Matrin ve oksimatrinin mikrobiyal transformasyonu ve metabolitlerinin in vitro biyolojik aktivitelerinin incelenmesi

Amaç: Matrin ve oksimatrin bileşiklerinin mikrobiyal transformasyon yolu ile metabolitlerin karşılaştırmalı olarak biyolojik aktivitelerinin incelenmesi hedeflenmiştir. Yöntem:30 farklı mikroorganizmanın sıvı besiyerinde üretilmesinden sonra, substratların ayrı ayrı ortama eklenerek yeni maddelere dönüşümü gözlemlenmiştir. Üretilen yeni maddeler besiyerinden uygun koşullarda ekstre edilerek, İnce Tabaka Kromatografisi ile maddelerin varlığı tespit edilmiştir. Antimikrobiyal aktivitePseudomonas aeruginosa ATCC 10145, Escherichia coli NRLL B-3008,Streptococcus epidermidis ATCC 14990, Staphylococcus aureus ATCC 6538, Helicobacter pylori ATCC 43504 ve Candida albicans ATCC 90028mikroorganizmalarına karşı mikrodilüsyon yöntemi kullanılarak incelenmiştir. Asetilkolinesteraz enzim inhibisyonu Ellman metodu ile araştırılmıştır. 5-lipooksijenaz enzim inhibisyonu deneyleri ise kolorimetrik yöntemlebelirlenmiştir. Bulgular: Matrin substratından Mucor ramannianus ve Enterococcus faecalis ile mikrobiyal biyotransformasyon sonucu iki metabolit (M1 ve M2) oluşmuştur. Oksimatrin substratının beş farklı mikroorganizma ile biyotransformasyonu sonucu matrin metabolit olarak elde edilmiştir. Sonuç: Matrin, oksimatrin, M1 ve M2 metabolitlerinin antimikrobiyal açıdan etkili olmadığı tespit edilmiştir. Matrin (%10.47), oksimatrin (%21.11), M1 (%24.23) ve M2 (%26.42)’nin 5-LOX enzim inhibisyonu açısından standart NDGA (%96.35) ile kıyaslandığında orta düzeyde aktivite gösterdiği görülmüştür. Asetilkolinesteraz/ bütirilkolinesteraz enzim inhibisyonu matrin (%34.16/ %20.49), oksimatrin (%23.68/ %22.76), M1 (%27.72/ %22.05) ve M2 (%30.63/ %23.98) açısından değerlendirildiğinde ise metabolitlerde az da olsa aktivitede artış gözlemlenmiştir.

Anahtar Kelimeler:

Biyotransformasyon, kolinesteraz, lipooksijenaz, matrin, oksimatrin

Microbial transformations of matrine and oxymatrine and in vitro biological evaulation of metabolites

Aim: It is aimed to examine the comparative biological activities of metabolites of matrine and oxymatrine compounds which were obtained by microbial transformation. Methods: After the cultivation of 30 different microorganisms in liquid medium, the transformation of substrates to new media was observed by adding them separately. The metabolites were initially identified by thin layer chromatography. Antimicrobial activity was investigated by microdilution method against microorganisms of Pseudomonas aeruginosa ATCC 10145, Escherichia coli NRLL B-3008, Staphylococcus aureus ATCC 6538, Helicobacter pylori ATCC 43504, Streptococcus epidermidis ATCC 14990, andCandida albicans ATCC 90028. The acetylcholinesterase enzyme inhibition was investigated by Ellman's method. 5-lipoxygenase enzyme inhibition experiments were determined by Baylac’s colorimetric method. Results: The biotransformation of the matrine with Mucor ramannianus and Enterococcus faecalis resulted in two metabolites (M1 and M2). Matrine was obtained as a metabolite by the biotransformation of oxymatrine with 5 different microorganisms. Conclusion: Matrine, oxymatrine, M1 and M2 metabolites were not effective for antimicrobial activity. Matrine (10.47%), oxymatrine (21.11%), M1 (24.23%) and M2 (26.42%) metabolites showed moderate activity compared to standard NDGA (96.35%) for 5-lipoxygenase enzyme inhibition. When acetylcholinesterase/ butyrylcholinesterase enzyme inhibitions are evaluated in terms of matrine (34,16%/ 20,49%), oxymatrine (23.68%/ 22.76%), M1 (27.72%/ 22.05%) and M2 (30.63%/23.98%) however, a slight increase in activity was observed in metabolites.

Keywords:

Biotransformation, cholinesterase, lipoxygenase, matrine, oxymatrine,

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