Literature DB >> 33361311

Radicicol, a Novel Lead Compound against the Migratory-Stage Schistosomula of Schistosoma japonicum.

Liangxiong Xu1,2, Qiuli Liu3, Qingren Zeng4, Ping Wu1, Quan Yu3, Kongzhen Gu3, Jinghua Xue1, Xiaoyi Wei5.   

Abstract

Schistosomiasis poses a serious threat to human health and remains a major tropical and parasitic disease in more than 70 countries. Praziquantel (PZQ) has been the primary treatment for schistosomiasis for nearly 4 decades. However, its efficacy against migratory-stage schistosomula is limited. Radicicol (RAD), a β-resorcylic acid lactone derived from Paecilomyces sp. strain SC0924, was investigated as an alternative treatment for Schistosoma japonicum In vitro tests showed that within 72 h, RAD (10 μmol/liter) completely killed schistosomula of both skin and liver stages with an efficacy significantly higher than that of PZQ, although it was less potent against adult worms than PZQ. In vivo, RAD reduced worm burdens and liver eggs by 91.18% and 86.01%, respectively, by killing migratory-stage schistosomula. Optical microscopy and scanning electron microscopy revealed that RAD damaged the epiderm and tegument morphology of S. japonicum worms at various stages and altered their motility to different degrees. RAD exhibited schistosomicidal effects at different stages in vitro and in vivo, especially at the migratory stage, implying that its mechanism could be different from that of PZQ. Collectively, these results showed that RAD is promising as a lead for the development of drugs to control the migratory-stage schistosomula of S. japonicum.
Copyright © 2021 American Society for Microbiology.

Entities:  

Keywords:  Schistosoma japonicum; migratory-stage schistosomula; radicicol; schistosomicidal efficacy

Mesh:

Substances:

Year:  2021        PMID: 33361311      PMCID: PMC8092499          DOI: 10.1128/AAC.01781-20

Source DB:  PubMed          Journal:  Antimicrob Agents Chemother        ISSN: 0066-4804            Impact factor:   5.191


  27 in total

1.  The timing of reproductive cell development and movement in Schistosoma mansoni, S. japonicum, and S. haematobium, using techniques of autoradiography and transplantation.

Authors:  P M Nollen; R D Floyd; R G Kolzow; D L Deter
Journal:  J Parasitol       Date:  1976-04       Impact factor: 1.276

2.  In-vivo activity of dihydroartemisinin against Schistosoma japonicum.

Authors:  H-J Li; W Wang; G-L Qu; Y-H Tao; Y-T Xing; Y-Z Li; J-Y Wei; J-R Dai; Y-S Liang
Journal:  Ann Trop Med Parasitol       Date:  2011-03

3.  M13 phage peptide ZL4 exerts its targeted binding effect on schistosoma japonicum via alkaline phosphatase.

Authors:  Yan Liu; Shenghui Yang; Jianhua Xiao; Liang Yu; Li Chen; Ju Zou; Kegeng Wang; Sijie Tan; Zhengyang Yu; Qingren Zeng
Journal:  Int J Clin Exp Pathol       Date:  2015-02-01

4.  Development of chiral praziquantel analogues as potential drug candidates with activity to juvenile Schistosoma japonicum.

Authors:  Yang Zheng; LanLan Dong; Changyan Hu; Bo Zhao; Chunhua Yang; Chaoming Xia; Dequn Sun
Journal:  Bioorg Med Chem Lett       Date:  2014-07-22       Impact factor: 2.823

5.  Anthelmintic activity in vitro and in vivo of Baccharis trimera (Less) DC against immature and adult worms of Schistosoma mansoni.

Authors:  Rosimeire Nunes de Oliveira; Vera Lúcia Garcia Rehder; Adriana Silva Santos Oliveira; Veronica de Lourdes Sierpe Jeraldo; Arício Xavier Linhares; Silmara Marques Allegretti
Journal:  Exp Parasitol       Date:  2014-03-03       Impact factor: 2.011

Review 6.  Comparison of skin invasion among three major species of Schistosoma.

Authors:  Yi-Xun He; Bernard Salafsky; Kalyanasundaram Ramaswamy
Journal:  Trends Parasitol       Date:  2005-05

7.  Immunization of mice with cells from juvenile worms of Schistosoma japonicum provides immunoprotection against schistosomiasis.

Authors:  TieBing Zeng; LiTing Cai; QingRen Zeng; ShengHui Yang; Rong Yu; YanQin Li; HuiLong Fang; BenWen Li; ShunKe Zhang
Journal:  Sci China C Life Sci       Date:  2007-12

8.  Halohydrin and oxime derivatives of radicicol: synthesis and antitumor activities.

Authors:  Tsutomu Agatsuma; Harumi Ogawa; Kazuhito Akasaka; Akira Asai; Yoshinori Yamashita; Tamio Mizukami; Shiro Akinaga; Yutaka Saitoh
Journal:  Bioorg Med Chem       Date:  2002-11       Impact factor: 3.641

Review 9.  Drug Repurposing for Schistosomiasis: Combinations of Drugs or Biomolecules.

Authors:  Maria João Gouveia; Paul J Brindley; Fátima Gärtner; José M Correia da Costa; Nuno Vale
Journal:  Pharmaceuticals (Basel)       Date:  2018-02-05

10.  Soil-transmitted helminths and schistosomiasis among pre-school age children in a rural setting of Busia County, Western Kenya: a cross-sectional study of prevalence, and associated exposures.

Authors:  Janet Masaku; Doris W Njomo; Ann Njoka; Collins Okoyo; Faith M Mutungi; Sammy M Njenga
Journal:  BMC Public Health       Date:  2020-03-18       Impact factor: 3.295

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