4.5 Article

Synthesis of chalcone derivatives as potential anti-diabetic agents

期刊

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
卷 22, 期 12, 页码 3912-3915

出版社

PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2012.04.108

关键词

Adipocyte; Aldol condensation; Chalcone; Diabetes; Structure-activity relationship

资金

  1. National Science Council, Taiwan [NSC 98-2323-B-037-004-, 99-2323-B-037-002-]

向作者/读者索取更多资源

Chalcones bearing electron donating or electron withdrawing substitutions were prepared and their glucose uptake activity was evaluated. Chalcone derivatives were synthesized in one step protocol with high purity and yield. Chalcones with chloro, bromo, iodo and hydroxy substitutions at position 2 on A-ring exhibited the highest activity with glucose medium concentration (210 to 236 mg/dl) compared to pioglitazone and rosiglitazone (230 and 263 mg/dl, respectively). Also chalcones with iodo substitution at position 3 on A-ring were comparably active (<= 238 mg/dl). The structure-activity relationship of the tested chalcones was studied and the findings were supported statistically (C) 2012 Elsevier Ltd. All rights reserved.

作者

我是这篇论文的作者
点击您的名字以认领此论文并将其添加到您的个人资料中。

评论

主要评分

4.5
评分不足

次要评分

新颖性
-
重要性
-
科学严谨性
-
评价这篇论文

推荐

Article Biochemistry & Molecular Biology

Protective Effects of the Chalcone-Based Derivative AN07 on Inflammation-Associated Myotube Atrophy Induced by Lipopolysaccharide

Wei-Yu Fang, Chih-Lung Lin, Wan-Hsuan Chang, Chih-Hsiang Chang, Yun-Cian Huang, Yi-Hong Tsai, Fang-Rong Chang, Yi-Ching Lo

Summary: The study found that AN07 significantly attenuated inflammation in LPS-treated muscle cells, improved mitochondrial function, and showed protective effects against myotube atrophy.

INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES (2022)

Review Cell Biology

Long Noncoding RNAs and Circular RNAs Regulate AKT and Its Effectors to Control Cell Functions of Cancer Cells

Jen-Yang Tang, Ya-Ting Chuang, Jun-Ping Shiau, Kun-Han Yang, Fang-Rong Chang, Ming-Feng Hou, Ammad Ahmad Farooqi, Hsueh-Wei Chang

Summary: AKT serine-threonine kinase and its effectors play essential roles in maintaining various cellular functions of cancer cells, while lncRNAs and circRNAs regulate the expression of these functions through multiple pathways. This review provides comprehensive information about the relationship between lncRNAs, circRNAs, and AKT in the regulation of cancer cell functions.
Review Biochemistry & Molecular Biology

The Impact of Oxidative Stress and AKT Pathway on Cancer Cell Functions and Its Application to Natural Products

Jun-Ping Shiau, Ya-Ting Chuang, Jen-Yang Tang, Kun-Han Yang, Fang-Rong Chang, Ming-Feng Hou, Ching-Yu Yen, Hsueh-Wei Chang

Summary: Oxidative stress and AKT pathway play crucial roles in regulating various cell functions in cancer cells. Natural products have the potential to modulate oxidative stress and AKT for anticancer effects. However, the underlying mechanisms of how they regulate cell functions, particularly the contribution of AKT downstream effectors, are not well understood. This review discusses the roles of oxidative stress and AKT pathway in ten cell functions and highlights the potential of natural products in regulating these functions, with a focus on AKT effectors that have been rarely reported.

ANTIOXIDANTS (2022)

Article Biochemistry & Molecular Biology

New 3,4-seco-3,19-Dinor- and Spongian-Based Diterpenoid Lactones from the Marine Sponge Spongia sp.

Chi-Jen Tai, Chih-Hua Chao, Atallah F. Ahmed, Chia-Hung Yen, Tsong-Long Hwang, Fang-Rong Chang, Yusheng M. Huang, Jyh-Horng Sheu

Summary: Chemical investigation of the Red Sea sponge Spongia sp. resulted in the discovery of four new compounds, secodinorspongins A-D (1-4), as well as a known compound sponginolide (5). The structures of these compounds and their absolute configurations were elucidated using spectroscopic methods and a comparison of calculated and experimental CD spectra. A possible biosynthetic pathway for compounds 1-4 was proposed. The cytotoxic, antibacterial, and anti-inflammatory activities of compounds 1-5 were also evaluated, with compound 1 showing inhibitory activity against Staphylococcus aureus growth, and compounds 4 and 5 suppressing superoxide-anion generation and elastase release in human neutrophils.

INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES (2023)

Article Plant Sciences

Development on potential skin anti-aging agents of Cosmos caudatus Kunth via inhibition of collagenase, MMP-1 and MMP-3 activities

Yen Chi Loo, Hao-Chun Hu, Szu-Yin Yu, Yi-Hong Tsai, Michal Korinek, Yang-Chang Wu, Fang-Rong Chang, Ying-Jung Chen

Summary: In this study, the anti-aging potential of Cosmos caudatus Kunth (CC) extracts and fractions was investigated. It was found that these extracts and fractions inhibited collagenase, MMP-1, and MMP-3 activities in human dermal fibroblasts and contained flavonoid glycosides as the major compounds. These findings suggest that CC has the potential to be developed as anti-aging products.

PHYTOMEDICINE (2023)

Review Oncology

Modulating Effects of Cancer-Derived Exosomal miRNAs and Exosomal Processing by Natural Products

Ya-Ting Chuang, Jen-Yang Tang, Jun-Ping Shiau, Ching-Yu Yen, Fang-Rong Chang, Kun-Han Yang, Ming-Feng Hou, Ammad Ahmad Farooqi, Hsueh-Wei Chang

Summary: Cancer cells produce exosomes to regulate cell functions for tumor progression, and the modulation of exosome processing by natural products is not well understood. This review focuses on the organization of cancer-derived exosomal miRNAs and their processing and cell functions modulation by natural products. It provides a comprehensive understanding of the potential mechanisms and targets for exosome processing and cancer cell functions by natural products.

CANCERS (2023)

Article Chemistry, Medicinal

Components with Anti-Diabetic Activity Isolated from the Leaves and Twigs of Glycosmis pentaphylla Collected in Vietnam

Minh Tuyet Thi Nguyen, I-Chi Hsu, Hui-Kang Liu, Yu-Chi Lin, Shu-Rong Chen, Fang-Rong Chang, Yuan-Bin Cheng

Summary: A phytochemical investigation of Glycosmis pentaphylla collected in Vietnam resulted in the discovery of three new compounds and twenty-five known compounds. The structures of the isolates were determined through various analytical methods. In the screening for anti-diabetic activity, several compounds showed potential inhibition of DPP4 and stimulation of GLP-1 secretion.

PHARMACEUTICALS (2022)

Review Biochemistry & Molecular Biology

Modulation of AKT Pathway-Targeting miRNAs for Cancer Cell Treatment with Natural Products

Jun-Ping Shiau, Ya-Ting Chuang, Ching-Yu Yen, Fang-Rong Chang, Kun-Han Yang, Ming-Feng Hou, Jen-Yang Tang, Hsueh-Wei Chang

Summary: This review aims to elucidate the relationship between natural products, miRNAs, and the AKT pathway in cancer cell development. By identifying the connections between miRNAs and the AKT pathway, as well as miRNAs and natural products, an miRNA/AKT/natural product axis was established to facilitate a better understanding of their anticancer mechanisms.

INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES (2023)

Article Medicine, Research & Experimental

Exploration of anti-leukemic effect of soft coral-derived 13-acetoxysarcocrassolide: Induction of apoptosis via oxidative stress as a potent inhibitor of heat shock protein 90 and topoisomerase II

Hsien-Kuo Chin, Mei-Chin Lu, Kai-Cheng Hsu, Mohamed El-Shazly, Tsen-Ni Tsai, Tzu-Yung Lin, Shou-Ping Shih, Tony Eight Lin, Zhi-Hong Wen, Yu-Chen S. H. Yang, Yi-Chang Liu

Summary: 13-AC is a compound derived from coral that can induce apoptosis in human acute lymphoblastic leukemia cells. It acts as a dual inhibitor of heat shock protein 90 and topoisomerase IIa, leading to its cytotoxic effects.

KAOHSIUNG JOURNAL OF MEDICAL SCIENCES (2023)

Review Oncology

Connection of Cancer Exosomal LncRNAs, Sponging miRNAs, and Exosomal Processing and Their Potential Modulation by Natural Products

Ya-Ting Chuang, Jun-Ping Shiau, Jen-Yang Tang, Ammad Ahmad Farooqi, Fang-Rong Chang, Yi-Hong Tsai, Ching-Yu Yen, Hsueh-Wei Chang

Summary: Cancer cells release exosomes containing tumor-promoting effects, and natural products can block exosome processing and inhibit cancer progression. However, the correlation between exosomal lncRNAs and natural product treatments is not well understood. By using bioinformatics, this study fills the gap by exploring the interaction between exosomal lncRNAs, miRNAs, and exosomal processing genes, and summarizes their roles in cancer progression and the anticancer effects of natural products.

