Tran Thi-Minh-Dinh, Aonbangkhen Chanat, Duong Thuc-Huy, Nguyen Thu-Hoang-Mai, Ho Minh-Truong-Tho, Chavasiri Warinthorn, Wongsuwan Sutthida, Chatwichien Jaruwan, Giao Vo Thi-Phi, Nguyen Ngoc-Hong, Kiriwan Duangnapa, Choowongkomon Kiattawee
Department of Biology, Ho Chi Minh City University of Education, 280 an Duong Vuong Street, District 5, Ho Chi Minh City, 748342, Viet Nam.
KU Institute for Advanced Studies, Kasetsart University, Bangkok, 10900, Thailand.
Heliyon. 2024 Feb 7;10(4):e25763. doi: 10.1016/j.heliyon.2024.e25763. eCollection 2024 Feb 29.
Cultured lichen mycobionts are valuable sources of new natural compounds. Mycobiont of growing in Vietnam was isolated, cultivated and chemically investigated. The crude extract of this cultured mycobiont showed potent alpha-glucosidase inhibition with an IC value of 50 μg/mL.
Multiple chromatographic methods were applied to the extract to isolate compounds. The combination of Nuclear Magnetic Resonance analysis and high-resolution mass spectroscopy determined their chemical structures. Electrophilic bromination/chlorination was applied to obtain new derivatives using NaBr/HO and NaCl/HO reagents. Compounds were evaluated for enzyme inhibitory activities, including alpha-glucosidase inhibition, HIV-1 reverse transcriptase inhibition, SARS-CoV-2 main protease (M) inhibition, anti-inflammatory activity, and cytotoxicity against several cancer cell lines. A molecular docking study for -SARS-CoV-2 was conducted to understand the inhibitory mechanism.
A new diphenyl ether, handelone () and a known compound xylarinic acid A () were isolated and elucidated. Four synthetic products 6'-bromohandelone (), 2'-bromohandelone ), 2',6'-dibromohandelone , and 2',6'-dichlorohandelone () were prepared. Compound showed good activity against M with an IC value of 5.2 μM but it showed weak or inactive activity in other tests. Other compounds were inactive in all assays.
A new compound, handelone () was isolated from the cultured mycobiont of . From these compounds, four new derivatives were prepared. Compound showed good activity against M with an IC value of 5.2 μM but it showed weak or inactive activity in other tests. Other compounds were inactive in all assays.
培养的地衣共生菌是新天然化合物的宝贵来源。对生长在越南的地衣共生菌进行了分离、培养和化学研究。该培养的地衣共生菌的粗提物显示出有效的α-葡萄糖苷酶抑制活性，IC50值为50μg/mL。
采用多种色谱方法对提取物进行分离化合物。结合核磁共振分析和高分辨率质谱确定其化学结构。使用NaBr/H2O和NaCl/H2O试剂进行亲电溴化/氯化反应以获得新的衍生物。对化合物进行酶抑制活性评估，包括α-葡萄糖苷酶抑制、HIV-1逆转录酶抑制、SARS-CoV-2主要蛋白酶（Mpro）抑制、抗炎活性以及对几种癌细胞系的细胞毒性。进行了针对SARS-CoV-2 Mpro的分子对接研究以了解抑制机制。
分离并鉴定了一种新的二苯醚化合物汉德洛酮（）和一种已知化合物木栓菌酸A（）。制备了四种合成产物：6'-溴汉德洛酮（）、2'-溴汉德洛酮（）、2',6'-二溴汉德洛酮（）和2',6'-二氯汉德洛酮（）。化合物对Mpro表现出良好的活性，IC50值为5.2μM，但在其他测试中表现出较弱或无活性。其他化合物在所有测定中均无活性。
从培养的地衣共生菌中分离出一种新化合物汉德洛酮（）。从这些化合物中制备了四种新衍生物。化合物对Mpro表现出良好的活性，IC50值为5.2μM，但在其他测试中表现出较弱或无活性。其他化合物在所有测定中均无活性。
