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1.
Environ Dev Sustain ; : 1-30, 2022 Nov 03.
Artigo em Inglês | MEDLINE | ID: mdl-36345298

RESUMO

COVID-19 has had an impact on the entire humankind and has been proved to spread in deadly waves. As a result, preparedness and planning are required to better deal with the epidemic's upcoming waves. Effective planning, on the other hand, necessitates detailed vulnerability assessments at all levels, from the national to the state or regional. There are several issues at the regional level, and each region has its own features. As a result, each region needs its own COVID-19 vulnerability assessment. In terms of climate, terrain and demographics, the state of Uttarakhand differs significantly from the rest of India. As a result, a vulnerability assessment of the next COVID-19 variation (Omicron BA.2) is required for district-level planning to meet regional concerns. A total of 17 variables were chosen for this study, including demographic, socio-economic, infrastructure, epidemiological and tourism-related factors. AHP was used to compute their weights. After applying min-max normalisation to the data, a district-level quantitative SWOT is created to compare the performance of 13 Uttarakhand districts. A COVID-19 vulnerability index (normalised R i ) ranging between 0 and 1 was produced, and district-level vulnerabilities were mapped. Quantitative SWOT results depict that Dehradun is a best performing district followed by Haridwar, while Bageshwar, Rudra Prayag, Champawat and Pithoragarh are on the weaker side and the normalised Ri proves Dehradun, Nainital, Champawat, Bageshwar and Chamoli to be least vulnerable to COVID-19 (normalised R i ≤ 0.25) and Pithoragarh to be the most vulnerable district (normalised R i > 0.90). Pauri Garwal and Uttarkashi are moderately vulnerable (normalised R i 0.50 to 0.75).

2.
Environ Sci Pollut Res Int ; 29(21): 31511-31540, 2022 May.
Artigo em Inglês | MEDLINE | ID: mdl-35001277

RESUMO

Disposal of waste without treatment is the least preferable way of sustainable solid waste management (SWM). But most cities in developing nations still use open dumps, causing negative impacts on the environment and human health. This study offered a novel approach for selecting landfill sites and sustainable SWM in Aligarh city, India. This was done through data collection, selecting models for criterion weighting, and validation. In order to prepare a landfill site suitability map, a geographic information system (GIS)-based ensemble fuzzy analytic hierarchy process-support vector machine (FAHP-SVM) and fuzzy analytic hierarchy process-random forest (FAHP-RF) models were implemented. Considering the previous studies and the study area characteristics, eighteen thematic layers were selected. The result revealed that land value; distance from residential roads, hospitals and clinics, and waste bins; and normalized difference built-up index (NDBI) have a fuzzy weight greater than 0.10, indicating significant factors. In contrast, land elevation, land slope, surface temperature, soil moisture index, normalized difference vegetation index (NDVI), and urban classification have a zero fuzzy weight, indicating these criteria have no importance. The result further revealed that FAHP-RF with an area under curve (AUC) value of 0.91 is the more accurate model than FAHP-SVM. According to the final weight-based overlay result, seven potential landfill sites were identified, out of which three were determined as most suitable by considering current land cover, public opinions, and environmental and economic concerns. This research proposed a zonal division model based on landfill sites location for sustainable SWM in Aligarh city. However, the findings may provide a guideline to the decision-makers and planners for optimal landfill site selection in other cities of developing countries.


Assuntos
Sistemas de Informação Geográfica , Eliminação de Resíduos , Algoritmos , Processo de Hierarquia Analítica , Humanos , Aprendizado de Máquina , Resíduos Sólidos , Instalações de Eliminação de Resíduos
3.
Nat Prod Res ; 36(21): 5530-5538, 2022 Nov.
Artigo em Inglês | MEDLINE | ID: mdl-34963398

RESUMO

Oryza sativa L. (Family Poaceae) is cultivated in tropical regions as a staple food all over the world. The rice grain husk is considered as a tonic and administered orally to relieve dysentery. The air-dried seeds husks of O. sativa were exhaustively extracted with methanol in a Soxhlet apparatus. The concentrated methanol extract was adsorbed on silica gel and chromatographed on a silica gel column. The column was eluted with petroleum ether, chloroform and methanol successively to isolate four phytoconstituents characterised as 7-ketostigmasterol (1), 3ß-benzyloxy-stigmast-7-one-22-en-19-oic acid 29-ethyleneglycol ether (2), sesquaurs-11-en- 2ß, 3ß,5α-triol (3) and 2'-(1''ß-hydroxypropyl)-7,4'-dimethoxyapigenin (4). These phytoconstituents were identified on the basis of spectral data analysis.


