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Biobased Products for Viral Diseases
Published in Mahendra Rai, Chistiane M. Feitosa, Eco-Friendly Biobased Products Used in Microbial Diseases, 2022
Gleice Ribeiro Orasmo, Giovanna Morghanna Barbosa do Nascimento, Maria Gabrielly de Alcântara Oliveira, Jéssica Missilany da Costa
Tan et al. (1991) evaluated 156 pure natural products known to be reverse transcriptase (HIV-1) inhibitors, which is a useful approach in the prophylaxis and intervention of AIDS. A total of 100 plant extracts were also evaluated and 15 of these extracts showed significant inhibitory activity. The ethanolic and methanolic extracts of the plants Arctium lappa L., Viola yedoensis japonica (Nakai) Hashim. ex E. Hama, Epidemium grandiflorum C. Morren and Prunella vulgaris L. present a significant reverse transcriptase inhibition rate, thus, it is possible that they contain high concentrations of TR-HIV-1 inhibitory bioproducts in these compounds (Tan et al. 1991). The authors reported that potent HIV-1 reverse transcriptase inhibitors from natural products discovered using the present protocol include compounds from the alkaloid classes benzophenanthridine, protoberberine alkaloid, isoquinoline alkaloid and iridoid.
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.
Lappaol F, an anticancer agent, inhibits YAP via transcriptional and post-translational regulation
Published in Pharmaceutical Biology, 2021
Xiao Li, Yi-Ying Lin, Jia-Yi Tan, Kang-Lun Liu, Xiao-Ling Shen, Ying-Jie Hu, Rui-Yi Yang
Arctium lappa L. (Asteraceae), commonly known as burdock, is often used as an anticancer, anti-inflammatory, antiviral, and antidiabetic agent in traditional Chinese medicine (Chan et al. 2011). Lappaol F (LAF) is a lignanoid compound isolated from its seeds. It has been reported that LAF has antiaging activity, inhibits lipopolysaccharide-induced nitric oxide production and reverses multidrug resistance (Park et al. 2007; Su et al. 2015; Su & Wink 2015). Our previous study showed that LAF had a strong killing effect on a variety of cancer cell lines through cell cycle arrest, with minimal cytotoxicity towards normal cell lines. Moreover, LAF significantly suppressed the growth of cervical cancer xenografts in a nude mouse model (Sun et al. 2014). However, the targets responsible for the antitumour activity of LAF are currently not well understood.
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
Fructus Arctii is the dry and ripe fruit of Arctium lappa L., a biennial herb of the Compositae family. Arctium lappa L. is one of the traditional Chinese Medicine commonly used in clinic, and its leaves and roots can also be used. Traditionally, it is used for dispelling wind and clearing heat, dispersing lung and resolving phlegm, promoting pharynx and promoting body fluid, detoxification and detumescence26. Arctium lappa L. has the functions of antibacterial, antioxidant, hypoglycaemic, lipid-lowering, vasodilation, improvement of atherosclerosis, anti-tumour, anti-mutagenesis, and immune regulation, and has potential application value27.