Phytochemical profiling of Blumea laciniata (Roxb.) DC. and its phytopharmaceutical potential against diabetic, obesity, and Alzheimer’s

Swaraz, A.M.; Sultana, Fariha; Bari, Md. Wasim; Ahmed, Khondoker Shahin; Hasan, Mehedi; Islam, Md. Monirul; Islam, Mohammad Amirul; Satter, Mohammed A.; Hossain, Hemayet; Islam, Md. Shofiqul; Khan, Iqbal; Raihan, Md. Obayed

doi:10.1016/j.biopha.2021.111859

Cited by 19 publications

(16 citation statements)

References 71 publications

Supporting

Mentioning

Contrasting

Order By: Relevance

“…The objective of pharmacophore modeling is to find chemical features responsible for a specific biological activity among potent ligands [ 258 ]. Therefore, the use of appropriate modeling for screening drugs for T2DM is important in evaluating the interaction between the receptor and ligand, defined as essential geometric arrangement of atoms or functional groups necessary to produce a given biological response [ 259 ]. For instance, Teresa et al (2015) used Ligandscout [ 260 ], which is a ligand-based pharmacophore modeling package to identify one of the most important structural properties that can prevent the increase of blood glucose levels.…”

Section: In Silico Approachesmentioning

confidence: 99%

In Silico Approaches to Identify Polyphenol Compounds as α-Glucosidase and α-Amylase Inhibitors against Type-II Diabetes

Riyaphan¹,

Pham

Leong

et al. 2021

Biomolecules

View full text Add to dashboard Cite

Type-II diabetes mellitus (T2DM) results from a combination of genetic and lifestyle factors, and the prevalence of T2DM is increasing worldwide. Clinically, both α-glucosidase and α-amylase enzymes inhibitors can suppress peaks of postprandial glucose with surplus adverse effects, leading to efforts devoted to urgently seeking new anti-diabetes drugs from natural sources for delayed starch digestion. This review attempts to explore 10 families e.g., Bignoniaceae, Ericaceae, Dryopteridaceae, Campanulaceae, Geraniaceae, Euphorbiaceae, Rubiaceae, Acanthaceae, Rutaceae, and Moraceae as medicinal plants, and folk and herb medicines for lowering blood glucose level, or alternative anti-diabetic natural products. Many natural products have been studied in silico, in vitro, and in vivo assays to restrain hyperglycemia. In addition, natural products, and particularly polyphenols, possess diverse structures for exploring them as inhibitors of α-glucosidase and α-amylase. Interestingly, an in silico discovery approach using natural compounds via virtual screening could directly target α-glucosidase and α-amylase enzymes through Monte Carto molecular modeling. Autodock, MOE-Dock, Biovia Discovery Studio, PyMOL, and Accelrys have been used to discover new candidates as inhibitors or activators. While docking score, binding energy (Kcal/mol), the number of hydrogen bonds, or interactions with critical amino acid residues have been taken into concerning the reliability of software for validation of enzymatic analysis, in vitro cell assay and in vivo animal tests are required to obtain leads, hits, and candidates in drug discovery and development.

show abstract

Section: In Silico Approachesmentioning

confidence: 99%

In Silico Approaches to Identify Polyphenol Compounds as α-Glucosidase and α-Amylase Inhibitors against Type-II Diabetes

Riyaphan¹,

Pham

Leong

et al. 2021

Biomolecules

View full text Add to dashboard Cite

show abstract

“…NMR spectra (see Supporting Information) were acquired on a Bruker Ultra Shield 500 instrument, running at 500 MHz for 1 H and 125 MHz for 13 C, respectively. Mass spectra (MS) were recorded on a Shimadzu LC/MS/MS 8040 mass spectrometer with ESI ionization.…”

Section: Methodsmentioning

confidence: 99%

“…Cinnamic acids (intermediate 2), a key building block for the formation of other more complex phenolic compounds, is generally used as a common food additive. [13] Initially, intermediate 2 was obtained from various benzaldehyde and propanedioic acids through Knoevenagel condensation with high yields (70-95 %) after purification by recrystallization from ethanol. Then, intermediate 3 was acquired through the reaction between intermediate 2 and excess oxalyl chloride.…”