Assuntos
Oryza , Metanol , Sílica Gel , Sementes , Poaceae
4.
Front Pharmacol ; 12: 628970, 2021.
Artigo em Inglês | MEDLINE | ID: mdl-33776772

RESUMO

Malaria remains one of the major health concerns due to the resistance of Plasmodium species toward the existing drugs warranting an urgent need for new antimalarials. Thymol derivatives were known to exhibit enhanced antimicrobial activities; however, no reports were found against Plasmodium spp. In the present study, the antiplasmodial activity of thymol derivatives was evaluated against chloroquine-sensitive (NF-54) and -resistant (K1) strains of Plasmodium falciparum. Among the thymol derivatives tested, 4-chlorothymol showed potential activity against sensitive and resistant strains of P. falciparum. 4-Chlorothymol was found to increase the reactive oxygen species and reactive nitrogen species level. Furthermore, 4-chlorothymol could perturb the redox balance by modulating the enzyme activity of GST and GR. 4-Chlorothymol also showed synergy with chloroquine against chloroquine-resistant P. falciparum. 4-Chlorothymol was found to significantly suppress the parasitemia and increase the mean survival time in in vivo assays. Interestingly, in in vivo assay, 4-chlorothymol in combination with chloroquine showed higher chemosuppression as well as enhanced mean survival time at a much lower concentration as compared to individual doses of chloroquine and 4-chlorothymol. These observations clearly indicate the potential use of 4-chlorothymol as an antimalarial agent, which may also be effective in combination with the existing antiplasmodial drugs against chloroquine-resistant P. falciparum infection. In vitro cytotoxicity/hemolytic assay evidently suggests that 4-chlorothymol is safe for further exploration of its therapeutic properties.

5.
Nat Prod Res ; 35(14): 2429-2432, 2021 Jul.
Artigo em Inglês | MEDLINE | ID: mdl-31578883

RESUMO

Chemical investigations on the stem of Cuscuta reflexa Roxb. (Convolvulaceae) led to the isolation of one new compound characterised as 3',4'-dimethoxy-1-phenyl-1α, 2-ethanediol (1), along with eight known compounds as tridecanyl palmitate, palmitic acid, n-pentatriacontane, n-triacont-21, 27-dien-1-ol, kaempherol, chlorogenic acid, 5,7-dimethoxyapigenin and quercitin. The chemical structures were established with the help of physical, chemical and spectroscopic methods. The antimicrobial potential of the new compound (1) was evaluated against three bacterial and three fungal pathogenic strain and showed significant activities.


Assuntos
Cuscuta/química , Compostos Fitoquímicos/farmacologia , Caules de Planta/química , Antibacterianos/farmacologia , Antifúngicos/farmacologia , Espectroscopia de Ressonância Magnética Nuclear de Carbono-13 , Testes de Sensibilidade Microbiana , Compostos Fitoquímicos/química , Extratos Vegetais/química , Extratos Vegetais/farmacologia , Espectroscopia de Prótons por Ressonância Magnética
6.
Environ Sci Pollut Res Int ; 28(6): 7528-7550, 2021 Feb.
Artigo em Inglês | MEDLINE | ID: mdl-33034852

RESUMO

Sanitary landfill is still considered as one of the most significant and least expensive methods of waste disposal. It is essential to consider environmental impacts while selecting a suitable landfill site. Thus, the site selection for sanitary landfill is a complex and time-consuming task needing an assessment of multiple criteria. In the present study, a decision support system (DSS) was prepared for selecting a landfill site in a growing urban region. This study involved two steps of analysis. The first step of analysis involved the application of spatial data to prepare the thematic maps and derive their weight. The second step employed a fuzzy multicriteria decision-making (FMCDM) technique for prioritizing the identified landfill sites. Thus, initially, the analytic hierarchy process (AHP) was used for weighting the selected criteria, while the fuzzy technique for order of preference by similarity to ideal solution (FTOPSIS) was applied for addressing the uncertainty associated with decision-making and prioritizing the most suitable site. A case study was conducted in the city of Memari Municipality. The main goal of this study was the initial evaluation and acquisition of landfill candidate sites by utilizing GIS and the following decision criteria: (1) environmental criteria consisting of surface water, groundwater, land elevation, land use land cover, distance from urban residence and buildup, and distance from sensitive places; and (2) socioeconomic criteria including distance from the road, population density, and land value. For preparing the final suitability map, the integration of GIS layers and AHP was used. On output, 7 suitable landfill sites were identified which were further ranked using FTOPSIS based on expert's views. Finally, candidate site-7 and site-2 were selected as the most suitable for proposing new landfill sites in Memari Municipality. The results from this study showed that the integration of GIS with the MCDM technique can be highly applied for site suitability. The present study will be helpful to local planners and municipal authorities for proposing a planning protocol and suitable sites for sanitary landfill in the near future.


