Cytotoxic and Schistosomidal Activities of Extract, Fractions and Isolated Compounds from Zanthoxylum Leprieurii (Rutaceae)

Authors

  • Ernestine Nkwengoua Tchouboun Zondegoumb Laboratory of Medicinal Chemistry, Department of Organic Chemistry, Faculty of Sciences, University of Yaounde I; POBOX 812, Yaounde, Cameroon Laboratory of Synthesis and Drug Delivery; Department of Biological Science, State University of Paraiba-Campus I; 58071-160, Joǎo Pessoa-Praraïba, Brazil Department of Chemistry, University of Pavia, Via Taramelli 12, 27100 Pavia, Italy Postgraduate Program in Natural and Synthetic Bioactive Products. Federal University of Paraiba-Campus V; 58071-760, Joǎo Pessoa, Brazil
  • Whistler Lucain Dibahteu Tankoua Laboratory of Medicinal Chemistry, Department of Organic Chemistry, Faculty of Sciences, University of Yaounde I; POBOX 812, Yaounde, Cameroon
  • Emmanuel Mouafo Tekwu Laboratory of Tuberculosis Research and Pharmacology, Biotechnology Centre, Nkolbisson, University of Yaoundé 1, Yaoundé, Cameroon
  • Olivier Eteme Ndogo Noguchi Memorial Institute for Medical Research (NMIMR), College of Health Sciences, University of Ghana, PO Box LG581 Legon, Accra, Ghana
  • Rodrigo Santos A. de Araujo Laboratory of Medicinal Chemistry, Department of Organic Chemistry, Faculty of Sciences, University of Yaounde I; POBOX 812, Yaounde, Cameroon
  • Giovanni Vidari Laboratory of Synthesis and Drug Delivery; Department of Biological Science, State University of Paraiba-Campus I; 58071-160, Joǎo Pessoa-Praraïba, Brazil
  • Yan Liu Department of Chemistry, University of Pavia, Via Taramelli 12, 27100 Pavia, Italy
  • Shihong Luo Kunming Institute of Botany, Chinese Academy of Sciences, 132# Lanhei Road, Heilongtan, Kunming 650201, Yunnan, China
  • Shenghong Li Kunming Institute of Botany, Chinese Academy of Sciences, 132# Lanhei Road, Heilongtan, Kunming 650201, Yunnan, China
  • Francisco Jaime Bezerra Mendonça Junior Kunming Institute of Botany, Chinese Academy of Sciences, 132# Lanhei Road, Heilongtan, Kunming 650201, Yunnan, China
  • Luciana Scotti Postgraduate Program in Natural and Synthetic Bioactive Products. Federal University of Paraiba-Campus V; 58071-760, Joǎo Pessoa, Brazil
  • Marcus Tullius Scotti Postgraduate Program in Natural and Synthetic Bioactive Products. Federal University of Paraiba-Campus V; 58071-760, Joǎo Pessoa, Brazil
  • Maria do Carmo Alves de Lima Department of Antibiotics, Research Group in Therapeutic Innovation, Federal University of Pernambuco, 50670-901 Recife, Pernambuco, Brazil
  • Barthelemy Nyasse Laboratory of Medicinal Chemistry, Department of Organic Chemistry, Faculty of Sciences, University of Yaounde I; POBOX 812, Yaounde, Cameroon

Keywords:

Acridone Alkaloids, Arborinine, Scoparone, Cercariae, Cytotoxic activity, Schistosomicidal activity, Zanthoxylum leprieurii.

Abstract

Schistosomiasis is a major and chronic neglected tropical disease. The existing treatment does not kill immature schistosomes and have serious adverse side effect.  It is well known that some parasites are responsible for causing speci?c cancers in humans including bladder cancer from Schistosoma haematobium infection. So, novel drugs discovery is an urgent need. In this study, were evaluated in vitro the cytotoxic on human hepatocarcinoma (HepG2) and normal cells (Chang liver), and the schistosomicidal properties of crude extract, fractions and isolated compounds (1-Hydroxy-3-methoxy-N-methylacridone (1) described in this species from Cameroon for the first time, Scoparone (2), and Arborinine (3)) from powdered fruits of Zanthoxylum leprieurii (Rutaceae). All fractions: hexanic (FH), methylene chloride (FC), ethyl acetate (FA) and methanolic (FM) killed all the cercariae within 2 hours exposure and presents LC50 values between 2 and 3 ?g/ml; Compounds 1 and 3 also displayed a good in vitro schistosomicidal activity against cercariae with LC50 values of 78.78 and 6.98 ?g/mL, respectively. For antitumor activity compounds 1-3 and fraction FC presents good activity with IC50 values range 18.27 - 74.61 ?g/mL on HepG2 cells, however most of these were more toxic on Chang cells than to HepG2 cells, with only exception for compound 2. The acridone Arborinine (3) can constitute a good lead for the research of schistosomiasis alternative therapy, and the coumarin Scoparone (2) can be used in drug design as scaffold for design new potential anticancer agents.

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Published

2019-03-01

How to Cite

Zondegoumb, E. N. T., Dibahteu Tankoua, W. L., Mouafo Tekwu, E., Eteme Ndogo, O., A. de Araujo, R. S., Vidari, G., Liu, Y., Luo, S., Li, S., Mendonça Junior, F. J. B., Scotti, L., Tullius Scotti, M., Alves de Lima, M. do C., & Nyasse, B. (2019). Cytotoxic and Schistosomidal Activities of Extract, Fractions and Isolated Compounds from Zanthoxylum Leprieurii (Rutaceae). International Journal of Sciences: Basic and Applied Research (IJSBAR), 44(1), 209–222. Retrieved from https://gssrr.org/index.php/JournalOfBasicAndApplied/article/view/9821

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