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Antihypertensive effects of oriental drugs in human and SHR
Published in H. Saito, Y. Yamori, M. Minami, S.H. Parvez, New Advances in SHR Research –, 2020
Hideaki Higashino, Aritomo Suzuki, Koichiro Komai
Oral intake of the second major constituent, 0.75-4.0 g coptisine, three to four times a day decreased the high blood pressure in twelve cases among thirteen patients to the normal level in 6-14 days. Since it was reported that coptisine dilated the vessel walls, preferable effects might be caused in hypertensive patients with acute nephritis or coronary insufficiency. Since berberin dilated the general vessels and decreased the blood pressure dramatically, should be careful to use the high doses of this drug in the patients with hypotension or acute infectious diseases accompanied by a shock.
Abies Spectabilis (D. Don) G. Don (Syn. A. Webbiana Lindl.) Family: Coniferae
Published in L.D. Kapoor, Handbook of Ayurvedic Medicinal Plants, 2017
Chemical constituents — The seeds yield 22 to 33% of a nauseous, bitter, nonedible oil. The stem and root of the plant contain 0.125% percent of total alkaloids, having 0.041% berberine and 0.084% of protopine. Besides the alkaloids other constituents consist of 1.10% tannins, 1.75% resin, and unidentified toxic principle in the oil.106 The crushed seeds were exposed for a week and fractioned by hydrogen chloride, resulting in seven fractions which were all toxic.107 Willaman et al.10 have reported the following alkaloids: α-allocryptopine from roots and whole plant above ground; berberine from roots, stem, leaf capsule, and seed; chelerythrine from roots; coptisine from stem, leaf, capsule, and seed; protopine from whole plant and roots; sanguinarine from roots, stem, leaf, capsule, seed, and seedlings; and an unnamed alkaloid from seeds.
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
Coptisine modulates the pharmacokinetics of florfenicol by targeting CYP1A2, CYP2C11 and CYP3A1 in the liver and P-gp in the jejunum of rats: a pilot study
Published in Xenobiotica, 2023
Si-cong Li, Min Zhang, Bin Wang, Xu-ting Li, Ge Liang
Coptisine (COP) (Figure 1) is a prominent alkaloid found in Coptis chinensis, a traditional Chinese medicine that exhibits various pharmacological effects. Its notable effects include the treatment of bacterial infections and anti-inflammatory (Kwon et al. 2016; Chen et al. 2017; Hu et al. 2019). In Chinese veterinary medicine, practitioners frequently combine COP-containing preparations with florfenicol to manage bacterial infections in animal intestines. However, the interaction between COP and florfenicol, particularly in terms of their mechanism of action, remains unclear. Although some studies have suggested that COP may modulate the expression or activity of P-gp or P450 enzymes, the exact nature of the interaction between COP and florfenicol requires further investigation.
Rollercoaster ride of kynurenines: steering the wheel towards neuroprotection in Alzheimer’s disease
Published in Expert Opinion on Therapeutic Targets, 2018
Radhika Sharma, Karan Razdan, Yashika Bansal, Anurag Kuhad
It has been found that Aβ1–42 directly stimulates IDO expression, consequently elevating the QUIN production in vitro [235] and in vivo [236]. Yu, Tao [245] investigated the effects of IDO inhibitor coptisine (one of the bioactive constituents of Oren-gedoku-to, a traditional Chinese medicine) on an AD mouse model. The study showed that oral administration of coptisine can ameliorate AD-like phenotypes both in vivo and in vitro. The inhibition of IDO by coptisine decreased the activation of microglia and astrocytes, thus preventing neuron loss, and reduced amyloid plaque formation. Consistent with the in vivo results, in vitro studies showed that coptisine could increase cell viability in PC12 cells treated by Aβ1–42 and IFN-γ.
Coptisine-induced inhibition of Helicobacter pylori: elucidation of specific mechanisms by probing urease active site and its maturation process
Published in Journal of Enzyme Inhibition and Medicinal Chemistry, 2018
Cailan Li, Ping Huang, Kambo Wong, Yifei Xu, Lihua Tan, Hanbin Chen, Qiang Lu, Chaodan Luo, Chunlai Tam, Lixiang Zhu, Ziren Su, Jianhui Xie
Our previous studies have indeed indicated that Rhizoma Coptidis and its major active alkaloids, palmatine and epiberberine, exhibit excellent anti-H. pylori activity and/or inhibit urease, possibly by binding to the urease active site and decreasing the reactivity of active-site thiols in the vicinity of nickel ions29,32,33. However, berberine fails to show any inhibitory activity against urease29. Previous reports indicate that these alkaloids might possess significantly different efficacy in their biological properties, despite their structural similarities. And the characteristic structure of alkaloids seems to be critical to their respective activities34–37. Coptisine (structure shown in Figure 1), an active protoberberine alkaloid present in Rhizoma Coptidis, has the same isoquinoline parent structure as alkaloids (berberine, palmatine, epiberberine, and jatrorrhizine) but differs in the appended groups (namely with two methylenedioxy groups). Coptisine exhibits anti-enzyme38, antimicrobial35, anti-tumour39, and gastroprotective effects40. However, comparisons of coptisine with other four alkaloids in their biological activities are rarely explored. In this study, we also found that coptisine had the strongest anti-H. pylori effects among the five major Rhizoma Coptidis alkaloids. As a follow-up study, we characterised the mechanisms underlying the anti-H. pylori activity of coptisine to better understand the anti-H. pylori effect of Rhizoma Coptidis alkaloids.