Antidiabetic Potential of Flavonoids from Traditional Chinese Medicine: A Review

Bai, Lan; Li, Xiaofang; He, Li; Zheng, Yu; Lu, Haiying; Li, Jinqi; Zhong, Lei; Tong, Rongsheng; Jiang, Zhongliang; Shi, Jianyou; Li, Jian

doi:10.1142/s0192415x19500496

Cited by 154 publications

(98 citation statements)

References 96 publications

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“…Among the top hits, one of the most promising drugs is Hesperidin, a citrus bioflavonoid, which possesses antioxidant, anti-inflammatory, antiviral, and anticarcinogenic properties [33,66]. It was used as the pharmaceutical raw material in the pharmaceutical industry and is one of the main components of a Chinese medicine, beniol [67]. Importantly, Hesperidin had demonstrated antiviral properties in in vitro models against influenza A virus (H1N1) by stimulating cellautonomous immunity through interferon gene expression [68].…”

Section: Discussionmentioning

confidence: 99%

Repurposing Therapeutics to Identify Novel Inhibitors Targeting 2'-O-Ribose Methyltransferase Nsp16 of SARS-CoV-2

Jiang¹,

Liu²,

Manning³

et al. 2020

Preprint

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Three coronaviruses (CoVs): severe acute respiratory syndrome coronavirus (SARS-CoV-1), Middle East respiratory syndrome coronavirus (MERS-CoV), and the recently identified SARS-CoV-2 in December 2019, have caused deadly pneumonia in humans since the beginning of the 21st century. The SARS-CoV-2 causes coronavirus disease-19 (COVID-19) with influenza-like symptoms ranging from mild discomfort to severe lung injury and multi-organ failure, eventually leading to death. As of April 30, 2020, more than three million (3,175,207) COVID-19 cases were reported worldwide, and more than 220,000 (224,172) patients have died (https://www.who.int/emergencies/diseases/novel-coronavirus-2019). Effective treatments and vaccines for SARS-CoV-2 infection do not currently exist. Thus, it will be of great benefit to identify and repurpose already well-characterized compounds and approved drugs for use in combating COVID-19. CoVs are positive-sense RNA viruses that replicate in the cytoplasm of infected cells. Replication and transcription of the CoV RNA genome are achieved by a complex RNA replication/transcription machinery, consisting of at least 16 viral nonstructural proteins (nsp). Previous studies demonstrated that nsp16 proteins of SARS-CoV-1 and MERS-CoV have methyltransferase (MTase) activities that catalyze methylation of the first transcribed nucleotide at the ribose 2’-O position (2’-O-Me). The 2’-O-Me of virus cap RNAs protects itself from degradation by 5′-3′ exoribonucleases, ensures efficient translation, and helps to prevent recognition by the host innate immune system. The importance of nsp16 2'-O-MTase activity for CoV infection and pathogenesis was previously documented by in vitro and in vivo studies. For SARS-CoV-1, the absence of nsp16 2′-O-MTase activity results in significant attenuation characterized by decreased viral replication, reduced weight loss, and limited breathing dysfunction in mice. In addition, nsp16 down-regulates the activities of innate immune sensing factors: retinoic acid-inducible gene I (RIG-I) and melanoma differentiation-associated gene 5 protein (MDA5). Thus, inhibition of nsp16 2’-O-MTase activities should restrain viral replication and enable recognition by the host innate immune system, making the nsp16-MTase a promising target for the identification of new anti-SARS-CoV-2 drugs. In the present study, we employed structural analysis, virtual screening, and systematic drug repurposing approaches to identify “approved” drugs which can act as promising inhibitors against nsp16 2′-O-MTase of SARS-CoV-2. We first performed comparative analysis of primary amino acid sequences and crystal structures of seven human CoVs and defined the key residues for nsp16 2-O’-MTase functions. From the virtual screening against nsp16 2′-O-MTase of SARS-CoV-2, we provide a ranking of the predicted binding affinities of 1,380 top hit compounds corresponding to 967 “approved” drugs. Furthermore, we have calculated various structural parameters of our top-ranking drugs. Our studies provided the foundation to further test and repurpose these candidate drugs experimentally and clinically for COVID-19 treatment.

