Article
Biochemistry & Molecular Biology
Qi Dong, Na Hu, Huilan Yue, Honglun Wang
Summary: This study demonstrated that hypericin could potentially be a novel alpha-glucosidase inhibitor by using enzyme kinetics analysis, real-time interaction analysis, and molecular docking simulation. The results showed strong and fast binding affinities between hypericin and alpha-glucosidase, leading to a decrease in enzyme activity and suggesting potential for development of anti-diabetic drugs.
Article
Food Science & Technology
Fengyu Guo, Jie An, Minlong Wang, Weibo Zhang, Chong Chen, Xueying Mao, Siyuan Liu, Pengjie Wang, Fazheng Ren
Summary: In this study, Quercimeritrin was identified as a selective inhibitor of alpha-glucosidase and shown to effectively control postprandial blood glucose in vivo. The results provide insights into using flavone aglycones to improve postprandial blood glucose levels.
Article
Biochemistry & Molecular Biology
Shuang Luo, Wei Yang, Yong Huang, Zhiyun Peng, Guangcheng Wang
Summary: The synthesized triazole-phenylacetamide derivatives demonstrated potent inhibition of α-glucosidase, with 5g exhibiting the best activity. This compound acted as a mixed-type inhibitor and its binding to the enzyme's active site caused structural changes. The findings suggest that these compounds could serve as lead compounds for the development of novel α-glucosidase inhibitors.
BIOORGANIC CHEMISTRY
(2023)
Article
Food Science & Technology
Karla A. Acevedo Martinez, Elvira Gonzalezde Mejia
Summary: The study aimed to compare different varieties of chickpea, evaluate their modulation of biochemical markers for type-2 diabetes, and produce functional ingredients using bromelain. Results showed that raw chickpea had better DPPIV IC50 values, and precooked chickpea hydrolysates exhibited the highest α-glucosidase inhibition.
FOOD RESEARCH INTERNATIONAL
(2021)
Article
Chemistry, Medicinal
Jin-He Zhang, Hong-Xu Xie, Yue Li, Kai-Ming Wang, Zhiling Song, Kong-Kai Zhu, Lei Fang, Juan Zhang, Cheng-Shi Jiang
Summary: Novel (E)-2-benzylidene-N-(3-cyano-4,5,6,7-tetrahydrobenzo[b]thiophen-2-yl) hydrazine-1-carboxamide derivatives were designed and synthesized in this study, showing promising inhibitory activity against alpha-glucosidase. The most potent compound 7 exhibited non-competitive inhibition towards alpha-glucosidase and demonstrated in vivo hypoglycemic activity in sucrose-treated rats.
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
(2021)
Article
Chemistry, Applied
Yi-Kao Hu, Li Wang, Ji-Hua Wang, Meng-Jia Li, Feng Li, Jing Yang, Yong Zhao
Summary: Nine resorcinol derivatives, including two novel compounds, were isolated from the leaves of Syzygium samarangense. Among them, four compounds exhibited significant alpha-glucosidase inhibitory activities, indicating that resorcinol derivatives with long aliphatic chains may serve as promising antidiabetic alternatives.
NATURAL PRODUCT RESEARCH
(2021)
Article
Chemistry, Multidisciplinary
Hua Zhu, Xin Zhong
Summary: In this study, six flavonoid derivatives were synthesized and tested for their anti-alpha-glucosidase activities. The results showed that all derivatives exhibited excellent inhibitory effects on alpha-glucosidase, with derivative four displaying the highest activity. Further analysis of the structure-activity relationship, inhibitory mechanism, and molecular docking revealed that the bromine group was the most beneficial group for anti-alpha-glucosidase activity.
FRONTIERS IN CHEMISTRY
(2022)
Article
Chemistry, Medicinal
Bibi Fatima, Faiza Saleem, Uzma Salar, Sridevi Chigurupati, Shatha G. Felemban, Zaheer Ul-Haq, Syeda S. Tariq, Suliman A. Almahmoud, Muhammad Taha, Syed T. A. Shah, Khalid M. Khan
Summary: A library of 22 derivatives of 1,3,4-oxadiazole-2-thiol was synthesized and evaluated for its inhibitory potential against various enzymes and antioxidant activities. Most of the compounds showed good to moderate inhibition potential, with compound 3f exhibiting the highest inhibition against alpha-glucosidase and alpha-amylase enzymes.
