Article
Chemistry, Multidisciplinary
Jing Lin, Qi-Ming Liang, Yuan-Na Ye, Di Xiao, Li Lu, Meng-Yue Li, Jian-Ping Li, Yu-Fei Zhang, Zhuang Xiong, Na Feng, Chen Li
Summary: Novel α-glucosidase inhibitors were synthesized and compounds 3d, 3f, and 3i showed significant inhibition. Kinetic mechanism study and molecular docking demonstrated the affinity between these compounds and α-glucosidase.
FRONTIERS IN CHEMISTRY
(2022)
Article
Biochemistry & Molecular Biology
Loghman Alaei, Zhila Izadi, Samira Jafari, Fatemeh Jahanshahi, Mehdi Jaymand, Pantea Mohammadi, Bilal Ahamad Paray, Anwarul Hasan, Mojtaba Falahati, Behrang Shiri Varnamkhasti, Ali Akbar Saboury, Zahra Moosavi-Nejad, Mehrnaz Sheikh-Hosseini, Hossein Derakhshankhah
Summary: In this study, the structure-activity relationship and kinetics of thermal inactivation of alpha-glucosidase A (AglA) were investigated using p-nitrophenyl alpha-D-glucopyranoside as the synthetic substrate in a potassium phosphate buffer at pH 6.8. The Arrhenius plot showed a biphasic appearance in the thermal inactivation rate constant before and after 45 degrees C, indicating the involvement of contact areas and active centers in the enzyme inactivation process.
JOURNAL OF BIOMOLECULAR STRUCTURE & DYNAMICS
(2021)
Article
Chemistry, Applied
Shan Wang, Yue Li, Dejian Huang, Shangwei Chen, Yongmei Xia, Song Zhu
Summary: This study demonstrated that the inhibitory activities of CA derivatives on enzymes were enhanced as lipophilicity increased, with C12-CA showing the strongest inhibitory effects. The effects of C12-CA on the microenvironments and secondary structures of the enzymes were greater than those of CA and other derivatives.
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
Mussarat Tasleem, Saeed Ullah, Sobia Ahsan Halim, Ifra Urooj, Nadeem Ahmed, Rabia Munir, Ajmal Khan, Attalla F. El-kott, Parham Taslimi, Sally Negm, Ahmed Al-Harrasi, Zahid Shafiq
Summary: Diabetes mellitus is a serious global health issue, and our synthesized hydrazone derivatives show promising potential as antidiabetic agents by inhibiting the essential enzyme alpha-glucosidase.
ARCHIV DER PHARMAZIE
(2023)
Article
Biochemistry & Molecular Biology
Ke Zhao, Shiwei Sun, Hui Wang, Lin Wang, Guoqing Qin, Jiahe Fan, Mengru Guo, Wei Wang
Summary: This study identified two new rare tetracyclic triterpenoids, fortunenones A and B, from the aerial parts of Euonymus fortunei, demonstrating significant inhibitory activity against alpha-glucosidase. The enzyme kinetics analysis showed that these active compounds exhibited mixed inhibition, and molecular docking revealed the importance of hydrophobic interactions and hydrogen bonds in the inhibition of alpha-glucosidase activity. These findings indicate the potential of E. fortunei extract and its constituents in inhibiting alpha-glucosidase.
BIOORGANIC CHEMISTRY
(2021)
Article
Chemistry, Multidisciplinary
Sajedeh Safapoor, Mohammad Halimi, Minoo Khalili Ghomi, Milad Noori, Navid Dastyafteh, Shahrzad Javanshir, Samanesadat Hosseini, Somayeh Mojtabavi, Mohammad Ali Faramarzi, Ensieh Nasli-Esfahani, Bagher Larijani, Azadeh Fakhrioliaei, Mohammad G. Dekamin, Maryam Mohammadi-Khanaposhtani, Mohammad Mahdavi
Summary: A new series of quinoline-quinazolinone-thioacetamide derivatives 9a-p were designed and synthesized. These compounds showed significant anti-a-glucosidase activity, with compound 9g being the most potent inhibitor. Molecular simulation studies revealed that compound 9g occupied the active site of a-glucosidase with favorable binding energy. In silico ADMET studies of the most potent compounds predicted their drug-likeness, pharmacokinetic, and toxicity properties.
