Simplified process of candidate certified reference material development for the analysis of Andrographis paniculata derived therapeutics

Gaur, Iti; Gaur, Pooja; Gautam, Parul; Tiwari, Neha; Khare, Puja; Tripathi, Sarita; Shanker, Karuna

doi:10.1016/j.microc.2021.106140

Cited by 6 publications

(3 citation statements)

References 15 publications

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“…The active pocket amino acid residues reported in IETH mainly include Phe78, Ile79, Asp80, Trp86, Tyr115, His152, Ser153, Phe216, Arg257, His264, and Leu265. 7,36 As shown in Table 4, all the identified potential active compounds could smoothly enter the active pocket of pancreatic lipase with low binding energy and form hydrogen bonds with active amino acid residues. In particular, compounds 5 and 6 had the lowest binding energy with IETH, indicating their strong binding ability with pancreatic lipase and great potential to be regarded as pancreatic lipase inhibitors.…”

Section: Molecular Docking Analysismentioning

confidence: 99%

Efficient screening of pancreatic lipase inhibitors from Rheum palmatum by affinity ultrafiltration–high‐performance liquid chromatography combined with high‐resolution inhibition profiling

Quan,

Wen,

et al. 2023

Phytochemical Analysis

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IntroductionPancreatic lipase is one of the most important key targets in the treatment of obesity. Inhibition of pancreatic lipase can effectively reduce lipid absorption and treat obesity and other related metabolic disorders.ObjectivesThe goal of this study is the efficient screening of pancreatic lipase inhibitors in the root and rhizome of Rheum palmatum using affinity ultrafiltration–high‐performance liquid chromatography (AUF‐HPLC) combined with high‐resolution inhibition profiling (HRIP).MethodsPotential pancreatic lipase ligands and pancreatic lipase inhibitors in ethyl acetate fraction of R. palmatum were screened using AUF‐HPLC and HRIP, respectively. All screened compounds were identified by HPLC– quadrupole time‐of‐flight (Q‐TOF)/MS. Eight compounds were screened out by both AUF‐HPLC and HRIP, and six compounds were screened out by either AUF‐HPLC or HRIP alone. The pancreatic lipase inhibitory activities of all screened compounds were verified by enzyme inhibition assay and molecular docking.ResultsFive new potent pancreatic lipase inhibitors were discovered, namely procyanidin B5 3,3′‐di‐O‐gallate (IC50 = 0.06 ± 0.01 μM), 1,6‐di‐O‐galloyl‐2‐O‐cinnamoyl‐β‐D‐glucoside (IC50 = 12.83 ± 0.67 μM), 1‐O‐(1,3,5‐trihydroxy)phenyl‐2‐O‐galloyl‐6‐O‐cinnamoyl‐β‐D‐glucoside (IC50 = 17.84 ± 1.33 μM), 1,2‐di‐O‐galloyl‐6‐O‐cinnamoyl‐β‐D‐glucoside (IC50 = 18.39 ± 1.52 μM), and 4‐(4′‐hydroxyphenyl)‐2‐butanone‐4’‐O‐β‐D‐(2”‐O‐galloyl‐6”‐O‐cinnamoyl)‐glucoside (IC50 = 2.91 ± 0.40 μM). It was found that procyanidin B5 3,3′‐di‐O‐gallate showed higher pancreatic lipase inhibitory activity than the positive control orlistat (IC50 = 0.12 ± 0.02 μM).ConclusionThe combination of affinity ultrafiltration–high‐performance liquid chromatography (AUF‐HPLC) and high‐resolution inhibition profiling (HRIP) could reduce the risk of false‐negative screening and missed screening and could achieve more efficient screening of bioactive compounds in complex natural products.

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Section: Molecular Docking Analysismentioning

confidence: 99%

Efficient screening of pancreatic lipase inhibitors from Rheum palmatum by affinity ultrafiltration–high‐performance liquid chromatography combined with high‐resolution inhibition profiling

Quan,

Wen,

et al. 2023

Phytochemical Analysis

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“…Andrographolide is a significant compound because of its pharmacological properties (Kumar et al 2021). The dry leaves of plants are used as a traditional medicine and reported its therapeutic potential for mild to moderate COVID-19 (Gaur et al 2021(Gaur et al , 2023.…”

Section: Introductionmentioning

confidence: 99%

Effect of biochar on soil microbial community, dissipation and uptake of chlorpyrifos and atrazine