Assuntos
Sistemas de Informação Geográfica , Eliminação de Resíduos , Cidades , Técnicas de Apoio para a Decisão , Índia , Instalações de Eliminação de Resíduos
7.
Curr Top Med Chem ; 21(8): 686-695, 2021.
Artigo em Inglês | MEDLINE | ID: mdl-33280598

RESUMO

BACKGROUND: Liver cancer is ranked as the fifth most prevalent and third most lethal cancer worldwide. The incidence rates of this cancer are on the rise, and only limited treatment options are available. METHODS: To identify and optimize the inhibitors of liver cancer cell-lines, a QSAR model was developed by using multiple linear regression methods. The robustness of the model was validated through statistical methods and wet-lab experiments. RESULTS: The developed QSAR models yielded high activity descriptor relationship accuracy of 91%, referred to by regression coefficient (r2= 0.91), and a high activity prediction accuracy of 89%. The external predicted (pred_r2) ability of the model was found to be 90%. CONCLUSION: The QSAR study indicates that chemical descriptors such as to measure of electronegative atom count (Epsilon3), atom type count descriptors (MMFF_10), number of a carbon atom connected with four single bonds (SssssCE- index), molecular weight and, number of oxygen atom connected with two aromatic bonds (SaaOE-index) are significantly correlated with anticancer activity. The model, which was validated statistically and through wet-lab experiments, was further used in the virtual screening of potential inhibitors against the liver cancer cell line WRL68. ADMET risk screening, synthetic accessibility, and Lipinski's rule of five are used to filter false positive hits. AfterwardS, to achieve a set of aligned ligand poses and rank the predicted active compounds, docking studies were carried out. The studied compounds and their metabolites were also analyzed for different pharmacokinetics parameters. Finally, a series of compounds was proposed as anticancer agents.


Assuntos
Antineoplásicos/farmacologia , Neoplasias Hepáticas/patologia , Antineoplásicos/química , Antineoplásicos/farmacocinética , Linhagem Celular Tumoral , Humanos , Simulação de Acoplamento Molecular , Relação Quantitativa Estrutura-Atividade , Reprodutibilidade dos Testes
8.
Nat Prod Res ; 34(2): 251-260, 2020 Jan.
Artigo em Inglês | MEDLINE | ID: mdl-30580605

RESUMO

Eugenol is a phytochemical present in aromatic plants has generated considerable interest in the pharmaceutical industries mainly in cosmetics. A series of eugenol esters (ST1-ST7) and chloro eugenol (ST8) have been synthesized. The structures of newly synthesized compounds were confirmed by 1H and 13C NMR and mass spectrometry. In an effort to evaluate the pharmacological activity of eugenol derivatives, we explored its anti-inflammatory potential against skin inflammation using in-vitro and in-vivo bioassay. Synthesized derivatives significantly inhibited the production of pro-inflammatory cytokines against LPS-induced inflammation in macrophages. Among all derivatives, ST8 [Chloroeugenol (6-chloro, 2-methoxy-4-(prop-2-en-1-yl)-phenol)] exhibited most potent anti-inflammatory activity without any cytotoxic effect. We have further evaluated the efficacy and safety in in-vivo condition. ST8 exhibited significant anti-inflammatory activity against TPA-induced skin inflammation without any skin irritation effect on experimental animals. These findings suggested that ST8 may be a useful therapeutic candidate for the treatment of skin inflammation.


