ABSTRACT
A ethanol extract of green walnut husks (Juglans regia L.) was isolated by various chromatographic techniques yielding 5 previously unknown diarylheptanoids, namely Juglanin F (1), Juglanin G (2), Juglanin H (3), Juglanin I (4) and Juglanin J (5), respectively, together with 12 known diarylheptanoids. The structures of these 17 compounds were elucidation on the basis of spectroscopic analysis. Upon evaluation of compounds 1-5 on the human hepatoma cells HepG2, compound 3 exhibited moderate inhibitory activity with IC50 27.72⯵M.
Subject(s)
Antineoplastic Agents, Phytogenic/pharmacology , Diarylheptanoids/pharmacology , Juglans/chemistry , Plant Extracts/pharmacology , Antineoplastic Agents, Phytogenic/isolation & purification , China , Diarylheptanoids/isolation & purification , Fruit/chemistry , Hep G2 Cells , Humans , Molecular Structure , Phytochemicals/isolation & purification , Phytochemicals/pharmacologyABSTRACT
A total of five components (Catechin, Caffeic acid, Ferulic acid, Rosmarinic acid, and Amentoflavone) were identified in Periploca angustifolia leaf methanolic extract. This extract did not cause any cytotoxic effect on HepG2 cell line within the range of concentrations tested (0-400 µg mL-1). Thus, pre-treatment with 100 µg mL-1 of P. angustifolia leaf methanolic extract (PAE) significantly (p < .05) protective HepG2 cells against cytotoxicity induced by cadmium exposure. However, Cd-intoxication significantly (p < .05) increased alanine and aspartate amino transferases serum activities (ALT and AST) and bilirubin content by 1.85-, 1.13-, and 3.55-fold, respectively. The levels of hepatic antioxidant parameters including superoxide dismutase (SOD), catalase (CAT), and glutathione peroxidase (GPx) were significantly (p < .05) decreased in Cd-intoxicated rats with concomitant enhancement of lipid peroxidation. Our results showed that P. angustifolia leaf methanolic extract can induce antioxidant effects and also exerts beneficial effects for the treatment of Cd-induced hepatotoxicity.
Subject(s)
Antioxidants/pharmacology , Cadmium/toxicity , Liver/drug effects , Liver/metabolism , Oxidative Stress/drug effects , Periploca/chemistry , Phenols/pharmacology , Animals , Antioxidants/chemistry , Apoptosis/drug effects , Cell Survival/drug effects , Cytoprotection/drug effects , Fatty Acids/metabolism , Hep G2 Cells , Humans , Liver/cytology , Mice , Phenols/chemistry , RatsABSTRACT
Objective: To design and synthetise the natural products caffeic acid ester derivatives, and to study the lipid metabolic disturbance regulation activity of the derivatives. Methods: Applying caffeic acid as material, the target compounds were prepared by two routes and evaluated for antihyperlipidemic effects in HepG2 cells. Results: Ten caffeic acid ester derivatives were synthesized, and compound C5 has not yet been reported. The structures of the target compounds were identified by spectrum. Pharmacological results showed that eight derivatives had potency of lipid-regulating in different levels. In particular, compounds C3 and C5 showed significant lipid-regulating effects compared to the lead compound caffeic acid and positive drug Simvastatin. Conclusion: Compound C5 is a new caffeic acid ester derivative. The primary structure-activity relationships are discussed in this article.
