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Piper longum (Long Pepper or Pipli) and Tinospora cordifolia (Giloy or Heart-Leaved Moonseed)
Published in Azamal Husen, Herbs, Shrubs, and Trees of Potential Medicinal Benefits, 2022
Yashashree Pradhan, Hina Alim, Nimisha Patel, Kamal Fatima Zahra, Belkıs Muca Yiğit, Johra Khan, Ahmad Ali
Piperine (Figure 12.3a) isolated from long pepper inhibits the adhesion of neutrophils to endothelium whereas piperlonguminine (Figure 12.3b) shows inhibitory activity in alpha-MSH-induced tyrosinase synthesis and reduces carcinogenesis in hamsters (Senthil et al., 2007). Piperine (Figure 12.3a) also shows effect as chemopreventive in animals having lung cancer and reduces metastasis (Selvendiran and Sakthisekaran, 2004). Piplartine and piperine (Figure 12.3a) alkaloid amide show cytotoxic activity against tumor and hence act as an antitumor agent (Bezerra et al., 2006).
Advances in research on the protective mechanisms of traditional Chinese medicine (TCM) in myocardial ischaemia-reperfusion injury
Published in Pharmaceutical Biology, 2022
Jiexin Zhang, Yonghe Hu, Han Wang, Jun Hou, Wenjing Xiao, Xudong Wen, Tingting Wang, Pan Long, Hezhong Jiang, Zhanhao Wang, Huawei Liu, Xin Chen
Reperfusion leads to intracellular Ca2+ overload, causing mitochondrial Ca2+ overload, which in turn prompts the opening of the MPTP and causes mitochondrial dysfunction (Hausenloy and Yellon 2013). We found eight kinds of Chinese herbs that reduce MI/R injury by regulating mitochondrial energy metabolism (Table 3). When reactive aldehydes are produced by oxidative stress due to sudden reperfusion of the damaged myocardium, aldehyde dehydrogenases (ALDHs) in mitochondria can convert the reactive aldehydes into harmless acids. Piperlonguminine (PPLG) is a kind of natural alkaloid extracted from Piper longum L. (Piperaceae). In a study in which a MI/R injury rat model was constructed and rat myocardial mitochondria were isolated (Yoval-Sánchez et al. 2020), PPLG was proved to reduce the levels of lipid peroxidation products, activate ALDHs to maintain mitochondrial function (No. 15 in Figure 1), and protect cardiomyocytes and tissues during MI/R injury.
Thioredoxin reductase inhibitors: updated patent review (2017-present)
Published in Expert Opinion on Therapeutic Patents, 2021
Evgeny Chupakhin, Mikhail Krasavin
The University of Nantong team patented [76] and published [77] piperlonguminine and piperine analogs having general phenyl allylidene cyclohexenone structure 13. These compounds (of which analogs 13a and 13b turned out to be rather potent, both displaying TrxR IC50 values of 0.2 μM). The same team also patented [78] and reported [79] a related series of Michael acceptors – benzylidene cyclohexanones 14 – that was also found to be inhibitory toward TrxR. Interestingly, the patent focus was more on 6-benzylidene-2-(aryl)ethynyl cyclohexenone derivatives such as 14a (TrxR IC50 20 μM) which generally showed lower potency compared to unsubstituted analogs such as 14b (TrxR IC50 0.11 μM).
Effects of Zuogui Wan on testis structure and expression of c-Kit and Oct4 in rats with impaired spermatogenesis
Published in Pharmaceutical Biology, 2020
Xiao Li, Lei Dong, Jingshang Wang, Song Sun, Bin Wang, Haisong Li
At the same time, a relevant network pharmacology study (Gao et al. 2018) has shown that the active ingredient of Zuogui Wan such as isorhamnetin, sitosterol, stigmasterol, diosgenin, sesamin, piperlonguminine, ethyl oleate, iso-fucosterol, etc., target genes AKT1, BAX, BCL2, etc., which are closely related to the spermatogenesis process. It provides an important basis for Zuogui Wan’s improving the spermatogenic disorder and improving the pluripotency of spermatogenic stem cells, and is consistent with our previous research results. However, due to the multi-target and multi-channel effects of traditional Chinese medicine formula, its specific active ingredients and mechanism of action still need further study.