ARCHIV DER PHARMAZIE
(2023)
Review
Plant Sciences
Neil Miller, Elizabeth Joubert
Summary: Postprandial hyperglycemia is typically treated with the oral antidiabetic drug acarbose, but the search for novel alpha-glucosidase inhibitors from plant extracts and natural sources has led to potential candidates outperforming acarbose. However, the use of nonmammalian sources for alpha-glucosidase inhibitor screening studies may limit the value of the results in identifying inhibitors with true in vivo hypoglycemic potential.
Article
Food Science & Technology
Yujia Liu, Jie Zhu, Jiamei Yu, Xu Chen, Shuyan Zhang, Yanxue Cai, Lin Li
Summary: Curcumin, a natural dietary ingredient, mildly inhibits alpha-glucosidases through a competitive inhibition mechanism, by interacting with the enzyme's active site through hydrogen bonds and steric hindrance, resulting in protein denaturation and inhibition. This study contributes to a better understanding of the application of curcumin in functional dietary foods.
INTERNATIONAL JOURNAL OF FOOD SCIENCE AND TECHNOLOGY
(2022)
Review
Microbiology
Xiaojing Wang, Jiaying Li, Jiaqi Shang, Jing Bai, Kai Wu, Jing Liu, Zhijun Yang, Hao Ou, Lei Shao
Summary: This review discusses the potential sources of alpha-glucosidase and alpha-amylase inhibitors from endophytes and marine microorganisms over the recent years, as well as the application of glycosidase inhibitors as drugs and dietary supplements. These studies are important for the future development of new microorganism-derived glycosidase inhibitors.
FRONTIERS IN MICROBIOLOGY
(2022)
Article
Chemistry, Multidisciplinary
Jun-Jie Ke, Jing Lin, Xin Zhang, Xiao-Zheng Wu, Ying-Ying Zheng, Chun-Mei Hu, Yu Kang, Kun Zhang, Zhuang Xiong, Zhi-Qiang Ma
Summary: A series of benzylidene analogs of oleanolic acid were synthesized and evaluated for their inhibitory activities against alpha-glucosidase and alpha-amylase. The results showed that all synthesized analogs exhibited effective inhibitory effects and were safe for cells.
FRONTIERS IN CHEMISTRY
(2022)
Article
Chemistry, Multidisciplinary
Xiao-Zheng Wu, Wen-Jian Zhu, Li Lu, Chun-Mei Hu, Ying-Ying Zheng, Xin Zhang, Jing Lin, Jing-Ying Wu, Zhuang Xiong, Kun Zhang, Xue-Tao Xu
Summary: A series of betulinic acid derivatives were synthesized and evaluated for their anti alpha-glucosidase activities. All derivatives exhibited stronger activities than betulinic acid and acarbose. Compound 3q showed outstanding inhibitory activity, comparable to 1100 times stronger than acarbose. It functioned as a reversible and noncompetitive a-glucosidase inhibitor. The interaction of compound 3q with a-glucosidase caused conformational and secondary structure changes. Molecular docking simulation and physicochemical parameter assessment were also conducted.
ARABIAN JOURNAL OF CHEMISTRY
(2023)
Article
Biochemistry & Molecular Biology
Nur Khaleeda Zulaikha Zolkeflee, Nurul Shazini Ramli, Azrina Azlan, Faridah Abas
Summary: This study evaluated the effect of different drying methods and ethanol:water ratios on the anti-diabetic activities of Muntingia calabura leaves. The most active extract was obtained from freeze-dried leaves extracted with 50% ethanol. Sixty-one compounds were identified from this extract, including geniposide and daidzein. These findings suggest that Muntingia calabura leaves extract could be a potential source of bioactive compounds for diabetic treatment.