Assuntos
Anti-Inflamatórios/farmacologia , Dermatite/tratamento farmacológico , Eugenol/síntese química , Animais , Anti-Inflamatórios/síntese química , Citocinas/antagonistas & inibidores , Eugenol/análogos & derivados , Eugenol/farmacologia , Macrófagos/efeitos dos fármacos , Macrófagos/patologia , Compostos Fitoquímicos/farmacologia
9.
Molecules ; 24(21)2019 Nov 01.
Artigo em Inglês | MEDLINE | ID: mdl-31683952

RESUMO

Four new constituents, as cis-6-oxogeran-4-enyl-10-oxy-O-ß-arabinopyranosyl-4'-O-ß-arabinopyranosyl-2''-octadec-9''',12''',15'''-trienoate (1), geran-3(10)-enyl-1-oxy-O-ß-arabinopyranosyl-4'-O-ß-arabinopyranosyl-2''-octadec-9''',12''',15'''-trienoate (2), geranilan-8-oxy-O-α-d-xylopyranosyl-2'-n-octadec-9'',12'',15''-trienoate (3), 1-cyclohex-2', 5'-dienyl 1-cyclohexylethanol-O-ß-d-xylopyranoside (4), along with six known constituents, guaiacol-O-ß-d-arabinopyaranoside (5), n-tetradecanyl oleate (6), oleyl-O-ß-d-xyloside (7), n-octadec-9,12-dienoyl-O-ß-d-arabinopyranoside (8), linolenyl-O-ß-d-arabinofuranoside (9) andglyceryl-1,3-dipalmito-2-olein (10), were isolated and identified from the Dendropanax morbifera bark. The new structures were established by one-and two-dimensional NMR (and in combination with IR, FAB-MSand HR-ESI-FTMS. The comparative evaluation of antioxidant potential by phosphomolybdenum, DPPH, FRAP and the NO assay of four different compounds (1-4), we have found that the compounds 1 and 2 have power as a natural antioxidant, whereas the compound 3 and 4 exhibited mild activity in comparison to compounds 1 and 2.


Assuntos
Antioxidantes/química , Araliaceae/química , Triterpenos/química , Antioxidantes/classificação , Ácidos Graxos/química , Ácidos Graxos/isolamento & purificação , Glicosídeos/química , Glicosídeos/isolamento & purificação , Estrutura Molecular , Casca de Planta/química , Extratos Vegetais/química , Extratos Vegetais/farmacologia , Saponinas/química , Saponinas/isolamento & purificação , Triterpenos/classificação , Triterpenos/isolamento & purificação
10.
Saudi Pharm J ; 27(5): 643-649, 2019 Jul.
Artigo em Inglês | MEDLINE | ID: mdl-31297018

RESUMO

This study was the first to detect the presence of the two compounds momilactone A (MA) and momilactone B (MB) in rice bran using liquid chromatography-electrospray ionization-mass spectrometry (LC-ESI-MS). By in vitro assays, both MA and MB exhibited potent inhibitory activities on pancreatic α-amylase and α-glucosidase which were significantly higher than γ-oryzanol, a well-known diabetes inhibitor. Remarkably, MA and MB indicated an effective inhibition on trypsin with the IC50 values of 921.55 and 884.03 µg/mL, respectively. By high-performance liquid chromatography (HPLC), quantities of MA (6.65 µg/g dry weight) and MB (6.24 µg/g dry weight) in rice bran were determined. Findings of this study revealed the α-amylase, α-glucosidase and trypsin inhibitors MA and MB contributed an active role to the diabetes inhibitory potential of rice bran.

11.
Molecules ; 24(5)2019 Mar 03.
Artigo em Inglês | MEDLINE | ID: mdl-30832436

RESUMO

This paper reports the successive isolation and purification of bioactive compounds from the stem bark of Jatropha podagrica, a widely known medicinal plant. The ethyl acetate extract of the stem bark exhibited the strongest antioxidant activity assessed by 2,2-diphenyl-1-picrylhydrazyl (DPPH), 2,2'-azinobis-(3-ethylbenzothiazoline-6-sulfonic acid) (ABTS) radical scavenging, and ferric reducing antioxidant power (FRAP) assays (IC50 = 46.7, 66.0, and 492.6, respectively). By column chromatography (CC) with elution of hexane and ethyl acetate at 8:2, 7:3, and 6:4 ratios, the isolation of this active extract yielded five fractions (C1⁻C5). Chemical structures of the constituents included in C1⁻C5 were elucidated by gas chromatography-mass spectrometry (GC-MS), electrospray ionization-mass spectrometry (ESI-MS), and nuclear magnetic resonance (NMR) and resolved as methyl gallate (C1, C2, C3, C4), gallic acid (C1, C2), fraxetin (C2, C3, C4, C5), and tomentin (C3). Mixture C2 (IC50 DPPH and ABTS = 2.5 µg/mL) and C3 (IC50 FRAP = 381 µg/mL) showed the highest antioxidant properties. Among the isolated fractions, C4 was the most potential agent in growth inhibition of six bacterial strains including Staphylococcus aureus, Escherichia coli, Klebsiella pneumoniae, Listeria monocytogenes, Bacillus subtilis, and Proteus mirabilis (MIC = 5, 20, 30, 20, 25, and 20 mg/mL, respectively). All identified constituents exerted an inhibitory activity on the growth of Lactuca sativa, of which the mixture C3 performed the maximal inhibition on shoot (IC50 = 49.4 µg/mL) and root (IC50 = 47.1 µg/mL) growth. Findings of this study suggest that gallic acid, methyl gallate, fraxetin, and tomentin isolated from J. podagrica possessed antioxidant, antibacterial, and growth inhibitory potentials.


