without drug resistance in tumor treatment, ,− TP can promote cell autophagy in treatment of different tumor models. Through elevating cell autophagy induced cell death, TP exerts anticancer effects against pancreatic cancer and the glioblastoma mouse model by increasing autophagy-related protein-microtubule-associated protein 1 light chain 3 (LC3) .…”