Du Qinyun, Meng Xianli, Wang Shaohui
State Key Laboratory of Southwestern Chinese Medicine Resources, School of Pharmacy, Chengdu University of Traditional Chinese Medicine, Chengdu, China.
State Key Laboratory of Southwestern Chinese Medicine Resources, Innovative Institute of Chinese Medicine and Pharmacy, Chengdu University of Traditional Chinese Medicine, Chengdu, China.
Front Pharmacol. 2022 Apr 26;13:890078. doi: 10.3389/fphar.2022.890078. eCollection 2022.
Tetrahydropalmatine (THP), a tetrahydroproberine isoquinoline alkaloid, is widely present in some botanical drugs, such as H.S. Lo (Menispermaceae; Radix stephaniae epigaeae), (Y.H.Chou & Chun C.Hsu) W.T. Wang ex Z.Y. Su and C.Y. Wu (Papaveraceae; Corydalis rhizoma), and C.K.Schneid (Berberidaceae; Phellodendri chinensis cortex). THP has attracted considerable attention because of its diverse pharmacological activities. In this review, the chemical properties, plant sources, pharmacological activities, pharmacokinetic and toxicological characteristics of THP were systematically summarized for the first time. The results indicated that THP mainly existed in and families. Its pharmacological activities include anti-addiction, anti-inflammatory, analgesic, neuroprotective, and antitumor effects. Pharmacokinetic studies showed that THP was inadequately absorbed in the intestine and had rapid clearance and low bioavailability , as well as self-microemulsifying drug delivery systems, which could increase the absorption level and absorption rate of THP and improve its bioavailability. In addition, THP may have potential cardiac and neurological toxicity, but toxicity studies of THP are limited, especially its long-duration and acute toxicity tests. In summary, THP, as a natural alkaloid, has application prospects and potential development value, which is promising to be a novel drug for the treatment of pain, inflammation, and other related diseases. Further research on its potential target, molecular mechanism, toxicity, and oral utilization should need to be strengthened in the future.
四氢巴马汀（THP）是一种四氢原小檗碱异喹啉生物碱，广泛存在于一些植物药中，如华千金藤（防己科；千金藤属植物地不容的根）、夏天无（罂粟科；伏生紫堇的块茎）和黄柏（小檗科；黄檗的树皮）。由于其多样的药理活性，THP已引起了相当大的关注。在本综述中，首次系统总结了THP的化学性质、植物来源、药理活性、药代动力学和毒理学特征。结果表明，THP主要存在于防己科和罂粟科植物中。其药理活性包括抗成瘾、抗炎、镇痛、神经保护和抗肿瘤作用。药代动力学研究表明，THP在肠道中吸收不足，清除迅速且生物利用度低，以及自微乳化药物递送系统，可提高THP的吸收水平和吸收率并改善其生物利用度。此外，THP可能具有潜在的心脏和神经毒性，但THP的毒性研究有限，尤其是其长期和急性毒性试验。总之，THP作为一种天然生物碱，具有应用前景和潜在的开发价值，有望成为治疗疼痛、炎症及其他相关疾病的新型药物。未来需要进一步加强对其潜在靶点、分子机制、毒性和口服利用率的研究。