Section: Synthesismentioning

confidence: 99%

See 1 more Smart Citation

Design, Synthesis, and Anticancer Activity of Cinnamoylated Barbituric Acid Derivatives

Liu

et al. 2022

Chemistry & Biodiversity

View full text Add to dashboard Cite

This work deals with the design and synthesis of 18 barbituric acid derivatives bearing 1,3‐dimethylbarbituric acid and cinnamic acid scaffolds to find potent anticancer agents. The target molecules were obtained through Knoevenagel condensation and acylation reaction. The cytotoxicity was assessed by the MTT assay. Flowcytometry was performed to determine the cell cycle arrest, apoptosis, ROS levels and the loss of MMP. The ratios of GSH/GSSG and the MDA levels were determined by using UV spectrophotometry. The results revealed that introducing substitutions (CF3, OCF3, F) on the meta‐ of the benzyl ring of barbituric acid derivatives led to a considerable increase in the antiproliferative activities compared with that of corresponding ortho‐ and para‐substituted barbituric acid derivatives. Mechanism investigation implied that the 1c could increase the ROS and MDA level, decrease the ratio of GSH/GSSG and MMP, and lead to cell cycle arrest. Further research is needed for structural optimization to enhance hydrophilicity, thereby improve the biological activity of these compounds.

show abstract

“…Thus, this plant is a potential herbal medicinal resource against various multifactorial diseases including obesity, Alzheimer's, and hypermelanoma, as detected phenolics have established biological roles against these diseases, as mentioned in the supplementary table of the earlier report. [45]…”

Section: B Lacera Phenolics Profilementioning

confidence: 99%

Polyphenols Profile and Enzyme Inhibitory Properties of Blumea lacera (Burm. f.) DC.: A Potential Candidate against Obesity, Aging, and Skin Disorder

Swaraz¹,

Sultana²,

Ahmed

et al. 2022

Chemistry & Biodiversity

Self Cite

View full text Add to dashboard Cite

Blumea lacera (Burm. f.) DC. is attracting scientific interest due to the diverse biological activities of its various parts and its use in folk medicine. The present study was undertaken to investigate the tissue-specific differential expression pattern of its total bioactive compounds. The study was further extended to whole plant phenolics profiling, in vitro enzyme inhibition activities, followed by in silico enzyme inhibition analysis to assess its potential as herbal medicine. The amount of total phenolics in different tissues was followed in decreasing order as old leaf, flower bud, root, young leaf, flower, old stem, and young stem, while that for the flavonoids was old leaf, root, young leaf, flower bud, flower, young stem, and old stem. This study identified rosmarinic acid, quercetin, and kaempferol in this plant for the first time. The solvent extracts demonstrated strong inhibition of lipase and tyrosinase activity, along with varying degrees of inhibition of acetylcholinesterase and butyrylcholinesterase activity. Among the detected compounds, ten displayed strong in silico binding affinities with the tested enzymes. The findings provide a new insight into further investigation of the medicinal potential of this species against obesity, neurological disorders, and aberrant skin color.

show abstract

Phytochemical profiling of Blumea laciniata (Roxb.) DC. and its phytopharmaceutical potential against diabetic, obesity, and Alzheimer’s

Cited by 19 publications

References 71 publications

In Silico Approaches to Identify Polyphenol Compounds as α-Glucosidase and α-Amylase Inhibitors against Type-II Diabetes

In Silico Approaches to Identify Polyphenol Compounds as α-Glucosidase and α-Amylase Inhibitors against Type-II Diabetes

Design, Synthesis, and Anticancer Activity of Cinnamoylated Barbituric Acid Derivatives

Polyphenols Profile and Enzyme Inhibitory Properties of Blumea lacera (Burm. f.) DC.: A Potential Candidate against Obesity, Aging, and Skin Disorder

Contact Info

Product

Resources

About