Assuntos
Antioxidantes/química , Jatropha/química , Extratos Vegetais/química , Staphylococcus aureus/efeitos dos fármacos , Antibacterianos/isolamento & purificação , Antibacterianos/farmacologia , Antioxidantes/isolamento & purificação , Antioxidantes/farmacologia , Benzotiazóis/química , Compostos de Bifenilo/química , Compostos de Bifenilo/farmacologia , Proliferação de Células/efeitos dos fármacos , Cumarínicos/química , Cumarínicos/farmacologia , Ácido Gálico/análogos & derivados , Ácido Gálico/química , Ácido Gálico/farmacologia , Humanos , Testes de Sensibilidade Microbiana , Picratos/química , Casca de Planta/química , Caules de Planta/química , Espectrometria de Massas por Ionização por Electrospray , Staphylococcus aureus/patogenicidade , Ácidos Sulfônicos/química
12.
Exp Gerontol ; 120: 50-61, 2019 06.
Artigo em Inglês | MEDLINE | ID: mdl-30825547

RESUMO

Ageing is a progressive deterioration in functional and structural well-being of the body, accompanied with age-associated neurological disorders such as Parkinson's disease (PD), Alzheimer's disease and Huntington's disease. PD is marked with motor function decline, progressive neurodegeneration due to aggregation of insoluble α-synuclein in the dopaminergic neuron. Here we investigated the effect of tambulin (3,5-dihydroxy-7,8-dimethoxy-2-(4-methoxyphenyl) chromen-4-one), a hydroxy substituted flavanol isolated from fruits of Zanthoxyllum armatum DC (Family-Rutaceae) for its longevity promoting and neuromodulatory activities using Caenorhabditis elegans model system. Our results show that tambulin treatment significantly enhance lifespan and stress tolerance in worms, along with mitigation of ageing biomarkers like lipofuscin and protein carbonyl. In line with the alleviated ROS levels, tambulin treatment led to upregulated mRNA expression of ROS scavenging genes viz., sod-1, sod-3, and ctl-2. Upregulation in daf-16 gene indicates the involvement of insulin signaling pathway in tambulin mediated longevity. Tambulin treatment exhibited curtailed PD manifestations in terms of reduced α-synuclein levels, lipid accumulation, improved locomotary behavior and dopamine levels. Altogether, our data suggest that tambulin mediated alleviation of PD manifestations possibly involved PD counter protective machinery as evident through upregulated mRNA expression of lagr-1, ymel-1, pdr-1, ubc-12, and lrk-1. Our studies present tambulin as a potential molecule for its properties against ageing and Parkinson's disease. Further studies are speculated to realize the mechanistic and pharmacological aspects of tambulin.


Assuntos
Envelhecimento/efeitos dos fármacos , Benzopiranos/farmacologia , Caenorhabditis elegans/efeitos dos fármacos , Longevidade/efeitos dos fármacos , Doença de Parkinson/tratamento farmacológico , Zanthoxylum/química , Animais , Apoptose/efeitos dos fármacos , Dopamina/análise , Lipofuscina/metabolismo , Locomoção/efeitos dos fármacos , Estresse Oxidativo/efeitos dos fármacos , Carbonilação Proteica , alfa-Sinucleína/química
13.
Molecules ; 24(3)2019 Jan 29.
Artigo em Inglês | MEDLINE | ID: mdl-30700006

