1. ChemInform Abstract: Novel Retrovirus Protease Inhibitors, RPI-856 A, B, C and D, Produced by Streptomyces sp. Al-322
- Author
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Atsushi Kakinuma, Yumiko Kitamura, Shigemi Iinuma, Tsuneo Asano, Takaki Hayakawa, Koichi Kato, Makoto Kobayashi, Kunio Matsuoka, and Tsuneaki Hida
- Subjects
Protease ,biology ,Chemistry ,Stereochemistry ,medicine.medical_treatment ,General Medicine ,Reversed-phase chromatography ,biology.organism_classification ,Streptomyces ,In vitro ,Acetic acid ,chemistry.chemical_compound ,Column chromatography ,Sephadex ,Asymmetric carbon ,medicine - Abstract
Four kinds of retrovirus protease inhibitors (RPI-856 A, B, C and D) were isolated as white powder from the culture filtrate of a soil isolate, Streptomyces sp. AL-322 by column chromatography using Diaion HP-20, Sephadex LH-20, ODS reversed phase HPLC and SP-2SW ion exchange HPLC. The structures of these inhibitors were elucidated by physico-chemical properties, chemical reactions and spectral analyses, as valyl-ADPAA-leucyl-AOPBA-valyl-valyl-aspartic acid (RPI-856 A and B) and valyl-ADPAA-leucyl-AOPBA-valyl-valine (RPI-856 C and D) [ADPAA = 2-amino-2-(3,5-dihydroxyphenyl)acetic acid, AOPBA = 3-amino-2-oxo-4-phenylbutyric acid]. RPI-856 A and B, and RPI-856 C and D were both determined to be diasteromers each other on the asymmetric carbon in AOPBA. These four inhibitors strongly inhibited in vitro HIV-1 protease and HTLV-I protease both derived from recombinant Escherichia coli with IC50 of 10(-7) approximately 10(-8) M.
- Published
- 2010
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