Article
Clinical Neurology
Maarten J. Mackenbach, Eline A. J. Willemse, Jan J. A. van den Dorpel, Nadine A. M. E. van der Beek, Jordi Diaz-Manera, Dimitris Rizopoulos, Charlotte Teunissen, Ans T. van der Ploeg, Johanna M. P. van den Hout
Summary: This study examines the association between neurofilament light (NfL) and central nervous system (CNS) involvement in patients with classic infantile Pompe disease. The results suggest that NfL levels may serve as a potential biomarker for assessing CNS damage in this population.
Article
Chemistry, Medicinal
Shibin Zhao, Julian Maceren, Mia Chung, Samantha Stone, Raphael Geiben, Melissa L. Boby, Bradley S. Sherborne, Derek S. Tan
Summary: Antibiotic resistance is a major threat to public health, with Gram-negative bacteria presenting unique challenges due to their low permeability and efflux pumps. Limited understanding of the chemical rules for overcoming these barriers hinders antibacterial drug discovery. Efforts to address this issue, such as screening compound libraries and using cheminformatic analysis, have led to the design of sulfamidoadenosines with diverse substituents, showing potential utility in accumulation in Escherichia coli.
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
(2024)
Article
Chemistry, Medicinal
Jichun Li, Qing Li, Shuai Xia, Jiahuang Tu, Longbo Zheng, Qian Wang, Shibo Jiang, Chao Wang
Summary: This study successfully developed a short peptide mimetic as a MERS-CoV fusion inhibitor by reproducing the key recognition features of the HR2 helix. The resulting 23-mer lipopeptide showed comparable inhibitory effect to the 36-mer HR2 peptide HR2P-M2. This has important implications for developing short peptide-based antiviral agents to treat MERS-CoV infection.
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
(2024)
Article
Chemistry, Medicinal
Krista Jaunsleine, Linda Supe, Jana Spura, Sten van Beek, Anna Sandstrom, Jessica Olsen, Carina Halleskog, Tore Bengtsson, Ilga Mutule, Benjamin Pelcman
Summary: Beta(2)-adrenergic receptor agonists can stimulate glucose uptake by skeletal muscle cells and are therefore potential treatments for type 2 diabetes. The chirality of compounds has a significant impact on the activity of these agonists. This study found that certain synthesized compounds showed higher glucose uptake activity. These findings provide important information for the design of novel beta(2)AR agonists for T2D treatment.
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
(2024)
Article
Chemistry, Medicinal
Xin Xu, Jia Chen, Guan Wang, Xiaojuan Zhang, Qiang Li, Xiaobo Zhou, Fengying Guo, Min Li
Summary: The study focuses on EZH2, a promising therapeutic target for various types of cancers. Researchers designed and synthesized a series of novel derivatives aiming to enhance the EZH2 inhibition activity. Among them, compound 28 displayed potent EZH2 inhibition activity and showed high anti-proliferative effects in lymphoma cell lines and xenograft mouse models. The study suggests that compound 28 has potential as a therapeutic candidate for EZH2-associated cancers.
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
(2024)
Article
Chemistry, Medicinal
Wei Zhang, Wei Liu, Ya-Dong Zhao, Li-Zi Xing, Ji Xu, Rui-Jun Li, Yun-Xiao Zhang
Summary: This study developed a series of aromatic amide derivatives based on Rhein and investigated their inhibitory activity against alpha-Syn aggregation. Two of these compounds showed promising potential in treating Parkinson's disease by stabilizing alpha-Syn's conformation and disassembling alpha-Syn oligomers and fibrils.
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
(2024)
Article
Chemistry, Medicinal
Mani Sharma, S. S. S. S. Sudha Ambadipudi, Neeraj Kumar Chouhan, V. Lakshma Nayak, Srihari Pabbaraja, Sai Balaji Andugulapati, Ramakrishna Sistla
Summary: Therapeutically active lipids in drug delivery systems can enhance the safety and efficacy of treatment. The liposome formulation created using synthesized biologically active lipids showed additive anti-cancer effects and reduced tumorigenic potential.
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
(2024)