Medicinal Plants of China Focusing on Tibet and Surrounding Regions
Raymond Cooper, Jeffrey John Deakin in Natural Products of Silk Road Plants, 2020
Chemical constituents: More than 70 compounds have been isolated and identified, including chlorogenic acid (Figure 2.9), and other phenylpropanoids: syringin, 1,3-dicaffeoylquinicacid, 3-caffeoylquinicacid, 1,5-dicaffeoyl-4-succinoylquinicacid, 1,4-dicaffeoylquinicacid; flavonoids: rutin (Figure 2.9) hispidulin, jaceosidin, luteolin, nepetin, apigenin; coumarins: coumarin, osthol, isopimpinellin, bergapten, xanthotoxol, alloisoimperatorin, oroselol; lignans: arctigenin-4-O-(6″-O-acetyl-β-D-glucoside), arctigenin-4-O-(2″-O-acetyl-β-D-glucoside), arctigenin-4-O-(3″-O-acetyl-β-D- glucoside), arctiin, and arctigenin (Chik et al., 2015); steroids: bufotalin, telocinobufagin, gamabufotalin (Zhang et al., 2011), daucosterol, β-sitosterol; sesquiterpenes: sausinlactoneA-(1S,3S,5S,6S,7S,11S)-3-hydroxyl-11; polysaccharides: glucose, galactose, xylose, rhamnose, arabinose, and galacturonic acid; and ceramides (Chik et al., 2015).
Protecting Pancreatic β-cells from Metabolic Insults
Christophe Wiart in Medicinal Plants in Asia for Metabolic Syndrome, 2017
A total lignan fraction of fruits of Arctium lappa L. given to spontaneously diabetic Goto–Kakizaki rats at a dose of 300 mg/K twice daily before each meal for 12 weeks (nateglinide twice daily before each meal for 12 weeks, 50 mg/kg) lowered fasting blood glucose by 51.4% (nateglinide, 50 mg/kg: 19.6%) close to normal values.279 This treatment improved glucose tolerance in oral glucose tolerance test done at the end of the treatment with a 35.1% postprandial glycemia at 60 minutes.279 The fraction boosted postprandial insulinemia in Goto–Kakizaki rats (Xu et al., 2014).279 This treatment improved pancreatic histoarchitecture. The fraction had no effect on plasma cholesterol or triglycerides.279 The fraction inhibited the activity of α-glucosidase in vitro as potently as acarbose with an IC50 of about 150 µg/mL.279 Arctigenic acid which is the metabolite of arctigenin (Figure 2.20) from fruits of Arctium lappa in Goto–Kakizaki rats, given orally at a dose of 50 mg/kg twice daily for 12 weeks lowered fasting glycemia by 37.6% (nateglinide at 50 mg/kg/day: 28.1%) and attenuated body weight gain.279 The treatment improved glucose tolerance in oral glucose tolerance test.280 Arctigenin treatment (as well as nateglinide) improved pancreatic histoarchitecture with enhanced regeneration of islets.279 A fraction of roots of Arctium lappa (dicaffeoylquinic acid derivatives 75.4%) at a concentration of 100 µg/mL increased intake of glucose by L6 myotubes by 16% in the presence of insulin and was inactive in absence of insulin.280 From this extract, 5-O-caffeoylquinic acid at 100 µg/mL had similar effect.280 The fraction and 5-O-caffeoylquinic acid at 50 µg/mL inhibited glucagon-induced release of glucose by rat hepatocytes in vitro and inhibited glucose 6-phosphatase activity.280 The fraction and 5-O-caffeoylquinic acid had no effect on insulin secretion by INS in the presence of glucose.280 The fraction given orally at a dose of 15 mg/kg/day orally for 4 days lowered 30 minutes glycemia peak during oral glucose tolerance test from 9.5 to 8.4 mmol/L with a concomitant increase of insulinaemia from 1.7 to 3.6 ng/mL.281 Clinical trials are warranted.
Preclinical Evidence that Arctigenin Effectively and Selectively Targets Clear Cell Renal Cell Carcinoma Via Suppressing EGFR and RhoA
Published in Nutrition and Cancer, 2023
Dongcao Liu, Guang Zhou, Mingwei Xu
Arctigenin, derived from a Chinese herb Arctium lappa, is a bioactive lignan. It demonstrated potential health benefits via anti-viral, anti-inflammatory and anticancer activities (6–8). Arctigenin’s effects to inhibit migration and invasion, as well as induce apoptosis and cell cycle arrest have been reported in various human cancers, which included gastric, breast and lung cancers (8–10). Additionally, arctigenin can enhance chemosensitivity via different mechanisms depending on tumor types, including STAT3, β-Catenin, mTOR, and autophagy (10–13). In this work, we systematically investigated arctigenin as a single agent and its combination with clinically used anti-RCC drugs on ccRCC. Using cellular culturing system and xenograft mouse tumor model, we demonstrate that arctigenin is active against ccRCC. Arctigenin significantly augments both in vivo and in vitro efficacies of 5-FU and sorafenib in ccRCC. In our study, the arctigenin inhibitory effects in ccRCC can be attributed to RhoA inhibition as well as EGFR signaling pathways.
Arctigenin: pharmacology, total synthesis, and progress in structure modification
Published in Journal of Enzyme Inhibition and Medicinal Chemistry, 2022
Dan Wu, Lili Jin, Xing Huang, Hao Deng, Qing-kun Shen, Zhe-shan Quan, Changhao Zhang, Hong-Yan Guo
The natural product arctigenin possesses good biological activity and acts as a lead compound. The main laboratory methods that have been utilised for the production of arctigenin are silica gel column chromatography purification37,99, organic reagent extraction55,69, centrifugal partition chromatography100, and chemical combination101, chemical combination101. However, all these methods have shortcomings such as low extraction efficiency, cumbersome steps, and necessity of laboratory equipments. The low content of active ingredients in herbal medicines and reliance on isolated extraction to obtain sufficient amounts of compounds not only renders production costly, but also leads to a series of problems related to sustainable use of natural medicinal resources and environmental sustainability. Therefore, artificial synthesis of natural products with excellent activity is an important means to solve the above problems. Current studies have shown that the technology for the total synthesis of arctigenin is readily available102.
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