title: Cytotoxic, Anti-inflammatory, and Leishmanicidal Activities of Diterpenes Isolated from the Roots of Caesalpinia pulcherrima.
abstract: A phytochemical investigation on the chloroform extract ofCaesalpinia pulcherrimaroots led to the isolation of ten known furanocassane diterpenoids, vouacapen-5α-ol (1), 8,9,11,14-didehydrovouacapen-5α-ol (2), 6β-cinnamoyl-7β-hydroxyvouacapen-5α-ol (3), pulcherrin A (4), pulcherrin B (5), pulcherrin J (6), pulcherrimin A (7), pulcherrimin B (8), pulcherrimin C (9), and pulcherrimin E (10). Chemical transformation of3and7gave compounds 6β-hydroxyisovouacapenol C (11), 6β-cinnamoyl-7β-acetoxyvouacapen-5α-ol (12), and pulcherrimin D (13). Cytotoxicity of compounds1-13was evaluated against three cancer cell lines (MCF-7, HeLa, and PC-3). Anti-inflammatory potential of the compounds was evaluated via the oxidative burst assay using a luminol-amplified chemiluminescence technique. Leishmanicidal activity was tested against promastigotes ofLeishmania major in vitro. Compounds3, 4, 8, 9, and10were found active against all three cancer cell lines with IC50s ranging from 7.02 ± 0.31 to 36.49 ± 1.39 µM. Compounds8and13exhibited a potent inhibitory effect on reactive oxygen species generated from human whole blood phagocytes (IC50= 15.30 ± 1.10 µM and 8.00 ± 0.80 µM, respectively). Compounds3, 9, and13showed significant activity against promastigotes ofL. major(IC50= 65.30 ± 3.20, 58.70 ± 2.80, and 55.90 ± 2.40 µM, respectively).
authors.affiliation: Department of Pharmaceutical Chemistry, Faculty of Pharmacy, University of Benin, Benin City, Nigeria.
authors.forename: Osayemwenre
authors.initials: O
authors.lastname: Erharuyi
authors.affiliation: H. E. J. Research Institute of Chemistry, International Centre for Chemical and Biological Sciences, University of Karachi, Karachi, Pakistan.
authors.forename: Achyut
authors.initials: A
authors.lastname: Adhikari
authors.affiliation: Department of Pharmaceutical Chemistry, Faculty of Pharmacy, University of Benin, Benin City, Nigeria.
authors.forename: Abiodun
authors.initials: A
authors.lastname: Falodun
authors.affiliation: Dr. Panjwani Center for Molecular Medicine and Drug Research, International Center for Chemical and Biological Sciences, University of Karachi, Karachi, Pakistan.
authors.forename: Almas
authors.initials: A
authors.lastname: Jabeen
authors.affiliation: Dr. Panjwani Center for Molecular Medicine and Drug Research, International Center for Chemical and Biological Sciences, University of Karachi, Karachi, Pakistan.
authors.forename: Rehan
authors.initials: R
authors.lastname: Imad
authors.affiliation: Dr. Panjwani Center for Molecular Medicine and Drug Research, International Center for Chemical and Biological Sciences, University of Karachi, Karachi, Pakistan.
authors.forename: Muhammad
authors.initials: M
authors.lastname: Ammad
authors.affiliation: H. E. J. Research Institute of Chemistry, International Centre for Chemical and Biological Sciences, University of Karachi, Karachi, Pakistan.
authors.forename: M Iqbal
authors.initials: MI
authors.lastname: Choudhary
authors.affiliation: Department of Molecular Biology and Genetics, Faculty of Science and Arts, Yıldız Technical University, Istanbul, Turkey.
authors.forename: Nezhun
authors.initials: N
authors.lastname: Gören
mesh_terms: D000893:Anti-Inflammatory Agents / Q000737:chemistry / Q000302:isolation & purification / Q000494:pharmacology*; D029911:Caesalpinia / Q000737:chemistry*; D045744:Cell Line, Tumor; D004224:Diterpenes / Q000737:chemistry / Q000302:isolation & purification / Q000494:pharmacology*; D006801:Humans; D015394:Molecular Structure; D018517:Plant Roots / Q000737:chemistry; D014344:Trypanocidal Agents / Q000737:chemistry / Q000302:isolation & purification / Q000494:pharmacology*
chemical_list: D000893:Anti-Inflammatory Agents; D004224:Diterpenes; D014344:Trypanocidal Agents