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Study on exosite inhibitor of cathepsin K from Herba Ecliptae fractions
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Yi-ping JIANG1, Yan-bin WU2, Lu-ping QIN1, Qiao-yan ZHANG1, Hai-liang XIN1, Bromme Dieter3, *, Li-ming XUE1, 3, 4, *
Acta Pharmaceutica Sinica | 2017, 52(6) : 936 - 942
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Acta Pharmaceutica Sinica | 2017, 52(6): 936-942
• ORIGINAL ARTICLES·Pharmacology •
Study on exosite inhibitor of cathepsin K from Herba Ecliptae fractions
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Yi-ping JIANG1, Yan-bin WU2, Lu-ping QIN1, Qiao-yan ZHANG1, Hai-liang XIN1, Bromme Dieter3, *, Li-ming XUE1, 3, 4, *
Affiliations
  • 1. School of Pharmacy, Second Military Medical University, Shanghai 200433, China
  • 2. Academy of Integrative Medicine, Fujian University of Traditional Chinese Medicine, Fuzhou 350108, China
  • 3. The University of British Columbia, Vancouver V6T1Z3, Canada
  • 4. Institute of Chemical Toxicity and Safety Assessment, Shanghai Municipal Center for Disease Control and Prevention, Shanghai 200336, China
Published: 2017-06-12 doi: 10.16438/j.0513-4870.2016-1234
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Cathepsin K (CTSK) is considered a critical pharmaceutical target in the treatment of osteoporosis. CTSK exerts proteolytic activities against regulatory proteins besides its collagenase function, which may account for some of the adverse reactions when blocked by active site-directed inhibitors. Exosite inhibitors that can discriminate between the therapeutic collagenase and other biological activities of CTSK specifically inhibit the collagenase activity of CTSK without interfering with the other proteolytic activities of the protease. Active recombinant CTSK was expressed in Pichia pastoris, and purified by n-butyl sepharose and SP sepharose column chromatography. Herba Ecliptae is a common traditional Chinese medicine in the treatment of bone diseases. Collagenase assay and benzyloxycarbonyl-Phe-Arg-7-amido-4-methylcoumarin (Z-FR-MCA) substrate assay based on CTSK are applied to verify the exosite inhibitors. n-Butanol extract of Herba Ecliptae are the most active fraction and eclalbasaponin Ⅸ isolated from n-butanol fraction is the potential exosite inhibitor of CTSK.

cathepsin K  /  Herba Ecliptae  /  active site inhibitor  /  exosite inhibitor  /  n-butanol fraction of Herba Ecliptae  /  eclalbasaponin Ⅸ
Yi-ping JIANG, Yan-bin WU, Lu-ping QIN, Qiao-yan ZHANG, Hai-liang XIN, Bromme Dieter, Li-ming XUE. Study on exosite inhibitor of cathepsin K from Herba Ecliptae fractions[J]. Acta Pharmaceutica Sinica, 2017 , 52 (6) : 936 -942 . DOI: 10.16438/j.0513-4870.2016-1234
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Article Info
doi: 10.16438/j.0513-4870.2016-1234
  • Receive Date：2016-12-28
  • Online Date：2026-01-14
  • Published：2017-06-12
Article Data
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History
  • Received：2016-12-28
  • Revised：2017-03-13
Funding
Affiliations
    1. School of Pharmacy, Second Military Medical University, Shanghai 200433, China
    2. Academy of Integrative Medicine, Fujian University of Traditional Chinese Medicine, Fuzhou 350108, China
    3. The University of British Columbia, Vancouver V6T1Z3, Canada
    4. Institute of Chemical Toxicity and Safety Assessment, Shanghai Municipal Center for Disease Control and Prevention, Shanghai 200336, China
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表12种不同金属材料的力学参数
科
Family		 属数
Number of
genus		 种数
Number of
species		 占总种数比例
Percentage of
total species (%)		 属
Genus		 种数
Number of
species		 占总种数比例
Percentage of total
species (%)
鹅膏菌科Amanitaceae 2 11 5.26 鹅膏菌属 Amanita 10 4.78
小菇科 Mycenaceae 2 12 5.74 丝盖伞属 Inocybe 5 2.39
多孔菌科 Polyporaceae 8 14 6.70 蜡蘑属 Laccaria 5 2.39
红菇科 Russulaceae 3 23 11.00 小皮伞属 Marasmius 6 2.87
小菇属 Mycena 11 5.26
光柄菇属 Pluteus 5 2.39
红菇属 Russula 17 8.13
栓菌属 Trametes 5 2.39
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