Article
Chemistry, Multidisciplinary
Daniela Rebollar-Ramos, Berenice Ovalle-Magallanes, Juan Francisco Palacios-Espinosa, Martha Lydia Macias-Rubalcava, Huzefa A. Raja, Martin Gonzalez-Andrade, Rachel Mata
Summary: An extract from the Malbranchea dendritica exhibited inhibitory activities, with compound 1 showing important inhibitory activity against yeast alpha-glucosidase and potential better drug-likeness properties, while compound 3 moderately inhibited PTP-1B in a noncompetitive fashion. Additionally, docking analysis suggested that compounds 1, 1a, and 1b bind to an allosteric site of the enzymes, providing further insights into their mechanisms of action.
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
Ryan P. Sweeney, Phillip M. Danby, Andreas Geissner, Ryan Karimi, Jesper Brask, Stephen G. Withers
Summary: Efforts have been made to find better amylase mutants through high-throughput screening, aided by the development of efficient active site titration reagents for quantitation of active mutants in crude cell lysates. The designed reagent incorporates a highly reactive fluorogenic leaving group onto unsaturated cyclitol ethers, providing a convenient titrant for alpha-amylases down to low nanomolar levels.
Article
Biochemistry & Molecular Biology
Xiao-Feng He, Ji-Jun Chen, Tian-Ze Li, Jing Hu, Xue-Mei Zhang, Chang-An Geng
Summary: The EtOH extracts of dried seeds of Alpinia katsumadai showed hypoglycemic effects on db/db mice, leading to the isolation of 16 new diarylheptanoidchalcone hybrids and 13 known analogues with antidiabetic activity. Many compounds displayed dual inhibition of alpha-glucosidase and PTP1B, with some demonstrating selective inhibition and higher activity than standard inhibitors.
BIOORGANIC CHEMISTRY
(2021)
Article
Food Science & Technology
Hui Wang, Xiaoli Kang, Shiwei Sun, Yichen Yin, Kun Jiang, Guodong Tang, Xinning Tang, Wei Wang
Summary: Roasting enhances the alpha-glucosidase inhibitory activity of pyrogallol in coffee beverages. Two potent alpha-glucosidase inhibitors, 4,4’-DP and 4,5’-DP, were identified as the thermal reaction products of pyrogallol. These compounds exhibited higher inhibitory activity compared to pyrogallol and acarbose, and showed uncompetitive and non-competitive inhibition against alpha-glucosidase, respectively. Docking simulations revealed hydrogen bonding and hydrophobic interactions between these compounds and alpha-glucosidase.
Article
Chemistry, Multidisciplinary
Xiao-Feng He, Ji-Jun Chen, Tian-Ze Li, Jing Hu, Xu-Ke Zhang, Yuan-Qiang Guo, Xue-Mei Zhang, Chang-An Geng
Summary: Two complicated flavanol-monoterpenoid hybrids, Tsaokols A and B, were isolated from Amomum tsao-ko fruits, showing significant enzyme inhibitory activity. Their structures and mechanisms of action were determined through spectroscopic analysis and docking studies.
CHINESE CHEMICAL LETTERS
(2021)
Article
Biochemistry & Molecular Biology
Haibo Wang, Senling Tang, Guoqing Zhang, Yang Pan, Wei Jiao, Huawu Shao
Summary: A series of N-substituted iminosugar C-glycosides were synthesized and tested for their inhibition on alpha-glucosidase. Compound 6e showed promise as a potent inhibitor of alpha-glucosidase and may be classified as an uncompetitive inhibitor based on enzymatic kinetic assays. The study of structure-activity relationships of these iminosugars serves as a starting point for the discovery of new alpha-glucosidase inhibitors.
Article
Chemistry, Physical
Ebrahim Saeedian Moghadam, Abdullah Mohammed Al-Sadi, Thuraya Al-Harthy, Mohammad Ali Faramarzi, Musa Shongwe, Mohsen Amini, Raid Abdel-Jalil
Summary: Diabetes, a chronic metabolic disorder, is a global health concern. In this study, a series of piperazin-1-yl benzimidazole-2-carbamates derivatives were synthesized and evaluated for their potential as α-glucosidase inhibitors. Among them, 7d-1 and 7f-2 showed the highest inhibitory activity with IC50 values of 118 and 155 μM, respectively. Kinetic studies revealed that 7d-1 is a competitive inhibitor of α-glucosidase. Molecular docking analysis provided insights into the binding interactions between these bioactive organic molecules and the amino acid residues at the active site of the enzyme.
