Studies of the binding of bisbenzylisoquinoline alkaloids to phosphatidylcholine vesicles and alveolar macrophages in relation to their antifibrogenic potential

Details

• Personal Author:
  Castranova, Vincent ; Ma JK ; Ma JY ; Malanga CJ ; Mo C
• Description:
  The relative lipophilicity and binding to phosphatidylcholine vesicles and rat alveolar macrophages of bisbenzylisoquinoline (BBIQ) alkaloids were compared and discussed in terms of their structures and antifibrogenic activities in silica (14808607) induced fibrosis. The BBIQs tested included tetrandrine (TE), fangchinoline (FA), berbamine (BE), cepharanthine (CE), tubocurine (TU), curine, cycleanine (CY) and methoxyadiantifoline (ME). ME, with nine methoxy groups, had the highest lipophilicity, followed by TE, CY, CE, FA and BE, with CU and TU, both containing two hydroxy groups, the least lipophilic. Relative binding affinities to dipalmitoyl-phosphatidylcholine lipid vesicles, measured by fluorescence and analyzed using the Scatchard equation, was consistent with the order of lipophilicity. An equilibrium dialysis method was employed to determined the binding affinities of the BBIQ alkaloids to Sprague-Dawley-rat alveolar macrophages. In this assay, TE was shown to have the greatest binding affinity, followed by ME and FA. No binding activity was detected for CU or TU. A statistical correlation between relative macrophage binding ability and antifibrotic activity was calculated. The authors conclude that the interaction of TE, ME and FA with alveolar macrophages may inhibit silica induced lung fibrosis, preventing further progression of silica induced pulmonary disease. [Description provided by NIOSH]
• Subjects:
  Lung Lung Diseases Occupational Health Respiratory System Respiratory Tract Diseases Safety
• Keywords:
  Alveolar-cells Lung-cells Lung-fibrosis Mammalian-cells Medical-treatment Molecular-structure Pulmonary-disorders Quinolines Respiratory-system-disorders Silicosis
• ISBN:
  9780873350983
• Publisher:
  Society for Mining, Metallurgy, and Exploration, Inc.
• Document Type:
  Text
• Genre:
  Proceedings
• Place as Subject:
  Colorado ; OSHA Region 3 ; OSHA Region 8 ; Pennsylvania ; West Virginia
• CIO:
  National Institute for Occupational Safety and Health (NIOSH)
• Division:
  DRDS - Division of Respiratory Disease Studies
• Topic:
  Workplace Safety & Health
• Location:
  North America
• Pages in Document:
  153-158
• NIOSHTIC Number:
  nn:00232443
• Citation:
  Respirable dust in the mineral industries, proceedings of the 3rd symposium on respirable dust in the mineral industries, October 17-19, 1990, Pittsburgh, Pennsylvania. Frantz RL, Ramani RV, eds. Littleton, CO: Society for Mining, Metallurgy, and Exploration, Inc., 1991 Jan; :153-158
• Contact Point Address:
  Joseph K.H. Ma, School of Pharmacy, West Virginia University, Morgantown, WV
• CAS Registry Number:
  Quartz (SiO2) (CAS RN 14808-60-7)
• Editor(s):
  Frantz RL; Ramani RV
• Federal Fiscal Year:
  1991
• Peer Reviewed:
  False
• Source Full Name:
  Respirable dust in the mineral industries, proceedings of the 3rd symposium on respirable dust in the mineral industries, October 17-19, 1990, Pittsburgh, Pennsylvania
• Collection(s):
  National Institute for Occupational Safety and Health
• Main Document Checksum:
  urn:sha-512:cffe7ec7f9fc857b8374953596b723caa65131cae4957f7e4861826841c7d47b6b9950a0cc7ccaec5b61e5c4f9bc74fcfb75c8fd26ae23d378ae2fb0b6979ed9
• Download URL:
  https://stacks.cdc.gov/view/cdc/205633/cdc_205633_DS1.pdf
• File Type:
  [PDF - 3.22 MB ]