Article
Multidisciplinary Sciences
Tejaswini Maradesha, Reshma Mary Martiz, Shashank M. M. Patil, Ashwini Prasad, Abdullatif Taha Babakr, Ekaterina Silina, Victor Stupin, Raghu Ram Achar, Ramith Ramu
Summary: This study investigates the efficacy of phytocompounds from whole green jackfruit flour methanol extract (JME) in treating obesity-linked diabetes mellitus using integrated network pharmacology and molecular modeling techniques. It explores the mechanism of action of JME phytocompounds in ameliorating this condition through various analyses and simulations. The study identifies 15 predicted genes and MAPK3 as the most important gene, and suggests that JME phytocompounds could be used for further research in inhibiting MAPK3 for the treatment of obesity-linked diabetes mellitus.
Article
Biochemistry & Molecular Biology
Shao-Dan Chen, Tian-Qiao Yong, Chun Xiao, Xiong Gao, Yi-Zhen Xie, Hui-Ping Hu, Xiang-Min Li, Di-Ling Chen, Hong-Hui Pan, Qing-Ping Wu
Summary: Bioassay-guided fractionation led to the isolation of a series of triterpenoids, including 12 new ones, from the mushroom Inonotus obliquus. Some of these compounds showed strong inhibition of alpha-glucosidase activity, with Inonotusol F exhibiting the strongest inhibitory activity.
BIOORGANIC CHEMISTRY
(2021)
Article
Biochemistry & Molecular Biology
Yang Liu, Xue Zhou, Dan Zhou, Yongxing Jian, Jingfu Jia, Fahuan Ge
Summary: This study discovered that chalcomoracin, an element found in mulberry leaves, has significant inhibitory activity against alpha-glucosidase, making it a potential substitute for current hypoglycemic drugs. The inhibitory mechanism of chalcomoracin involves both competitive and non-competitive pathways. The binding of chalcomoracin and alpha-glucosidase is an entropy-driven spontaneous reaction.
Article
Biochemistry & Molecular Biology
Liang Xu, Lu Zhang, Yi-hua Li, Li-ya Li, Zuo-hua Xie, Zong-cai Tu
Summary: This study investigated the inhibitory activity and mechanism of Guavinoside B (GUB) on alpha-glucosidase. The results showed that GUB exhibited significant inhibitory ability on alpha-glucosidase, and its inhibitory activity was about 10 times that of acarbose. The study also revealed the kinetics and mechanism of inhibition.
JOURNAL OF FOOD BIOCHEMISTRY
(2022)
Article
Polymer Science
David March, Valentino Bianco, Giancarlo Franzese
Summary: This study investigated the influence of a hydrophobic surface on the behavior of proteins near interfaces, showing that the hydrophobic surface as well as other parameters affect protein unfolding and aggregation. These results have potential implications for neurodegenerative diseases.
Article
Biochemistry & Molecular Biology
Shilpi Goenka, Francis Johnson, Sanford R. Simon
Summary: This study investigated four novel chemically modified curcumin (CMC) derivatives and compared them to the parent compound curcumin for inhibition of tyrosinase activity and melanin production. The results showed that CMC2.24 exhibited the greatest efficacy as a tyrosinase inhibitor among all the CMCs, surpassing curcumin and kojic acid.
Article
Chemistry, Physical
Mandeep Kaur, Raj Kaushal
Summary: A new series of chalcone derivatives and their vanadyl complexes were designed and synthesized, showing significant abilities to lower blood sugar levels and potent enzyme inhibitory activities. Molecular docking studies and DFT calculations were used to analyze the interactions and stabilities of the complexes, revealing mixed inhibition with enzyme kinetics and remarkable antiradical activities in complex 3 and 4.
JOURNAL OF MOLECULAR STRUCTURE
(2022)
Review
Biotechnology & Applied Microbiology
Yinghui Mu, Fanjin Meng, Xin Ju, Liangzhi Li
Summary: Lignocellulosic biomass is a promising environmental resource. Enzyme catalysis is an environmentally friendly and efficient tool used for biomass conversion. Cellulase, composed of BGL, EG, and CBH, hydrolyzes cellulose into monosaccharides. This review focuses on factors affecting BGL activity during hydrolysis and proposes methods to improve BGL inactivation. It provides novel ideas for studying BGL inactivation mechanism and enhancing its activity.
APPLIED MICROBIOLOGY AND BIOTECHNOLOGY
(2023)