JOURNAL OF MOLECULAR STRUCTURE
(2023)
Article
Chemistry, Applied
Raghavakumari R. Sunagar, Yadahally N. Sreerama
Summary: This study compared the phenolic profiles, antioxidant activities, DNA protection, and enzyme inhibitory properties of browntop millet extracts obtained using solvents with varying polarities (water, methanol, acetone (80%), ethanol (70%)). The results showed that acetone (80%) and ethanol (70%) were the most effective solvents for extracting millet phenolics. Gallic, caffeic, and ferulic acids were the major phenolic acids, while myricetin and kaempferol were the most abundant flavonoids in all the extracts. Phenolics extracted using 80% acetone and 70% ethanol showed significant contributions to antioxidant mechanisms and prevention of oxidative DNA damage compared to water and methanol extracts. All the millet extracts exhibited strong inhibition of alpha-glucosidase and alpha-amylase activities. These findings highlight the impact of solvents and their polarities on the extraction and bioactivities of millet phenolics, providing valuable insights for the effective utilization of browntop millet as a functional food ingredient for managing hyperglycemia.
Article
Chemistry, Medicinal
Jun Liu, Jia-Hao Li, Si-Yu Zhao, Yi-Qun Chang, Qiu-Xian Chen, Wen-Fu Wu, Shu-Meng Jiao, Haichuan Xiao, Qiang Zhang, Jian-Fu Zhao, Jun Xu, Ping-Hua Sun
Summary: In this study, a series of novel nonsugar alpha-glucosidase inhibitors were designed, synthesized, and evaluated for their inhibitory activities. Compound W24 showed promising alpha-glucosidase inhibitory effects with low cytotoxicity, making it a competitive candidate for the development of alpha-glucosidase inhibitors.
DRUG DEVELOPMENT RESEARCH
(2023)
Review
Chemistry, Medicinal
Neetu Agrawal, Manisha Sharma, Shikha Singh, Ahsas Goyal
Summary: This article presents a novel approach and progress in the treatment of type 2 diabetes with α-glucosidase inhibitors. These inhibitors effectively lower blood glucose levels and can be obtained from synthetic and natural sources. This article is of great significance for medicinal chemists in the development of clinically viable drugs.
CURRENT TOPICS IN MEDICINAL CHEMISTRY
(2022)
Article
Chemistry, Applied
Qing-Qing Lv, Juan-Juan Cao, Rui Liu, Han-Qing Chen
Summary: Two polysaccharide fractions, WXA-1 and AXA-1, were isolated from wheat bran in this study. Structural analysis revealed that they are heteropolysaccharides, with AXA-1 showing stronger inhibitory effects on enzyme activities compared to WXA-1.
Review
Chemistry, Medicinal
Alia Mushtaq, Uzma Azam, Saba Mehreen, Muhammad Moazzam Naseer
Summary: Diabetes mellitus is a major challenge in the 21st century, contributing to high mortality rates and serious health complications. Inhibiting the enzyme alpha-glucosidase has been an effective therapeutic approach for controlling hyperglycemia, but current drugs have undesirable gastrointestinal side effects. Therefore, there is a need for novel and more effective inhibitors with improved safety and pharmacological profiles. This review highlights promising alpha-glucosidase inhibitors based on aromatic heterocyclic scaffolds.
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
(2023)
Article
Biochemistry & Molecular Biology
Lingling Liu, Jianwei Chen, Xiang Li
Summary: The research aimed to investigate the alpha-glucosidase inhibitory activity of peptides derived from Changii Radix protein under various enzymatic and digestive conditions. The most active fraction, GID-3-SG2-RP-2, exhibited the highest effect, suggesting the potential role of Changii Radix peptides in the prevention and management of type 2 diabetes.
PROCESS BIOCHEMISTRY
(2021)
Article
Agriculture, Multidisciplinary
Fanshan Feng, Wei Xiang, Han Gao, Yanan Jia, Yuansong Zhang, Lingshu Zeng, Jiaxin Chen, Xianzhi Huang, Li Xu
Summary: This study quickly and accurately identified nonalkaloid alpha-glucosidase inhibitors from mulberry twigs and found that kuwanon G and kuwanon H had better inhibition activity than DNJ. The molecular docking results also showed that the action sites of these two isopentenyl flavonoids on alpha-glucosidase were different from that of DNJ.
