Department of Medical Biotechnology, College of Biomedical Sciences, Kangwon National University, Chuncheon, Gangwon, 24341, Republic of Korea.
Department of Food Science and Biotechnology, College of Agriculture and Life Science, Kangwon National University, Chuncheon, Republic of Korea.
Microb Pathog. 2019 Mar;128:236-244. doi: 10.1016/j.micpath.2019.01.001. Epub 2019 Jan 3.
This work tested anti- Helicobacter pylori, free radicals scavenging and toxicity property as well as chemical constituents in the extract of chloroform (CE) and ethyl acetate (EAE) from the pedicel of Diospyros kaki L. (PDK-CE and PDK-EAE). There were 33 and 36 chemical constituents respectively in the extracts of PDK-CE and PDK-EAE, belonging to the fatty acids methyl ester, fatty acids, and stearic acids, as revealed by Gas Chromatography-Mass Spectrometry (GC-MS). The extracts did not exhibit any toxicity on NIH3T3 cells, but they significantly showed scavenging of NO, DPPH, and HO free radicals. The extracts displayed in vitro anti-H. pylori activity. PDK-CE had the maximum inhibitory zone at a minimal inhibitory concentration (MIC) of 10 μg. ml and the extract also triggered the cellular damage in the bacteria. PDK-CE extract had a high urease inhibitory activity (IC value of 8.5 μg). Further, in silico studies was performed by using 41 compounds against H. pylori urease (HPU) and H. pylori peptide deformylase (HPPD). The score value was the maximum (-19.58 kcal/mol) against HPU with 17-(5-ethyl-6-methylheptan-2-yl)-10,13-dimethyl-2,3,4,7,8,9,11,12,14,15,16,17-dodecahydro-1H-cyclopenta[a]phenanthren-3-ol, while the score value was the maximum (-14.51 kcal/mol) against HPPD with hexadecanoic acid. The results demonstrated the importance of the pedicel extracts in future pharmaceutical drug development against H. pylori infections.
本研究测试了来自柿蒂（Diospyros kaki L.）花梗的氯仿（CE）和乙酸乙酯（EAE）提取物（PDK-CE 和 PDK-EAE）的抗幽门螺杆菌、自由基清除和毒性特性以及化学成分。气相色谱-质谱联用（GC-MS）表明，PDK-CE 和 PDK-EAE 提取物分别含有 33 种和 36 种化学成分，属于脂肪酸甲酯、脂肪酸和硬脂酸。提取物对 NIH3T3 细胞没有任何毒性，但它们能显著清除 NO、DPPH 和 HO 自由基。提取物显示出体外抗幽门螺杆菌活性。PDK-CE 在最低抑菌浓度（MIC）为 10μg/ml 时具有最大抑菌圈，且该提取物还能引发细菌的细胞损伤。PDK-CE 提取物具有较高的脲酶抑制活性（IC 值为 8.5μg）。此外，还对 41 种化合物进行了针对幽门螺杆菌脲酶（HPU）和幽门螺杆菌肽脱甲酰酶（HPPD）的计算机模拟研究。HPU 的得分值最高（-19.58kcal/mol），化合物为 17-（5-乙基-6-甲基庚烷-2-基）-10,13-二甲基-2,3,4,7,8,9,11,12,14,15,16,17-十二氢-1H-环戊并[a]菲-3-醇，而 HPPD 的得分值最高（-14.51kcal/mol），化合物为十六烷酸。研究结果表明，花梗提取物在未来针对幽门螺杆菌感染的药物开发中具有重要意义。