RESUMO

Momilactones A (MA) and B (MB) are the active phytoalexins and allelochemicals in rice. In this study, MA and MB were purified from rice husk of Oryza sativa cv. Koshihikari by column chromatography, and purification was confirmed by high-performance liquid chromatography, thin-layer chromatography, gas chromatography-mass spectrometry, liquid chromatography-electrospray ionization-mass spectrometry (LC-ESI-MS), and ¹H and 13C nuclear magnetic resonance analyses. By in vitro assays, both MA and MB exerted potent inhibition on α-amylase and α-glucosidase activities. The inhibitory effect of MB on these two key enzymes was greater than that of MA. Both MA and MB exerted greater α-glucosidase suppression as compared to that of the commercial diabetic inhibitor acarbose. Quantities of MA and MB in rice grain were 2.07 ± 0.01 and 1.06 ± 0.01 µg/dry weight (DW), respectively. This study was the first to confirm the presence of MA and MB in refined rice grain and reported the α-amylase and α-glucosidase inhibitory activity of the two compounds. The improved protocol of LC-ESI-MS in this research was simple and effective to detect and isolate MA and MB in rice organs.


Assuntos
Diterpenos/farmacologia , Inibidores de Glicosídeo Hidrolases/química , Lactonas/farmacologia , Oryza/química , alfa-Amilases/antagonistas & inibidores , Amilases/antagonistas & inibidores , alfa-Glucosidases/metabolismo
14.
Saudi Pharm J ; 27(1): 17-24, 2019 Jan.
Artigo em Inglês | MEDLINE | ID: mdl-30627048

RESUMO

This paper reports comparative extraction efficiencies and enhancement methods for natural herbicidal (growth inhibitors) compounds, momilactone A and B, respectively from the dried husks of Oryza sativa using different extraction techniques and different solvent systems. Four different extraction techniques viz. percolation, agitation with heat, sonication and soxhlet using five solvent systems as ethyl acetate, acetone, acetonitrile, methanol and methanol:water (8:2) were evaluated. In these studies, it was observed that maximum extract yield was obtained using in methanol and methanol/water mixture as extracting solvent by soxhlet technique although the content of total momilactones A and B was higher in the methanol/water mixture in comparison to other extractions. The successive and simple isolation enrichment technique for momilactones A and B were achieved by solid-matrix partitioning after the treatment of methanolic extract with charcoal and using ethyl acetate as extracting solvent for momilactones A and B. The quantitative analysis of the extraction and enrichment development protocol was validated by a simple, accurate, reproducible RP-HPLC-UV-VIS method using a binary gradient elution comprising of acetonitrile and water (70:30). The separation was achieved on a waters Spherisorb S10 ODS 2 column (250 × 4.6 mm, I.D., 10 µm) that achieved a greater degree of linearity within an overall concentration of extracts and momilactones A and B, 1 mg mL-1 and higher degree of correlation (0.9928 ≤ r2 ≤ 0.9936) for momilactones A and B. So far, comparative extraction of momilactones A and B and HPLC of these compounds has not been reported. Standards of momilactones A (1) and B (2) were isolated along with other two compounds as orizaterpenoid (3) and 7-ketostigmaterol (4) from ethyl acetate extract of rice hulls of O. sativa and checked purity by HPLC-PDA-MS and identification of these isolated compounds (1-4) by complete spectroscopic techniques as IR, 1H NMR, 13C NMR, 2D NMR and HR-MS. The qualitative analysis of momilactone A and B separation technique by thin layer chromatography was also developed.

15.
Nat Prod Res ; 33(5): 665-672, 2019 Mar.
Artigo em Inglês | MEDLINE | ID: mdl-29161887

RESUMO

Chemical investigations on the fruits of Zanthoxylum armatum Roxb. (Rutaceae) led to the isolation of two new constituents characterised as 2α-methyl-2ß-ethylene-3ß-isopropyl-cyclohexan-1ß, 3α-diol (1) and phenol-O-ß-D-arabinopyranosyl-4'-(3″, 7″, 11″, 15″-tetramethyl)-hexadecan-1″-oate (2) along with known compounds m-methoxy palmityloxy benzene (3), acetyl phenyl acetate (4), linoleiyl-O-α-D-xylopyranoside (5), m-hydroxyphenoxy benzene (6) and palmitic acid (7). The chemical structures were established with the help of physical, chemical and spectroscopic methods. The anti-inflammatory potential of isolated compounds 1 and 2 was evaluated using in vitro target-based anti-inflammatory activity in LPS-stimulated primary peritoneal macrophages isolated from mice. Production of pro-inflammatory cytokines (TNF-α and IL-6) was significantly inhibited by the treatment of isolated compounds 1 and 2 in a dose-dependent manner.