JOURNAL OF AGRICULTURAL AND FOOD CHEMISTRY
(2022)
Article
Chemistry, Physical
A. Espinoza Vazquez, I. A. Figueroa, F. J. Rodriguez Gomez, A. Perez Vasquez, R. Mata, D. Angeles Beltran, A. Miralrio, M. Castro
Summary: Epicatechin gallate (EG), isolated from green tea, was studied as a corrosion inhibitor for metallic materials like bronze in a corrosive solution of 3% NaCl. The results showed that 10 ppm of EG is the best concentration to protect the bronze surface. Adsorption of EG onto the bronze surface follows a mixed process of physisorption-chemisorption and helps protect against nucleophilic and electrophilic attacks.
JOURNAL OF MOLECULAR STRUCTURE
(2021)
Editorial Material
Plant Sciences
Marcy J. Balunas, Gordon M. Cragg, Simon Gibbons, Rachel Mata
JOURNAL OF NATURAL PRODUCTS
(2021)
Article
Plant Sciences
Jose A. Gutierrez-Gonzalez, Araceli Perez-Vasquez, Rafael Torres-Colin, Manuel Rangel-Grimaldo, Daniela Rebollar-Ramos, Rachel Mata
Summary: Fractionation of an aqueous extract from the aerial parts of Ageratina grandifolia yielded a new natural product, 4-hydroxy-3-((S)-1'-angeloyloxy-(R)- 2', 3'-epoxy-3'-methyl)butylacetophenone (1), along with eight known compounds, including three flavonoids (2-4) and five chromenes (5-9). NMR data interpretation and DFT-calculated chemical shifts combined with DP4+ statistical and J-DP4 probability analyses allowed for the complete characterization of compound 1.
JOURNAL OF NATURAL PRODUCTS
(2021)
Article
Biochemistry & Molecular Biology
Miriam Diaz-Rojas, Huzefa Raja, Martin Gonzalez-Andrade, Jose Rivera-Chavez, Manuel Rangel-Grimaldo, Isabel Rivero-Cruz, Rachel Mata
Summary: Three undescribed compounds, named alboluteins A-C, were isolated from solid rice-based cultures of Malbranchea albolutea. These compounds showed inhibitory activity against PTP1B, with albolutein C behaving as a noncompetitive inhibitor. Docking and molecular dynamic studies indicated that the compounds prefer to bind at the allosteric site of the enzyme, providing insights into their mechanism of action.
Article
Biochemistry & Molecular Biology
Araceli Perez-Vasquez, Sofia Padilla-Mayne, Ana Laura Martinez, Jose S. Calderon, Martha L. Macias-Rubalcava, Rafael Torres-Colin, Manuel Rangel-Grimaldo, Rachel Mata
Summary: A decoction prepared from the aerial parts of Melampodium divaricatum showed antinociceptive and antihyperalgesic responses in the formalin model in mice. Two new secondary metabolites were separated from the decoction, along with flavonoids possessing noted antinociceptive properties. The major constituents of the essential oil of the plant were also analyzed, with (E)-caryophyllene identified as the main volatile compound.
CHEMISTRY & BIODIVERSITY
(2021)
Article
Chemistry, Multidisciplinary
Daniela Rebollar-Ramos, Berenice Ovalle-Magallanes, Juan Francisco Palacios-Espinosa, Martha Lydia Macias-Rubalcava, Huzefa A. Raja, Martin Gonzalez-Andrade, Rachel Mata
Summary: An extract from the Malbranchea dendritica exhibited inhibitory activities, with compound 1 showing important inhibitory activity against yeast alpha-glucosidase and potential better drug-likeness properties, while compound 3 moderately inhibited PTP-1B in a noncompetitive fashion. Additionally, docking analysis suggested that compounds 1, 1a, and 1b bind to an allosteric site of the enzymes, providing further insights into their mechanisms of action.
