title: Identification of antitumor lignans from the seeds of morning glory (Pharbitis nil).
abstract: In the search for antitumor compounds from Korean natural resources, activity-guided fractionation and purification processes were used on seeds of morning glory (Pharbitis nil). Air-dried P. nil seeds were extracted with ethanol and separated into n-hexane, chloroform, ethyl acetate, and n-butanol. Four new lignans, pharbilignans A-D (1-4) were isolated from the most active ethyl acetate fraction of the ethanol extract. Their structures were characterized on the basis of spectroscopic methods, including one- and two-dimensional nuclear magnetic resonance (NMR) techniques, high resolution mass spectrometry (HRMS), and circular dichroism (CD) spectroscopy. The cytotoxic activities of the isolates (1-4) were evaluated by determining their inhibitory effects on four human tumor cell lines (A549, SK-OV-3, SK-MEL-2, and HCT15) using a sulforhodamine B (SRB) bioassay. Pharbilignan C (3) showed potent cytotoxicity against A549, SK-OV-3, SK-MEL-2, and HCT-15 cell lines with IC50 values of 1.42, 0.16, 0.20, and 0.14 μM, respectively. On the basis of the expanded understanding that inflammation is a crucial cause in tumor progress, we also evaluated anti-inflammatory activity of the isolates (1-4). Pharbilignan C (3) strongly inhibited nitric oxide (NO) production in the lipopolysaccharide (LPS)-activated BV-2 microglia cell line with an IC50 value of 12.8 μM.
authors.affiliation: Natural Products Laboratory, School of Pharmacy, Sungkyunkwan University , Suwon 440-746, Korea.
authors.forename: Ki Hyun
authors.initials: KH
authors.lastname: Kim
authors.forename: Kyeong Wan
authors.initials: KW
authors.lastname: Woo
authors.forename: Eunjung
authors.initials: E
authors.lastname: Moon
authors.forename: Sang Un
authors.initials: SU
authors.lastname: Choi
authors.forename: Sun Yeou
authors.initials: SY
authors.lastname: Kim
authors.forename: Sang Zin
authors.initials: SZ
authors.lastname: Choi
authors.forename: Mi Won
authors.initials: MW
authors.lastname: Son
authors.forename: Kang Ro
authors.initials: KR
authors.lastname: Lee
mesh_terms: D000893:Anti-Inflammatory Agents / Q000494:pharmacology; D000972:Antineoplastic Agents, Phytogenic / Q000737:chemistry / Q000302:isolation & purification / Q000494:pharmacology*; D045744:Cell Line, Tumor; D006801:Humans; D049915:Ipomoea nil / Q000737:chemistry*; D017705:Lignans / Q000737:chemistry / Q000302:isolation & purification / Q000494:pharmacology*; D010936:Plant Extracts / Q000737:chemistry; D056910:Republic of Korea; D012639:Seeds / Q000737:chemistry*
chemical_list: D000893:Anti-Inflammatory Agents; D000972:Antineoplastic Agents, Phytogenic; D017705:Lignans; D010936:Plant Extracts