scholarly journals In Vitro Metabolism of 25B-NBF, 2-(4-Bromo-2,5-Dimethoxyphenyl)-N-(2-Fluorobenzyl)ethanamine, in Human Hepatocytes Using Liquid Chromatography–Mass Spectrometry

Molecules ◽  
2019 ◽  
Vol 24 (4) ◽  
pp. 818
Author(s):  
Ju-Hyun Kim ◽  
Sunjoo Kim ◽  
Jaesin Lee ◽  
Sangwhan In ◽  
Yong-Yeon Cho ◽  
...  
Keyword(s):  
Mass Spectrometry ◽  
Liquid Chromatography ◽  
High Resolution Mass Spectrometry ◽  
Human Hepatocytes ◽  
Liquid Chromatography Mass Spectrometry ◽  
Metabolic Characteristics ◽  
Hepatic Extraction Ratio ◽  
Potent Agonist

25B-NBF, 2-(4-bromo-2,5-dimethoxyphenyl)-N-(2-fluorobenzyl)ethanamine, is a new psychoactive substance classified as a phenethylamine. It is a potent agonist of the 5-hydroxytryptamine receptor, but little is known about its metabolism and elimination properties since it was discovered. To aid 25B-NBF abuse screening, the metabolic characteristics of 25B-NBF were investigated in human hepatocytes and human cDNA-expressed cytochrome P450 (CYP) and UDP-glucuronosyltransferase (UGT) enzymes using liquid chromatography–high resolution mass spectrometry. At a hepatic extraction ratio of 0.80, 25B-NBF was extensively metabolized into 33 metabolites via hydroxylation, O-demethylation, bis-O-demethylation, N-debenzylation, glucuronidation, sulfation, and acetylation after incubation with pooled human hepatocytes. The metabolism of 25B-NBF was catalyzed by CYP1A1, CYP1A2, CYP2B6, CYP2C9, CYP2C19, CYP2D6, CYP2J2, CYP3A4, and UGT2B7 enzymes. Based on these results, it is necessary to develop a bioanalytical method for the determination of not only 25B-NBF but also its metabolites in biological samples for the screening of 25B-NBF abuse.

scholarly journals Aktivitas Antimalaria Ekstrak Kasar Etanol dan Fraksi n-Heksana Rumput Bambu (Lophatherum gracile B.) secara in Vitro

ALCHEMY ◽  
2018 ◽  
Vol 6 (1) ◽  
pp. 18
Author(s):  
Ella Wulandari ◽  
Dewi Yuliani ◽  
Elok Kamilah Hayati ◽  
Roihatul Muti'ah
Keyword(s):  
Mass Spectrometry ◽  
Plasmodium Falciparum ◽  
Liquid Chromatography ◽  
Antimalarial Activity ◽  
Ethanol Extract ◽  
Hexane Fraction ◽  
Liquid Chromatography Mass Spectrometry ◽  
Mosquito Bite

<p>Malaria is a disease caused by infectious parasite <em>Plasmodium falciparum</em> and can be transmitted through mosquito bite. The aim of this research was to study antimalarial activity <em>in vitro</em> on crude ethanol extract and n-hexane fraction of bamboo grass (<em>Lophatherum gracile</em> B.). Extraction was carried out by ethanol 80% solvent and fractionation was conducted by n-hexane. Determination of antimalarial activity was subjected to <em>P. falciparum</em> strain 3D7. According to phytochemical test, crude ethanol extract contained tannin and terpenoid, whilst n-hexane fraction contained tannin and steroid. The capability of crude ethanol extract and n-hexane fraction to inhibit <em>P. falciparum</em> was represented by IC<sub>50</sub> value. The value of both samples respectively was 12.49 and 61.49 µg/mL. Identification based on LC-MS (liquid chromatography-mass spectrometry), n-hexane fraction shown the presence of tannin and steroid compounds.</p><p>  </p><p>Malaria merupakan penyakit yang disebabkan oleh infeksi parasit <em>Plasmodium falciparum</em> yang dapat ditularkan melalui gigitan nyamuk. Penelitian ini bertujuan untuk mengetahui aktivitas antimalaria secara <em>in vitro</em> pada ekstrak kasar etanol dan fraksi n-heksana rumput bambu (<em>L</em><em>ophat</em><em>h</em><em>erum gracile </em>B.). Proses ekstraksi dilakukan dengan pelarut etanol 80% dan fraksinasi dengan n-heksana. Uji aktivitas antimalaria dilakukan pada parasit <em>P. falciparum </em><em>strain</em> 3D7<em>.</em> Hasil uji fitokimia menunjukkan ekstrak etanol mengandung tanin dan terpenoid, sedangkan fraksi n-heksana mengandung tanin dan steroid. Kemampuan ekstrak etanol dan fraksi n-heksana dalam menghambat parasit <em>P. falciparum</em> menghasilkan nilai IC<sub>50</sub> masing-masing sebesar 12,49 dan 61,49 µg/mL. Identifikasi senyawa dengan KC-SM (kromatografi cair-spektrometri massa) pada fraksi n-heksana menunjukkan adanya senyawa tanin dan steroid.</p>

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