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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
Alkaloids, such as jatrorrhizine, magnoflorine and palmetine (Figure 12.4i) isolated from T. cordifolia show effect against gestational diabetes by reduction in birth defects in the fetus. This effect was studied in the streptozotocin-induced diabetic rat. Root extract of giloy reduces urinary glucose levels as well as blood glucose levels. It also reduces creatinine levels (Sharma et al., 2019). Root extract also reduces serum and tissue lipid levels which further helps in the reduction of risk of coronary heart disease (Stanely and Menon, 2003).
Selected Antimalarial Plants
Published in Woon-Chien Teng, Ho Han Kiat, Rossarin Suwanarusk, Hwee-Ling Koh, Medicinal Plants and Malaria, 2016
Woon-Chien Teng, Ho Han Kiat, Rossarin Suwanarusk, Hwee-Ling Koh
Several alkaloids in the plant are found to have antimalarial activity (berberine, allocryptopine, and protopine, with IC50 [μg/ml] against W2 [chloroquine-resistant P. falciparum strain] in vitro of 0.32, 0.32, and 1.46, respectively) (Avello 2009). However, in some animal models, berberine was found to have poor oral absorption. Protopine and allocryptopine demonstrated good selectivity for Plasmodium, with low cytotoxicities. Other compounds include dehydrocorydalmine, jatrorrhizine, columbamine, and oxyberberine from the whole plant (Singh et al. 2010) and rotomexicine, mexitin, 8-methoxydihydrosanguinarine, 13-oxoprotopine, rutin, and quercetrin from the aerial parts of the methanol extract of the plant (Singh, Pandey, and Singh 2012).
Inhibiting Insulin Resistance and Accumulation of Triglycerides and Cholesterol in the Liver
Published in Christophe Wiart, Medicinal Plants in Asia for Metabolic Syndrome, 2017
Coptisine for this plant at concentration of 0.2 µg/mL reduced the accumulation of triglycerides in HepG2 cells cultured in the presence of fatty acids by 48.9%.70 Jatrorrhizine at a concentration of 15 µM reduced triglyceride contents in HepG2 cells challenged with fatty acids by 30% with modest effects on adenosine monophosphate-activated protein kinase phosphorylation.71 As for in vivo studies, Brusq et al. administered orally to rodent on high-fat diet berberine given at a dose of 100 mg/kg/day for 10 days and noted a decrease in plasma low-density lipoprotein–cholesterol by 39% and at the hepatic level a reduction of triglycerides, cholesterol, and cholesteryl ester by 23%, 27%, and 41%, respectively.69 In a subsequent study, Cao et al. provided evidence that an alkaloidal extract of rhizomes of a member of the genus Coptis Salisb. given orally to Sprague–Dawley rats on high-fat diet for 14 days at a dose of 100 mg/kg/day reduced plasma cholesterol and low-density lipoprotein–cholesterol and normalized triglycerides and high-density lipoprotein–cholesterol.73 Furthermore, this regimen doubled the production of bile in the liver and tripled the presence of bile acids in the feces.73 The extract at a dose of 100 mg/kg/day for 14 days increased the expression of peroxisome proliferator-activated receptor-α and decreased the expression of farnesoid X receptor and therefore increased the expression of cholesterol 7α-hydroxylase also known as CYP7A1, a key enzyme in bile acids synthesis from cholesterol.73 Jatrorrhizine from Coptis chinensis Franch. at a dose of 100 mg/kg to mice induced a reduction of glycaemia from 5.9 to 4.6 mmol/L and a decrease in liver glycogen from 17.4 to 8.4 mg/.74 In alloxan-induced diabetic mice the glycaemia was reduced by daily administration of jatrorrhizine oral at a dose 100 mg/kg/day for 5 days from 21.6 to 16.4 mmol.74 The enzymatic activity of succinate dehydrogenase was increased from 6.8 to 11.2 U/mg protein suggesting an increase in aerobic utilization of glucose in hepatocytes.74 In a subsequent study, this