title: Secondary metabolites from Vietnamese marine invertebrates with activity against Trypanosoma brucei and T. cruzi.
abstract: Marine-derived natural products from invertebrates comprise an extremely diverse and promising source of the compounds from a wide variety of structural classes. This study describes the discovery of five marine natural products with activity against Trypanosoma species by natural product library screening using whole cell in vitro assays. We investigated the anti-trypanosomal activity of the extracts from the soft corals and echinoderms living in Vietnamese seas. Of the samples screened, the methanolic extracts of several marine organisms exhibited potent activities against cultures of Trypanosoma brucei and T. cruzi (EC50 < 5.0 μg/mL). Among the compounds isolated from these extracts, laevigatol B (1) from Lobophytum crassum and L. laevigatum, (24S)-ergost-4-ene-3-one (2) from Sinularia dissecta, astropectenol A (3) from Astropecten polyacanthus, and cholest-8-ene-3β,5α,6β,7α-tetraol (4) from Diadema savignyi showed inhibitory activity against T. brucei with EC50 values ranging from 1.57 ± 0.14 to 14.6 ± 1.36 μM, relative to the positive control, pentamidine (EC50 = 0.015 ± 0.003 μM). Laevigatol B (1) and 5α-cholest-8(14)-ene-3β,7α-diol (5) exhibited also significant inhibitory effects on T. cruzi. The cytotoxic activity of the pure compounds on mammalian cells was also assessed and found to be insignificant in all cases. This is the first report on the inhibitory effects of marine organisms collected in Vietnamese seas against Trypanosoma species responsible for neglected tropical diseases.
authors: College of Pharmacy, Chungnam National University, Daejeon 305-764, Korea. thaonp@imbc.vast.vn.
authors: Nguyen Phuong
authors: NP
authors: Thao
authors: Chemical Biology of Pathogens Group, Institute Pasteur Korea, Seongnam-si, Gyeonggi-do 463-400, Korea. celestial7@ip-korea.org.
authors: Joo Hwan
authors: JH
authors: No
authors: College of Pharmacy, Chungnam National University, Daejeon 305-764, Korea. luyenbthoaduoc@gmail.com.
authors: Bui Thi Thuy
authors: BT
authors: Luyen
authors: Chemical Biology of Pathogens Group, Institute Pasteur Korea, Seongnam-si, Gyeonggi-do 463-400, Korea. gyongseon@ip-korea.org.
authors: Gyongseon
authors: G
authors: Yang
authors: Chemical Biology of Pathogens Group, Institute Pasteur Korea, Seongnam-si, Gyeonggi-do 463-400, Korea. runaway1010@ip-korea.org.
authors: Soo Young
authors: SY
authors: Byun
authors: Chemical Biology of Pathogens Group, Institute Pasteur Korea, Seongnam-si, Gyeonggi-do 463-400, Korea. goojh@ip-korea.org.
authors: Junghyun
authors: J
authors: Goo
authors: College of Pharmacy, Chungnam National University, Daejeon 305-764, Korea. devilkkt@nate.com.
authors: Kyung Tae
authors: KT
authors: Kim
authors: Institute of Marine Biochemistry (IMBC), Vietnam Academy of Science and Technology (VAST), 18-Hoang Quoc Viet, Caugiay, Hanoi 10000, Vietnam. cuongnx@imbc.vast.vn.
authors: Nguyen Xuan
authors: NX
authors: Cuong
authors: Institute of Marine Biochemistry (IMBC), Vietnam Academy of Science and Technology (VAST), 18-Hoang Quoc Viet, Caugiay, Hanoi 10000, Vietnam. namnguyenhoai@imbc.vast.vn.
authors: Nguyen Hoai
authors: NH
authors: Nam
authors: Institute of Marine Biochemistry (IMBC), Vietnam Academy of Science and Technology (VAST), 18-Hoang Quoc Viet, Caugiay, Hanoi 10000, Vietnam. cvminh@vast.ac.vn.
authors: Chau
authors: C
authors: Van Minh
authors: Institute of Pharmaceutical Biology and Phytochemistry (IPBP), University of Münster, PharmaCampus, Corrensstrasse 48, Münster D-48149, Germany. thomschm@uni-muenster.de.
authors: Thomas J
authors: TJ
authors: Schmidt
authors: College of Pharmacy, Chungnam National University, Daejeon 305-764, Korea. kangjss@cnu.ac.kr.
authors: Jong Seong
authors: JS
authors: Kang
authors: College of Pharmacy, Chungnam National University, Daejeon 305-764, Korea. yhk@cnu.ac.kr.
authors: Young Ho
authors: YH
authors: Kim
mesh_terms: D000818:Animals; D037421:Anthozoa / Q000378:metabolism*; D059001:Aquatic Organisms / Q000378:metabolism; D001688:Biological Products / Q000009:adverse effects / Q000494:pharmacology*; D002460:Cell Line; D002470:Cell Survival / Q000187:drug effects; D014355:Chagas Disease / Q000188:drug therapy*; D004447:Echinodermata / Q000378:metabolism*; D057809:HEK293 Cells; D056945:Hep G2 Cells; D006801:Humans; D058069:Neglected Diseases / Q000188:drug therapy; D064210:Secondary Metabolism; D014344:Trypanocidal Agents / Q000494:pharmacology; D014346:Trypanosoma brucei brucei / Q000187:drug effects; D014349:Trypanosoma cruzi / Q000187:drug effects; D014353:Trypanosomiasis, African / Q000188:drug therapy*; D014744:Vietnam
chemical_list: D001688:Biological Products; D014344:Trypanocidal Agents