Inhibition of Carbonic Anhydrase, Acetylcholinesterase and Butyrylcholinesterase by BisPMB, A Synthetic Analogue of Ajoene

Nashia STELLENBOOM

doi:https://doi.org/10.18596/jotcsa.484444

Makale detayları

Inhibition of Carbonic Anhydrase, Acetylcholinesterase and Butyrylcholinesterase by BisPMB, A Synthetic Analogue of Ajoene

Yazarlar:

Nashia STELLENBOOM

Yayıncı:

Turkish Chemical Society

Ana Başlıklar:

Kimya ve ilgili bilimler

Dergi:

Journal of the Turkish Chemical Society Section A: Chemistry 2019 Vol.6 Issue 2, pp.143-148

Belge Tipi:

Makale

Yayın Tarihi:

6/2019

Belge Dili:

İngilizce

Document ID (Org No.):

2000502846

Sıklık:

Üç Aylık

eISSN:

2149-0120

DOI:

https://doi.org/10.18596/jotcsa.484444

Özet:

 

BisPMB (1,8-(bis-p-methoxyphenyl)-2,3,7-trithiaocta-4-ene 7-oxide) is a synthetic
analogue of the natural compound ajoene, which is a bioactive natural product
obtained from rearrangement of the unstable and reactive organosulfur compound
allicin produced when garlic is freshly crushed. BisPMB has been shown to have
superior cancer-cell cytotoxicity compared with ajoene and a modest selectivity
towards cancer cells over non-cancerous ones. In this study, the inhibition
effects of E/Z-bisPMB and Z-bisPMB
against human carbonic anhydrase isozymes I and II (hCA I and II),
acetylcholinesterase (AChE) and butyrylcholinesterase (BuChE) were investigated
in which E/Z-bisPMB and Z-bisPMB
showed similar inhibition profiles against the four enzymes tested, with the IC50
values ranging from 10.9 to 439.7 nM and the Ki values ranging from 5.4 to 195.4 nM. Furthermore, bisPMB
was more potent at inhibiting CA I, CA II and AChE compared with commercially
available inhibitors.

Makale detayları

Inhibition of Carbonic Anhydrase, Acetylcholinesterase and Butyrylcholinesterase by BisPMB, A Synthetic Analogue of Ajoene

Yazarlar: Nashia STELLENBOOM

Yayıncı: Turkish Chemical Society

Ana Başlıklar: Kimya ve ilgili bilimler

Dergi: Journal of the Turkish Chemical Society Section A: Chemistry 2019 Vol.6 Issue 2, pp.143-148

Belge Tipi: Makale

Yayın Tarihi: 6/2019

Belge Dili: İngilizce

Document ID (Org No.): 2000502846

Sıklık: Üç Aylık

eISSN: 2149-0120

DOI: https://doi.org/10.18596/jotcsa.484444

Sayı

Yazarlar:

Nashia STELLENBOOM

Yayıncı:

Turkish Chemical Society

Ana Başlıklar:

Kimya ve ilgili bilimler

Dergi:

Journal of the Turkish Chemical Society Section A: Chemistry 2019 Vol.6 Issue 2, pp.143-148

Belge Tipi:

Makale

Yayın Tarihi:

6/2019

Belge Dili:

İngilizce

Document ID (Org No.):

2000502846

Sıklık:

Üç Aylık

eISSN:

2149-0120

DOI:

https://doi.org/10.18596/jotcsa.484444