CANCERS (2023)

Article Biochemistry & Molecular Biology

High-Purity Bioactive Ingredient-3S,3′S-Astaxanthin: A New Preparation from Genetically Modified Kluyveromyces marxianus without Column Chromatography and Gel Filtration

Wei-Cheng Yuan, Tung-Ying Wu, Pei-Yi Chu, Fang-Rong Chang, Yang-Chang Wu

Summary: An efficient method for preparing bioactive ingredient 3S,3 ' S-astaxanthin (3S,3 ' S-AST) from genetically modified yeast was developed. The combination of enzyme-assisted extraction and salt-assisted liquid-liquid extraction (SALLE) resulted in a high yield of 3S,3 ' S-AST with over 99% purity. The antioxidant capacity of the purified 3S,3 ' S-AST products was found to be 18.3 times higher than that of the original raw material extract. This new method has the potential to replace previous methods and can be scaled up for the production of high-purity 3S,3 ' S-AST with lower cost and simpler equipment in the food and/or drug industries.

ANTIOXIDANTS (2023)

Article Environmental Sciences

Sex-specific interactive effect of melamine and DEHP on a marker of early kidney damage in Taiwanese adults: A national population-based study from the Taiwan Biobank

Sih-Syuan Li, Jia-Jen Chen, Ming-Wei Su, Chien-Wei Lin, Chu-Chih Chen, Yin-Han Wang, Chia-Chu Liu, Yi-Chun Tsai, Tusty-Jiuan Hsieh, Ming-Tsang Wu, Chia-Fang Wu

Summary: Taiwan has a high incidence of chronic kidney disease (CKD), and this study examined the associations between daily exposure to phthalates and melamine, two common nephrotoxins, and the risk of kidney damage. The study used data from the Taiwan Biobank and found a significant positive association between the daily intake levels of melamine and phthalates and the urine microalbumin to creatinine ratio (ACR). This association was particularly prominent in men.

ECOTOXICOLOGY AND ENVIRONMENTAL SAFETY (2023)

Article Environmental Sciences

Environmental melamine exposure and adverse kidney outcomes in patients with type 2 diabetes mellitus

Yi-Chun Tsai, Chia-Fang Wu, Wei-Wen Hung, Ping-Shaou Yu, Chia-Chu Liu, Tusty-Jiuan Hsieh, Chu-Chih Chen, Sih-Syuan Li, Jia-Jen Chen, Yi-Wen Chiu, Shang-Jyh Hwang, Ming-Tsang Wu

Summary: This prospective cohort study investigated the impact of melamine exposure on kidney outcomes in type 2 diabetes mellitus (T2D) patients. The findings showed a significant association between melamine exposure and adverse kidney outcomes in T2D patients, especially in those with male, well sugar control or good baseline kidney function.

ENVIRONMENTAL POLLUTION (2023)

Review Biochemistry & Molecular Biology

Connection between Radiation-Regulating Functions of Natural Products and miRNAs Targeting Radiomodulation and Exosome Biogenesis

Jen-Yang Tang, Ya-Ting Chuang, Jun-Ping Shiau, Ching-Yu Yen, Fang-Rong Chang, Yi-Hong Tsai, Ammad Ahmad Farooqi, Hsueh-Wei Chang

Summary: This review focuses on the regulating effects of natural products on miRNAs to assess the potential impacts of radiomodulation and exosome biogenesis for both the radiosensitization of cancer cells and the radioprotection of non-cancer cells.

INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES (2023)

Review Chemistry, Medicinal

Polysaccharides (pectin, mucilage, and fructan inulin) and their fermented products: A critical analysis of their biochemical, gut interactions, and biological functions as antidiabetic agents

Heba A. S. El-Nashar, Mohamed Taleb, Mohamed EL-Shazly, Chao Zhao, Mohamed A. Farag

Summary: This review comprehensively discusses the antidiabetic effects and mechanisms of action of major soluble dietary fibers (SDF), which can aid in the development of novel natural antidiabetic drugs from SDF.

PHYTOTHERAPY RESEARCH (2023)

Article Chemistry, Medicinal

Design and synthesis of a library of C2-substituted sulfamidoadenosines to probe bacterial permeability

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

Design of MERS-CoV entry inhibitory short peptides based on helix-stabilizing strategies

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

Development of novel β2-adrenergic receptor agonists for the stimulation of glucose uptake - The importance of chirality and ring size of cyclic amines

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

Conformationally constrained potent inhibitors for enhancer of zeste homolog 2 (EZH2)

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

The potential of Rhein's aromatic amines for Parkinson's disease prevention and treatment: α-Synuclein aggregation inhibition and disaggregation of preformed fibers

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

Design, synthesis and biological evaluation of novel cationic liposomes loaded with melphalan for the treatment of cancer

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)