Assuntos
Anti-Inflamatórios/farmacologia , Frutas/química , Macrófagos Peritoneais/efeitos dos fármacos , Zanthoxylum/química , Animais , Anti-Inflamatórios/isolamento & purificação , Citocinas/metabolismo , Feminino , Índia , Camundongos , Camundongos Endogâmicos BALB C , Estrutura Molecular , Compostos Fitoquímicos/isolamento & purificação , Compostos Fitoquímicos/farmacologia
16.
J Ethnopharmacol ; 230: 1-8, 2019 Feb 10.
Artigo em Inglês | MEDLINE | ID: mdl-30342965

RESUMO

ETHNOPHARMACOLOGICAL RELEVANCE: Tejovati (Zanthoxylum armatum DC; Family- Rutaceae) popularly known as toothache tree is widely distributed in sub-tropical Himalaya region. Traditionally, The Southeast Asian population of Indo-Nepal origin uses it to treat asthma, gout, pain, and inflammation. The Ayurvedic action of the plant includes the balancing of Vata-Kapha in the body. Which lead to various ailments related to the circulation of blood and water, digestion, immunity, and skin. Therefore, in-vitro xanthine oxidase (XO) inhibition potential of the extract could be worth to explore prospect in the prevention/treatment of gouty affections of the joints and other diseases. AIM OF STUDY: Anti-inflammatory and antioxidant potential of Z. armatum fruit (ZAF) has been reported. To date, no scientific study to validate the claim for gout treatment/management has been attempted so far. The present study deals with the xanthine oxidase inhibitory potential of a various extract of ZAF and marker-based high-performance liquid chromatography (HPLC) standardization of most active fraction. MATERIALS AND METHODS: Liquid-liquid partioning of crude methanol extract of the ZAF followed by repeated column chromatography of most active fraction has resulted in the isolation of seven compounds. Five distinct groups of compounds were isolated, purified, and identified. We have investigated the therapeutic action of ZAF in the management of gout through in-vitro assay of XO, a key enzyme involved in gout pathogenesis. RESULTS: Phytochemical investigation of ZAF has resulted in the isolation of seven compounds of diverse nature. It is noteworthy to mention that out of seven, five compounds have shown the xanthine oxidase inhibitory action. The ethyl acetate fraction was most potent to inhibit XO. The XO inhibitory activity (IC50 values) of isolated marker chemical was ranging from 5.62 to 41.21 µM. Three compounds viz. acetyl phenyl acetate (ZA-2), prudomestin (ZA-6), and tambulin (ZA-7) showed the most potent XO inhibitory activity (IC50 ≈ 6 µM) comparable with a positive control (Allopurinol, IC50, 3.38 µM). This is the first validated HPLC-PDA method for simultaneous analysis and accurate quantification of seven compounds (phenolic acid, acetyl phenyl acetate, xylopyranoside, diphenyl ether and three flavones) in ZAF as well as their distribution in other tissues of the plant. CONCLUSION: Most potent three chemicals (ZA-2, 6 and 7) could be considered as bioactive to ensure the robust quality of the enriched fraction of ZAF with defined XO inhibition potential. Therefore, either single purified component or their enriched fraction could be a better choice for the management of gout than the crude extract of ZAF. Developed HPLC method is suitable for quality assurance analysis and process control of ZAF derived product intended for gout management. XO inhibitory potential exhibited by the characterized compounds validate the traditional use of this ZAF for the treatment of gout. Further, a detailed study is required to assess the effect of ZAF chemicals on serum uric acid and mechanism of XO inhibition.


Assuntos
Supressores da Gota/farmacologia , Extratos Vegetais/farmacologia , Xantina Oxidase/antagonistas & inibidores , Zanthoxylum , Frutas
17.
Molecules ; 24(1)2018 Dec 25.
Artigo em Inglês | MEDLINE | ID: mdl-30585211

RESUMO

Rice (Oryza sativa L.) contains generous amounts of carbohydrates, proteins, vitamins, and dietary fibers, in addition to secondary metabolites such as phenols and flavonoids that act as antioxidants. The phenolic compounds detected in rice (organic rice (OR), conventional rice (CR), and pesticide-free rice (PFR)), namely, protocatechuic, gentisic, p-hydroxybenzoic, p-coumaric, ferulic, salicylic, and caffeic acids, are notable free radical scavengers. The sum of these phenolic compounds was found to be higher in PFR, followed by CR and OR (p < 0.0001), when the rice types were classified based on the farming system employed. In addition, significant differences were observed in the p-hydroxybenzoic acid levels for the OR and CR groups compared with the PFR groups (p < 0.01). Furthermore, greater quantities of p-coumaric acid were found in CR-08 and OR-02, although these groups contained overall higher and lower sums of phenolic compounds, respectively. Moreover, significance was observed in the sum of the phenolic compounds, although only small quantities were found in polished rice. Further research is thus required to provide a clearer picture regarding the phenolic profiles of different rice brands.


