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Medicinal Plants of China Focusing on Tibet and Surrounding Regions
Published in Raymond Cooper, Jeffrey John Deakin, Natural Products of Silk Road Plants, 2020
Jiangqun Jin, Chunlin Long, Edward J. Kennelly
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
Published in Christophe Wiart, 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.
Research progress on therapeutic targeting of quiescent cancer cells
Published in Artificial Cells, Nanomedicine, and Biotechnology, 2019
Jinhua Zhang, Jing Si, Lu Gan, Cuixia Di, Yi Xie, Chao Sun, Hongyan Li, Menghuan Guo, Hong Zhang
Moreover, dormant colorectal cancer cells are reported to respond to itraconazole, which suppresses the Wnt pathway through non-canonical Hedgehog signaling. Itraconazole treatment initially caused a proliferative burst, forcing dormant cells to cycle briefly and subsequently enter irreversible G1 cell cycle arrest and senescence [31,48]. Furthermore, tubeimoside-1 potently suppressed the growth of human prostate cancer cells via inducing oxidative stress-mediated apoptosis and G0/G1 phase arrest [49]. Arctigenin, the active component of burdock root, enhanced p27Kip1 protein levels through inhibition of Akt and stimulation of FOXO3a activity, in turn, suppressing CDK2 kinase activity and finally inducing overall inhibition of HSC proliferation and G0/G1 phase arrest [50]. Altogether, our findings suggest that dormancy can be effectively sustained through inhibition of proliferative signaling, activation of dormant pathways or delivering the components of dormant niches.
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
Arctigenin has anti-tumour effect against a variety of cancers such as pancreatic cancer, gastric cancer, colon cancer, and liver cancer. Details about the anti-cancer activity of arctigenin and its mechanism of action are given in this section.