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Section: Discussionmentioning

confidence: 99%

Repurposing Therapeutics to Identify Novel Inhibitors Targeting 2'-O-Ribose Methyltransferase Nsp16 of SARS-CoV-2

Jiang¹,

Liu²,

Manning³

et al. 2020

Preprint

View full text Add to dashboard Cite

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“…It has a variety of biological functions and is widely used in various clinical fields. The ingredient can relieve coronary heart disease angina pectoris, provide adjuvant treatment for myocardial [1,2] and cerebral infarction, and promote the recovery of neurological functions [3][4][5]. However, Pur is a BCS IV drug with low oral bioavailability [6].…”

Section: Introductionmentioning

confidence: 99%

“…The ionic gelation method consists of the spontaneous reaction of cationic CS with an anionic crosslinking agent, usually TPP, forming a polyelectrolyte complex named TPP/CS. This complex is stabilized by the cross-linked electrostatic interaction between CS-NH 3 + and TPP-O-groups, resulting in a three-dimensional entanglement that precipitates from an aqueous solution in the form of gel-like nanoparticles, also named microgels, where encapsulation then occurs, causing Pur to form nanoparticles [19,20]. This method is simple to operate, and it is easily adaptable to industrialized production.…”

Section: Introductionmentioning

confidence: 99%

Preparation of Puerarin Chitosan Oral Nanoparticles by Ionic Gelation Method and Its Related Kinetics

et al. 2020

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In this paper, as an active ingredient, puerarin chitosan nanoparticles (Pur-CS/TPP-NPs) are prepared by an ionic gelation method. The chitosan (CS) concentration, pH of the CS solution, sodium tripolyphosphate (TPP) concentration, stirring speed, stirring time, ultrasonic power, and dosage are used as single factors for investigation, and the encapsulation efficiency, drug loading capacity, particle size, and polydispersity index (PDI) are used as indicators for investigation. The optimal prescription is determined using the Box–Behnken effect surface design method. The characterization of the best formulation, which is determined via an in vitro release assay and liquid chromatography/tandem mass spectrometry (LC-MS/MS) analysis methods, is used here for pharmacokinetic studies. An in situ single-pass intestinal perfusion model is used to investigate drug absorption in the intestine. After characterization, the morphologies of the nanoparticles are intact. It can be seen from the in vitro release experiments that the equation fitted by the nanoparticles is the Higuchi model, the nanoparticle release process is very stable and without sudden release, indicating that the nanoparticles are well-released in vitro. The pharmacokinetic results and the in situ single-pass intestinal perfusion model study show that the bioavailability and absorption of Pur-CS/TPP-NPs were significantly higher than Pur. Thus, all the results show that the prepared nanoparticles can significantly improve the bioavailability of Pur, and we hope to lay the foundation for the development of new products of Pur.

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“…is was possible due to the compound 1 ability to neutralize free radicals that inhibit the formation of β-cells in the pancreas. Flavonoid compounds in the case of e Scientific World Journal diabetes were used for maintaining the function of β-cell pancreatic and increasing the reformation of β-cells in the pancreas [59].…”

Section: Anti-type 2 Diabetes Mellitus Activitymentioning

confidence: 99%

Macrophylloflavone: A New Biflavonoid fromGarcinia macrophyllaMart. (Clusiaceae) for Antibacterial, Antioxidant, and Anti-Type 2 Diabetes Mellitus Activities

Cane

Saidi

Yahya

et al. 2020

The Scientific World Journal

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Investigations of antibacterial, antioxidant, and anti-type 2 diabetes mellitus activities have been carried out on Garcinia macrophylla Mart. plant extract fractions. An isolate from a fraction of ethyl acetate extract was characterized with spectroscopic data. A new biflavonoid compound was found to have a skeleton of 5,7,4′,5″,7″,3‴,4‴-heptahydroxyflavanone[3-6″] flavones which was named macrophylloflavone (1). The compound was evaluated for its antibacterial activity against Escherichia coli ATCC 25922 and Staphylococcus aureus ATCC 25923 with cephazolin as a positive control, antioxidant assay against 2,2 diphenyl-1-picrylhydrazyl (DPPH) with ascorbic acid as the positive control, and anti-type 2 diabetes mellitus treatment with metformin as a positive control. The biflavonoid compound exhibited a good inhibition for bacteria and free radical DPPH. Furthermore, biflavonoid compound treatment on the diabetic rats suggested its ability to decrease the blood glucose level. This study provided evidence that the plant has antibacterial, antioxidant, and antidiabetic properties.

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Antidiabetic Potential of Flavonoids from Traditional Chinese Medicine: A Review

Cited by 154 publications

References 96 publications

Repurposing Therapeutics to Identify Novel Inhibitors Targeting 2'-O-Ribose Methyltransferase Nsp16 of SARS-CoV-2

Repurposing Therapeutics to Identify Novel Inhibitors Targeting 2'-O-Ribose Methyltransferase Nsp16 of SARS-CoV-2

Preparation of Puerarin Chitosan Oral Nanoparticles by Ionic Gelation Method and Its Related Kinetics

Macrophylloflavone: A New Biflavonoid fromGarcinia macrophyllaMart. (Clusiaceae) for Antibacterial, Antioxidant, and Anti-Type 2 Diabetes Mellitus Activities

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