title: The depolymerized fucosylated chondroitin sulfate from sea cucumber potently inhibits HIV replication via interfering with virus entry.
abstract: Fucosylated chondroitin sulfate (FuCS-1) is a nontoxic and water-soluble depolymerized glycosaminoglycan obtained from the sea cucumber Thelenota ananas. Anti-HIV activities of FuCS-1 were evaluated in the present study. FuCS-1 was effective in blocking laboratory strain HIV-1IIIB entry and replication (4.26μg/mL and 0.73μg/mL, respectively), and inhibiting infection by clinic isolate HIV-1KM018 and HIV-1TC-2 (23.75μg/mL and 31.86μg/mL, respectively) as well as suppressing HIV-1 drug-resistant virus. It also inhibited HIV-2ROD and HIV-2CBL-20 replication (100μg/mL). Notably, FuCS-1 showed highly effective antiviral activity against T-20-resistant strains (EC50 values ranging from 0.76μg/mL to 1.13μg/mL). Further studies indicated that FuCS-1 can potently bind the recombinant HIV-1 gp120 protein, but no inhibition of recombinant HIV-1 reverse transcriptase was observed. In conclusion, FuCS-1 inhibited several strains of HIV-1 replication with different potencies. These results suggest that FuCS-1 may possess great potential to be further developed as novel HIV-1 entry inhibitor for treatment of HIV/AIDS patients, particularly for those infected by T-20-resistant variants.
authors: Key Laboratory of Animal Models and Human Disease Mechanisms of the Chinese Academy of Science & Yunnan Province, Kunming Institute of Zoology, Chinese Academy of Sciences, Kunming, Yunnan 650223, China; School of Basic Medical, Kunming Medical University, Kunming, Yunnan 650500, China.
authors: Ning
authors: N
authors: Huang
authors: Ming-Yi
authors: MY
authors: Wu
authors: Chang-Bo
authors: CB
authors: Zheng
authors: Lin
authors: L
authors: Zhu
authors: Jin-Hua
authors: JH
authors: Zhao
authors: Yong-Tang
authors: YT
authors: Zheng
mesh_terms: D000818:Animals; D019380:Anti-HIV Agents / Q000737:chemistry / Q000494:pharmacology*; D002460:Cell Line; D002809:Chondroitin Sulfates / Q000737:chemistry / Q000494:pharmacology*; D005643:Fucose / Q000737:chemistry*; D006678:HIV / Q000187:drug effects* / Q000502:physiology; D006801:Humans; D058105:Polymerization; D012616:Sea Cucumbers / Q000737:chemistry*; D053586:Virus Internalization / Q000187:drug effects*; D014779:Virus Replication / Q000187:drug effects*
chemical_list: D019380:Anti-HIV Agents; D005643:Fucose; D002809:Chondroitin Sulfates
keywords: Anti-HIV agent; Fucosylated chondroitin sulfate; HIV entry; HIV-1