1. Academic Validation
  2. Phytochemical and cytotoxic studies on the leaves of Calotropis gigantea

Phytochemical and cytotoxic studies on the leaves of Calotropis gigantea

  • Bioorg Med Chem Lett. 2017 Jul 1;27(13):2902-2906. doi: 10.1016/j.bmcl.2017.04.087.
Khang D H Nguyen 1 Phu H Dang 1 Hai X Nguyen 1 Mai T T Nguyen 2 Suresh Awale 3 Nhan T Nguyen 4
Affiliations

Affiliations

  • 1 Faculty of Chemistry, VNUHCM-University of Science, 227 Nguyen Van Cu Street, District 5, Ho Chi Minh City, Viet Nam.
  • 2 Faculty of Chemistry, VNUHCM-University of Science, 227 Nguyen Van Cu Street, District 5, Ho Chi Minh City, Viet Nam; Cancer Research Laboratory, Vietnam National University, Ho Chi Minh City, 227 Nguyen Van Cu Street, District 5, Ho Chi Minh City, Viet Nam.
  • 3 Division of Natural Drug Discovery, Institute of Natural Medicine, University of Toyama, 2630 Sugitani, Toyama 930-0194, Japan. Electronic address: suresh@inm.u-toyama.ac.jp.
  • 4 Faculty of Chemistry, VNUHCM-University of Science, 227 Nguyen Van Cu Street, District 5, Ho Chi Minh City, Viet Nam; Cancer Research Laboratory, Vietnam National University, Ho Chi Minh City, 227 Nguyen Van Cu Street, District 5, Ho Chi Minh City, Viet Nam. Electronic address: ntnhan@hcmus.edu.vn.
Abstract

A new lignan, 9'-methoxypinoresinol (1), and two new glycosylated 5-hydroxymethylfurfurals, calofurfuralside A (2), and calofurfuralside B (3), together with nine known compounds (4-12) have been isolated from the active fractions, CHCl3 (IC50, 0.32μgmL-1) and EtOAc (IC50, 0.55μgmL-1) fractions of the leaves of Calotropis gigantea. Their structures were elucidated based on NMR and MS data. Among the isolated compounds, compounds 1 and 9 exhibited potent cytotoxicity against PANC-1 human pancreatic Cancer cell line under the normoglycemic condition with IC50 values of 3.7 and 3.3μM, respectively. 9'-Methoxypinoresinol (1) significantly inhibited the colony formation of PANC-1 cells in a concentration-dependent manner.

Keywords

9′-Methoxypinoresinol; Asclepiadaceae; Calotropis gigantea; Glycosylated 5-hydroxymethylfurfural; PANC-1 human pancreatic cancer cell line.

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