protoberberine given orally to Syrian golden hamsters at a dose of 70 mg/kg/day for 90 days lowered plasma cholesterol, triglycerides, and low-density lipoprotein–cholesterol by 20%, 43%, and 19%, respectively, and increased high-density lipoprotein–cholesterol and bile acids content in feces.75 Besides, jatrorrhizine upregulated the expression of low-density lipoprotein–cholesterol receptor and cholesterol 7α-hydroxylase but exhibited no effect on the expression of 3-hydroxy-3-methyl-glutaryl-CoA reductase and sodium-dependent bile acid transporter in hamsters.75 In human, a direct effect of berberine is improbable because oral administration of decoction of rhizomes of a member of the genus Coptis Salisb. in healthy volunteers is followed by the presence of jatrorrhizine 3-O-β-d-glucuronide, columbamine 2-O-β-d-glucuronide, jatrorrhizine 3-O-sulfate, and traces of berberine.76
Involvement of organic anion-transporting polypeptides and organic cation transporter in the hepatic uptake of jatrorrhizine
Published in Xenobiotica, 2020
Rui-Feng Liang, Wen-Jing Ge, Xian-Mei Song, Jun-Ping Zhang, Wei-Feng Cui, She-Feng Zhang, Geng-Sheng Li
Despite a wide interest in the pharmacologic effects and mechanisms of jatrorrhizine, few studies have been conducted to investigate its pharmacokinetic characterizations as well as absorption, distribution, metabolism and excretion. It was reported jatrorrhizine was present at a very low level in the blood after an oral dose administration (Yan et al., 2012). However, the concentration of jatrorrhizine in the liver is much greater than that in the blood (Wang et al., 2010). Hepatobiliary distribution of drugs in the liver is influenced by multiple determinants, such as active uptake, metabolism and biliary efflux (Swift et al., 2013). In addition to nonsaturable passive diffusion, saturable active process which involves carrier-mediated mechanisms may contribute to the specific liver distribution (Chen et al., 2018). High hepatic exposure of jatrorrhizine may be associated with transporter expressed in the cytomembrane because of poor passive permeability of jatrorrhizine.
Jatrorrhizine reduces 5-HT and NE uptake via inhibition of uptake-2 transporters and produces antidepressant-like action in mice
Published in Xenobiotica, 2019
Siyuan Sun, Sisi Zhou, Shaowei Lei, Shujie Zhu, Kai Wang, Huidi Jiang, Hui Zhou
Jatrorrhizine is a quaternary isoquinoline alkaloid (Figure 1) isolated from various plant sources, such as Coptis chinensis and other medicinal plants. It displays a wide range of biological activities, such as antibiotic (Yu et al., 2007), hypoglycemic (Patel & Mishra, 2011), antihypertensive (Han & Fang, 1989) and antiarrhythmic (Chao et al., 1989) functions and is regarded as a potential gastric prokinetic drug candidate for its efficacy in promoting gastrointestinal motility (Wu et al., 2006; Yuan et al., 2011; Zhang et al., 2012). We have demonstrated that jatrorrhizine interacts with OCT1, 2 and 3 as a substrate and inhibitor in our recent study (Li et al., 2016). However, whether jatrorrhizine is an inhibitor of PMAT has not been identified.
Recent advances towards natural plants as potential inhibitors of SARS-Cov-2 targets
Published in Pharmaceutical Biology, 2023
Zhouman He, Jia Yuan, Yuanwen Zhang, Runfeng Li, Meilan Mo, Yutao Wang, Huihui Ti
Jatrorrhizine is a tetrahydroisoquinoline alkaloid isolated from Tinospora sagittata (Oliv.) Gagnep. (Menispermaceae) and Coptis chinensis with anticancer, cholesterol-lowering, and antioxidant effects. Pooja et al. (2021) reported that good affinity of jatrorrhizine for the active site of TMPRSS2, with a binding energy of −7.5 kcal/mol. Magnoflorine is an important aporphine-type alkaloid in Coptis chinensis. Alagu Lakshmi et al. (2021) found that magnoflorine displayed a good binding to 3CLpro and S protein of SARS-CoV-2 and ACE2.