A Comprehensive Review on the Chemical Properties, Plant Sources, Pharmacological Activities, Pharmacokinetic and Toxicological Characteristics of Tetrahydropalmatine

Abstract

Tetrahydropalmatine (THP), a tetrahydroproberine isoquinoline alkaloid, is widely present in some botanical drugs, such as Stephania epigaea H.S. Lo (Menispermaceae; Radix stephaniae epigaeae), Corydalis yanhusuo (Y.H.Chou & Chun C.Hsu) W.T. Wang ex Z.Y. Su and C.Y. Wu (Papaveraceae; Corydalis rhizoma), and Phellodendron chinense 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 Papaveraceae and Menispermaceae 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 in vivo, 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.

Large‐scale separation of alkaloids from Corydalis decumbens by pH‐zone‐refining centrifugal partition chromatography and their anticomplement activity

“…Tetrahydropalmatine, which is majorly extracted from Corydalis and Stephania, exerts multiple bioactive properties, such as anti-addiction, anti-oxidation, anti-coagulation, and antiviral effects [29]. Recent studies have reported that tetrahydropalmatine exhibits anti-inflammatory activities by reducing the release of inflammatory cytokines (TNF-α, IL-1, and IL-6) related to the nuclear factor κB and tumor necrosis factor-receptor associated factor-6/c-Jun N-terminal kinase signaling pathways [30][31][32]. The results of this study show that tetrahydropalmatine exhibits anticomplement activity, acting on C1q, C3, C4, and C5 components in the complement activation cascade.…”

High-Throughput Sequencing Reveals That Rotundine Inhibits Colorectal Cancer by Regulating Prognosis-Related Genes

“…It is included in the Chinese Pharmacopoeia. Rotundine has been reported to be widely used for its analgesic and hypnotic effects [ 5 , 6 ], and its pharmacological effects include anti-inflammatory, anti-virus, and anti-tumor [ 7 ]. For example, L-THP inhibits the growth of hepatocellular carcinoma by promoting HepG2 cell autophagy through activation of the AMPK pathway [ 8 ].…”

Corydalis and Drug-Induced Liver Injury: A Series of 2 Cases

“…Studies in cells and rodents have demonstrated anti-inflammatory, neuroprotective, anti-tumor, antihypertensive, cholesterol-lowering, and anticirrhotic properties, among others. [2][3][4][5][6][7][8] Yet, there have also been human studies implicating it as a cause of drug-induced liver injury. In one study, rechallenging with kedaling tablets, which contain extract of corydalis, demonstrated elevations in aspartate transaminase, alanine transaminase, alkaline phosphatase (ALP), and g-glutamyl transferase.…”