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Review
. 2021 Nov 23:12:715359.
doi: 10.3389/fphar.2021.715359. eCollection 2021.

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

Junqi Zhao  1 , Fangling Zhang  1 , Xiaolin Xiao  2 , Zhao Wu  1 , Qichao Hu  1 , Yinxiao Jiang  1 , Wenwen Zhang  1 , Shizhang Wei  1 , Xiao Ma  1 , Xiaomei Zhang  3
Affiliations
Free PMC article
Review

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

Junqi Zhao et al. Front Pharmacol. .
Free PMC article

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.

Keywords: Tripterygium hypoglaucum (Lévl.) Hutch.; pharmacokinetics; pharmacology; phytochemistry; toxicity.

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Conflict of interest statement

The authors declare that the research was conducted in the absence of any commercial or financial relationships that could be construed as a potential conflict of interest.

Figures

FIGURE 1
FIGURE 1
Climatic and ecological adaptability distribution of THH in China. (A) Dried root bark of THH, (B) Aerial view of THH.
FIGURE 2
FIGURE 2
Timeline of the isolation and identification of main chemical components from the genus Tripterygium.
FIGURE 3
FIGURE 3
Chemical structures of the existing potential quality control markers in THH.
FIGURE 4
FIGURE 4
The main signalling pathways and molecular targets of the pharmacologically active components in THH.
FIGURE 5
FIGURE 5
Illustration of the main signalling pathways involved in THH-based therapy and organ toxicities observed at high doses.
See this image and copyright information in PMC

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References

    1. Abdin A. A., Hasby E. A. (2014). Modulatory Effect of Celastrol on Th1/Th2 Cytokines Profile, TLR2 and CD3+ T-Lymphocyte Expression in a Relapsing-Remitting Model of Multiple Sclerosis in Rats. Eur. J. Pharmacol. 742, 102–112. 10.1016/j.ejphar.2014.09.001 - DOI - PubMed
    1. Abu Bakar M. H., Cheng K.-K., Sarmidi M. R., Yaakob H., Huri H. Z. (2015). Celastrol Protects against Antimycin A-Induced Insulin Resistance in Human Skeletal Muscle Cells. Molecules 20, 8242–8269. 10.3390/molecules20058242 - DOI - PMC - PubMed
    1. Abu Bakar M. H., Sarmidi M. R., Tan J. S., Mohamad Rosdi M. N. (2017). Celastrol Attenuates Mitochondrial Dysfunction and Inflammation in Palmitate-Mediated Insulin Resistance in C3A Hepatocytes. Eur. J. Pharmacol. 799, 73–83. 10.1016/j.ejphar.2017.01.043 - DOI - PubMed
    1. Abu Bakar M. H., Tan J. S. (2017). Improvement of Mitochondrial Function by Celastrol in Palmitate-Treated C2C12 Myotubes via Activation of PI3K-Akt Signalling Pathway. Biomed. Pharmacother. 93, 903–912. 10.1016/j.biopha.2017.07.021 - DOI - PubMed
    1. Bakar M. H. A., Sarmidi M. R., Kai C. K., Huri H. Z., Yaakob H. (2014). Amelioration of Mitochondrial Dysfunction-Induced Insulin Resistance in Differentiated 3T3-L1 Adipocytes via Inhibition of NF-Κb Pathways. Int. J. Mol. Sci. 15, 22227–22257. 10.3390/ijms151222227 - DOI - PMC - PubMed

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