Article
Chemistry, Medicinal
Katsuki Takashima, Mika Sakano, Eri Kinouchi, Shinya Nakamura, Shinsuke Marumoto, Fumihiro Ishikawa, Kiyofumi Ninomiya, Isao Nakanishi, Toshio Morikawa, Genzoh Tanabe
Summary: Four chain-extended analogs and two de-O-sulfonated analogs of salacinol were synthesized and evaluated for their inhibitory activities against human intestinal maltase. The results showed that elongating the side chains of salacinol was effective in increasing inhibitory activity against human intestinal maltase, making these analogs potential candidates for treating diabetes.
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
(2021)
Article
Chemistry, Applied
Qi-Wu Zhong, Tao-Shun Zhou, Wen-Hui Qiu, Ya-Kun Wang, Qiao-Li Xu, Song-Ze Ke, Si-Jia Wang, Wei-Hua Jin, Jian-Wei Chen, Hua-Wei Zhang, Bin Wei, Hong Wang
Summary: The brown seaweed Undaria pinnatifida polysaccharides have shown potential hypoglycemic effects by reducing postprandial and induced hyperglycemia through improved glucose uptake and insulin resistance. These polysaccharides could be a promising agent for diabetes treatment.
Review
Chemistry, Medicinal
Toshio Morikawa, Kiyofumi Ninomiya, Genzoh Tanabe, Hisashi Matsuda, Masayuki Yoshikawa, Osamu Muraoka
Summary: Studies have shown that active components isolated from plants in the Salacia genus have anti-diabetic effects, traditionally used in Ayurvedic medicine for early-stage diabetes treatment and widely consumed as a food supplement for obesity and diabetes prevention worldwide.
JOURNAL OF NATURAL MEDICINES
(2021)
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
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
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
Food Science & Technology
Zehong Chen, Yuxuan Liu, Dan Wang, Niuniu Wu, Kaiping Wang, Yu Zhang
Summary: In this study, sulfated modification was performed on Grifola frondosa polysaccharide (GFP) using the chlorosulfonic acid-pyridine method. The sulfated GFP (S-GFP) exhibited alpha-glucosidase inhibitory activity and changed the conformation of the enzyme. The results suggest that sulfation alters the structure and inhibitory mechanism of polysaccharides.
JOURNAL OF FUNCTIONAL FOODS
(2022)
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, Applied
Fitra Tunnisa, Didah Nur Faridah, Ani Afriyanti, Dian Rosalina, Mohamad Ana Syabana, Noviyan Darmawan, Nancy Dewi Yuliana
Summary: This study aimed to identify compounds in minor Zingiberaceae spices grown in Indonesia that are linked with antioxidant and alpha-glucosidase inhibitor activities. The results showed that Zingiber aromaticum Val., Alpinia malaccensis (Burm.f.) Roscoe, Amomum compactum Sol. ex Maton, and Zingiber purpureum Roscoe exhibited the highest antioxidant and alpha-glucosidase inhibitor activities. Furthermore, the total phenolic content positively influenced the antioxidant activities.
Article
Food Science & Technology
Yao Liu, Jingjing Zhang, Chao An, Chen Liu, Qiwen Zhang, Hao Ding, Saijian Ma, Wenjiao Xue, Daidi Fan
Summary: This study investigated the inhibition of α-glucosidase activity by ginsenoside Rg1. The results showed that Rg1 reversibly inhibited α-glucosidase activity and reduced postprandial blood glucose levels by decreasing glucose uptake and transport.
JOURNAL OF FUNCTIONAL FOODS
(2023)
Review
Food Science & Technology
Fei Ren, Nairu Ji, Yunping Zhu
Summary: Research on microbial-derived alpha-glucosidase inhibitors (alpha-GIs) is gaining attention due to the easy cultivation of microorganisms and their short life cycle. Fermentation with specific bacterial strains enhances the nutritional value of food raw materials and enables the production of hypoglycemic products. Using industrial food raw materials and processing byproducts as a medium for fermentation presents an innovative solution.
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
Biochemistry & Molecular Biology
Lotfi M. Aroua, Hind R. Almuhaylan, Fahad M. Alminderej, Sabri Messaoudi, Sridevi Chigurupati, Suliman Al-mahmoud, Hamdoon A. Mohammed
Summary: A series of benzoylarylbenzimidazole compounds were synthesized from specific routes and evaluated for their antioxidant and antidiabetic enzyme activities, showing significant activity for most compounds. Compound 3f exhibited remarkable inhibition against alpha-amylase and alpha-glucosidase, comparable to the reference drug acarbose. In silico molecular docking calculations confirmed the strong binding affinity of compounds 3a-h with human pancreatic alpha-amylase and human lysosomal acid-alpha-glucosidase active sites, supporting the excellent activity of most tested compounds.
BIOORGANIC CHEMISTRY
(2021)
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, 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)