Article
Chemistry, Multidisciplinary
R. Jenifer Munoz-Gomez, Isabel Rivero-Cruz, Berenice Ovalle-Magallanes, Edelmira Linares, Robert Bye, Armando R. Tovar, Lilia G. Noriega, Claudia Tovar-Palacio, Rachel Mata
Summary: This study investigates the medicinal plant Peniocereus greggii roots' hypoglycemic and antihyperglycemic effects on treating diabetes. The active compounds found were a series of cholestane steroids and a new chemical entity. One of the compounds showed insulin sensitizer action. A quantification method for certain compounds in the crude drug was also developed and validated.
Review
Biochemical Research Methods
Isabel Rivero-Cruz, Jose Alberto Gutierrez-Gonzalez, Araceli Perez-Vasquez, Jose Luis Villasenor, Rachel Mata
Summary: This review summarizes the chemical and pharmacological properties of 37 species of the Ageratina genus. The results show that Ageratina plants contain various specialized metabolites with multiple biological activities, including antiviral, antioxidant, antimicrobial, anti-inflammatory, analgesic, antifeedant, larvicidal, acaricidal, antidiabetic, antiprotozoal, and wound-healing effects. However, the pharmacological potential of Ageratina genus remains largely unexplored.
COMBINATORIAL CHEMISTRY & HIGH THROUGHPUT SCREENING
(2023)
Article
Chemistry, Applied
Valeria Reyes-Perez, Vinicio Granados-Soto, Edelmira Linares, Robert Bye, Rachel Mata, Myrna Deciga-Campos
Summary: This study evaluated the effects of Zinnia grandiflora essential oil and its major compound on neuropathic pain, allodynia, and inflammation in mice. The results showed that the essential oil alleviated inflammation and allodynia, and the most abundant compounds were germacrene D and desmethylisoencecalin.
JOURNAL OF ESSENTIAL OIL RESEARCH
(2022)
Article
Electrochemistry
Gabriel Espinosa Casillas, Araceli Espinoza Vazquez, Francisco Javier Rodriguez Gomez, Araceli Perez Vasquez, Rachel Mata, Alan Miralrio, Miguel Castro, Ricardo Galvan Martinez, Ricardo Orozco Cruz
Summary: The effect of perezone concentration and the behavior of the hydrotalcite MgAl coating impregnated with perezone on AS21 magnesium alloy were studied. The results showed that perezone molecule can protect the magnesium surface, with 10 ppm concentration being the best. When the inhibitor was impregnated with hydrotalcite, the corrosion protection was significantly improved, with 91.1% inhibition efficiency. The adsorption mechanism of perezone on magnesium surfaces was elucidated using density functional theory calculations, and the formation of a protective layer was observed with SEM-EDS.
ELECTROCHIMICA ACTA
(2023)
Article
Plant Sciences
Jose A. Gutierrez-Gonzalez, Araceli Perez-Vasquez, Martin Gonzalez-Andrade, Annia Galano, Jose L. Villasenor, Rachel Mata
Summary: Four new natural chemical entities were isolated from Ageratina grandifolia, along with 11 known compounds. The structures of these compounds were determined using various techniques. Compounds 8, 10, 11, and 12 showed high affinity for calmodulin and displayed potential therapeutic and research applications.
JOURNAL OF NATURAL PRODUCTS
(2023)
Article
Plant Sciences
Sofia Padilla-Mayne, Berenice Ovalle-Magallanes, Mario Figueroa, Edelmira Linares, Robert Bye, Isabel Rivero-Cruz, Martin Gonzalez-Andrade, Rodrigo Aguayo-Ortiz, Rachel Mata
Summary: A decoction of roots from Stevia serrata Cav. showed hypoglycemic effects in mice, as did the main component. Compounds isolated from the extract demonstrated inhibitory activity against PTP1B1-400. One compound in particular reduced blood glucose levels. The volatile compounds found in S. serrata were characterized. Finally, a method to quantify the content of one of the compounds was developed.
JOURNAL OF NATURAL PRODUCTS
(2023)
Review
Biochemistry & Molecular Biology
R. Mata, L. Flores-Bocanegra, B. Ovalle-Magallanes, M. Figueroa
Summary: Diabetes is a metabolic disease with a negative economic impact. Recent research has shown that natural compounds from plants can affect key enzymes involved in glucose homeostasis. Targeting enzymes in drug discovery offers the advantage of simple assays for analyzing enzyme activity.
NATURAL PRODUCT REPORTS
(2023)
