当前位置:
X-MOL 学术
›
Chem. Bio. Drug Des.
›
论文详情
Our official English website, www.x-mol.net, welcomes your feedback! (Note: you will need to create a separate account there.)
O-prenylated carbostyrils as a novel class of 15-lipoxygenase inhibitors: Synthesis, characterization, and inhibitory assessment
Chemical Biology & Drug Design ( IF 3 ) Pub Date : 2021-08-28 , DOI: 10.1111/cbdd.13944 Seyed Jamal Alavi 1 , Amir Zebarjadi 1 , Mahdi Hosseini Bafghi 1 , Hossein Orafai 2 , Hamid Sadeghian 1, 3
Chemical Biology & Drug Design ( IF 3 ) Pub Date : 2021-08-28 , DOI: 10.1111/cbdd.13944 Seyed Jamal Alavi 1 , Amir Zebarjadi 1 , Mahdi Hosseini Bafghi 1 , Hossein Orafai 2 , Hamid Sadeghian 1, 3
Affiliation
Catalyzed peroxidation of unsaturated lipid in animals and plants intimately is linked to the activity of 15-Lipoxygenase enzymes. Lipoxygenases (LOXs) are well known to play an important role in many acute and chronic syndromes such as inflammation, asthma, cancer, and allergy. In this study, a series of mono prenyloxycarbostyrils were synthesized and evaluated as potential inhibitors of soybean 15-Lipoxygenase (SLO) and their inhibitory potencies were compared to mono prenyloxycoumarins which had been reported in the previous works. The synthetic compounds inhibit lipoxygenase enzyme by competitive mechanism like the prenyloxy coumarins. The results showed that position and length of the prenyl moiety play the important role in lipoxygenase inhibitory activity. Among all of the synthetic compounds (coumarin and carbostyril derivatives), 5-farnesyloxycoumarin and 8-farnesyloxycarbostyril demonstrated the best inhibitory activity by IC50 values of 1.1 µM and 0.53 µM, respectively.
中文翻译:
O-异戊烯化喹诺酮作为一类新型 15-脂氧合酶抑制剂:合成、表征和抑制评估
动物和植物中不饱和脂质的催化过氧化与 15-脂氧合酶的活性密切相关。众所周知,脂氧合酶 (LOX) 在炎症、哮喘、癌症和过敏等许多急性和慢性综合征中发挥重要作用。在这项研究中,合成了一系列单异戊二烯氧基香豆素,并对其作为大豆 15-脂氧合酶 (SLO) 的潜在抑制剂进行了评估,并将其抑制效力与之前报道的单异戊二烯氧基香豆素进行了比较。合成化合物通过竞争机制抑制脂氧合酶,如异戊烯氧基香豆素。结果表明异戊二烯基的位置和长度在脂氧合酶抑制活性中起重要作用。在所有合成化合物(香豆素和喹诺酮衍生物)中,50 个 值分别为 1.1 µM 和 0.53 µM。
更新日期:2021-10-29
中文翻译:
O-异戊烯化喹诺酮作为一类新型 15-脂氧合酶抑制剂:合成、表征和抑制评估
动物和植物中不饱和脂质的催化过氧化与 15-脂氧合酶的活性密切相关。众所周知,脂氧合酶 (LOX) 在炎症、哮喘、癌症和过敏等许多急性和慢性综合征中发挥重要作用。在这项研究中,合成了一系列单异戊二烯氧基香豆素,并对其作为大豆 15-脂氧合酶 (SLO) 的潜在抑制剂进行了评估,并将其抑制效力与之前报道的单异戊二烯氧基香豆素进行了比较。合成化合物通过竞争机制抑制脂氧合酶,如异戊烯氧基香豆素。结果表明异戊二烯基的位置和长度在脂氧合酶抑制活性中起重要作用。在所有合成化合物(香豆素和喹诺酮衍生物)中,50 个 值分别为 1.1 µM 和 0.53 µM。