从海洋海绵中分离得到的抗利什曼原虫和细胞毒性化合物。

Anti-leishmanial and cytotoxic compounds isolated from marine sponge .

机构信息

Department of Pharmacognosy, Faculty of Pharmacy, Minia University, Minia, Egypt.

National Center for Natural Products Research, School of Pharmacy, University of Mississippi, University, Mississippi, USA.

出版信息

Nat Prod Res. 2024 Oct;38(20):3581-3587. doi: 10.1080/14786419.2023.2256448. Epub 2023 Sep 10.

DOI:10.1080/14786419.2023.2256448

PMID:37690006

Abstract

The methanolic extract of the marine sponge . yielded two new compounds; 1-(2'-methyl heptadecyl) phenol () and a new pyrazole derivative; 4-(hydroxymethyl)-1-pyrazol-3-ol (), together with previously isolated (2')-2'-hydroxy-N-((2,3,4)-1,3,4-trihydroxy-16-methylpentadecan-2-yl)docosanamide (), cholesterol (), 5, 8-dioxycholest-6-en-3-ol () and 3-acetylsesterstatin 3 (), which were firstly reported from family Hymedesmiidae. Their structure elucidation was based on extensive nuclear magnetic resonance spectroscopy and high resolution-electrospray ionization-mass spectrometry. The isolated compounds were evaluated for their anti-leishmanial and cytotoxic activities. Compound showed remarkable anti-leishmanial activity with IC value of 15.8 ± 0.92 µg/mL comparable with the standard miltefosine (IC = 3.2 ± 0.07 µg/mL), while compound exhibited noteworthy cytotoxicity against A594 cell line with IC value of 29.6 ± 1.68 µg/mL compared to etoposide (IC = 10.9 ± 1.30 µg/mL).

摘要

海洋海绵的甲醇提取物产生了两个新化合物；1-(2'-甲基十七烷基)苯酚()和一个新的吡唑衍生物；4-(羟甲基)-1-吡唑-3-醇()，以及先前分离出的(2')-2'-羟基-N-((2,3,4)-1,3,4-三羟基-16-甲基十五烷-2-基)二十二酰胺()、胆固醇()、5,8-二氧代胆甾-6-烯-3-醇()和 3-乙酰酯甾醇 3()，这些化合物首次从 Hymedesmiidae 科中分离出来。它们的结构阐明是基于广泛的核磁共振光谱和高分辨率电喷雾电离质谱。对分离得到的化合物进行了抗利什曼原虫和细胞毒性活性评价。化合物显示出显著的抗利什曼原虫活性，IC 值为 15.8±0.92μg/mL，与标准米替福新(IC=3.2±0.07μg/mL)相当，而化合物对 A594 细胞系显示出显著的细胞毒性活性，IC 值为 29.6±1.68μg/mL，与依托泊苷(IC=10.9±1.30μg/mL)相比。