Singh,

Yadav,

Pandey

et al. 2024

Biochar

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For the application of biochar in restoring pesticide-contaminated soils and minimizing the risk associated with their uptake in plants, it is crucial to understand the biochar impact on soil biological activities and dissipation and accumulation of pesticides in plant and soil systems. In this study, the effect of Mentha-distilled waste-derived biochar was investigated on chlorpyrifos and atrazine contaminated sandy loam soil. The four application rates of atrazine (2, 4, 6, and 8 mg kg−1) and chlorpyrifos (2, 4, 6, and 12 mg kg−1) and a single application rate of biochar (4%) were used in this study. The degradation of pesticides, the diversity of the bacterial community, and enzymatic activities (alkaline phosphatase, dehydrogenase, arylsulfatase, phenol oxidase, urease activity and N-acetyl glucosaminidase) were examined in soil. The uptake of two pesticides and their effect on growth and stress parameters were also investigated in plants (A. paniculata). The dissipation of chlorpyrifos and atrazine followed simple first-order kinetics with a half-life of 6.6–74.6 and 21–145 days, respectively. The presence of deisopropyl atrazine desethyl atrazine (metabolites of atrazine) and 3,5,6-trichloro-2-pyridinol (a metabolite of chlorpyrifos) was observed in soil and plant tissues. Biochar application significantly (p = 0.001) enhanced the degradation rate of chlorpyrifos and atrazine leading to the lower half-life of chlorpyrifos and atrazine in soil. A significant reduction (p = 0.001) in the uptake of chlorpyrifos and atrazine and alteration in their binding affinity and uptake rate in plant tissues was observed in biochar treatments. The incorporation of biochar improved chlorpyrifos/atrazine degrader and plant growth-promoting bacterial genera such as Balneimonas, Kaistobacter, Rubrobacter, Ammoniphilus, and Bacillus. The upregulation of functional genes associated with nucleotide, energy, carbohydrate, amino acid metabolism, xenobiotic biodegradation, and metabolism: atrazine degradation was observed in biochar treatments. The biochar amendments significantly (p = 0.001) reduced the plant’s uptake velocity (Vmax) and affinity (Km) of chlorpyrifos and atrazine. These results delineated that Mentha-distilled waste-derived biochar can potentially remediate chlorpyrifos and atrazine contaminated soils and ensure the safety of plants for consumption. Graphical Abstract

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“…21 Additionally, pancreatic lipase plays an important role in diseases related to lipid metabolism, especially obesity. 22 Protein tyrosine phosphatase 1B (PTP1B) negatively regulates cell signalling transmitted from leptin and insulin receptors and has been developed as a new target to cure obesity and type 2 diabetes mellitus (T2DM). 23 In addition, 3-hydroxy-3-methylglutaryl-coenzyme A reductase (HMGCR) is a crucial target enzyme for cholesterol synthesis and has been developed as a target for the treatment of hyperlipidemia.…”

Section: Introductionmentioning

confidence: 99%

Screening and identification of potential hypoglycemic and hypolipidemic compounds from aqueous extract of Scutellaria baicalensis Georgi root combing affinity ultrafiltration with multiple drug targets and in silico analysis

Xu,

Li,

Chen

et al. 2023

Phytochemical Analysis

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IntroductionScutellaria baicalensis Georgi, a traditional Chinese medicine, is widely applied to treat various diseases among people, especially in East Asia. However, the specific active compounds in S. baicalensis aqueous extracts (SBAEs) responsible for the hypoglycemic and hypolipidemic properties as well as their potential mechanisms of action remain unclear.ObjectivesThis work aimed to explore the potential hypoglycemic and hypolipidemic compounds from SBAE and their potential mechanisms of action.MethodologyThe in vitro inhibitory tests against lipase and α‐glucosidase, and the effects of SBAE on glucose consumption and total triglyceride content in HepG2 cells were first performed to evaluate the hypoglycemic and hypolipidemic effects. Then, affinity ultrafiltration liquid chromatography–mass spectrometry (LC–MS) screening strategy with five drug targets, including α‐glucosidase, α‐amylase, protein tyrosine phosphatase 1B (PTP1B), lipase and 3‐hydroxy‐3‐methylglutaryl‐coenzyme A reductase (HMGCR) was developed to screen out the potential active constituents from SBAE, and some representative active compounds were further validated.ResultsSBAE displayed noteworthy hypoglycemic and hypolipidemic properties, and 4, 10, 4, 8, and 8 potential bioactive components against α‐amylase, α‐glucosidase, PTP1B, HMGCR, and lipase were initially screened out, respectively. The interaction network was thus constructed between the potential bioactive compounds screened out and their corresponding drug targets. Among them, baicalein, wogonin, and wogonoside were revealed to possess remarkable hypoglycemic and hypolipidemic effects.ConclusionThe potential hypolipidemic and hypoglycemic bioactive compounds in SBAE and their mode of action were initially explored through ligand–target interactions by combining affinity ultrafiltration LC–MS strategy with five drug targets.

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Simplified process of candidate certified reference material development for the analysis of Andrographis paniculata derived therapeutics

Cited by 6 publications

References 15 publications

Efficient screening of pancreatic lipase inhibitors from Rheum palmatum by affinity ultrafiltration–high‐performance liquid chromatography combined with high‐resolution inhibition profiling

Efficient screening of pancreatic lipase inhibitors from Rheum palmatum by affinity ultrafiltration–high‐performance liquid chromatography combined with high‐resolution inhibition profiling

Effect of biochar on soil microbial community, dissipation and uptake of chlorpyrifos and atrazine

Screening and identification of potential hypoglycemic and hypolipidemic compounds from aqueous extract of Scutellaria baicalensis Georgi root combing affinity ultrafiltration with multiple drug targets and in silico analysis

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