Assuntos
Oryza/química , Fenóis/análise , Antioxidantes/análise , Antioxidantes/química , Cromatografia Líquida de Alta Pressão , Flavonoides/análise , Flavonoides/química , Espectrometria de Massas em Tandem/métodos
18.
Molecules ; 23(10)2018 Oct 21.
Artigo em Inglês | MEDLINE | ID: mdl-30347888

RESUMO

Soybeans are low in saturated fat and a rich source of protein, dietary fiber, and isoflavone; however, their nutritional shelf life is yet to be established. This study evaluated the change in the stability and quality of fatty acids in raw and roasted soybean flour under different storage temperatures and durations. In both types of soybean flour, the fatty-acid content was the highest in the order of linoleic acid (18-carbon chain with two double bonds; C18:2), oleic acid (C18:1), palmitic acid (C16:0), linolenic acid (18:3), and stearic acid (C18:0), which represented 47%, 26%, 12%, 9%, and 4% of the total fatty-acid content, respectively. The major unsaturated fatty acids of raw soybean flour-oleic acid, linoleic acid, and linolenic acid-decreased by 30.0%, 94.4%, and 97.7%, and 38.0%, 94.8%, and 98.0% when stored in polyethylene and polypropylene film, respectively, after 48 weeks of storage under high-temperature conditions. These values were later increased due to hydrolysis. This study presents the changes in composition and content of two soybean flour types and the changes in quality and stability of fatty acids in response to storage temperature and duration. This study shows the influence of storage conditions and temperature on the nutritional quality which is least affected by packing material.


Assuntos
Ração Animal , Ácidos Graxos/química , Farinha/análise , Glycine max/química , Ácidos Graxos/classificação , Ácidos Graxos/isolamento & purificação , Temperatura Alta , Ácido Linoleico/química , Ácido Linoleico/isolamento & purificação , Valor Nutritivo , Ácido Oleico/química , Ácido Oleico/isolamento & purificação , Ácido Palmítico/química , Ácido Palmítico/isolamento & purificação , Ácidos Esteáricos/química , Ácidos Esteáricos/isolamento & purificação , Temperatura , Ácido alfa-Linolênico/química , Ácido alfa-Linolênico/isolamento & purificação
19.
Molecules ; 23(8)2018 Aug 02.
Artigo em Inglês | MEDLINE | ID: mdl-30072644

RESUMO

Four new constituents, as 5, 7-dihydroxy-4'-methoxyflavonol-3-O-ß-d-arabinopyranosyl-(2''→1''')-O-ß-d-arabinopyrnosyl-2'''-O-3'''', 7''''-dimethylnonan-1''''-oate (1), 5-hydroxy-7, 4'-dimethoxyflavone-5-O-α-d-arabinopyranosyl-(2"→1''')-O-α-d-arabinopyranosyl-2'''-O-3'''', 7''''-dimethylnonan-1''''-oate (2), 5-hydroxy-7, 4'-dimethoxyflavone-5-O-ß-d-arabinofuranosyl-(2"→1''')-O-ß-d-arabinopyranosyl-2'''-O-lanost-5-ene (3) and 4',4''-diferuloxy feruloyl-O-α-d-arabinopyranosyl-(2a→1b)-O-α-d-arabinopyranosyl-(2b→1c)-O-α-d-arabinopyranosyl-(2c→1d)-O-α-d-arabinopyranosyl-(2d→1e)-O-α-d-arabinopyranosyl-2e-3''', 7'''-dimethylnonan-1'''-oate (4), along with three known compounds (5⁻7) were isolated from Oryza sativa leaves and straw. The structures of new and known compounds were elucidated by 1D (¹H and 13C NMR) and 2D NMR spectral methods, viz: COSY, HMBC, and HSQC aided by mass techniques and IR spectroscopy. The cytotoxicity of these constituents was assessed by using (RAW 264.7) mouse macrophage cell line, and allelopathic effects of compounds (1⁻7) on the germination and seedling growth characteristics such as seedling length and root length of barnyardgrass (Echinochloa oryzicola) were evaluated. Significant inhibitory activity was exhibited by compounds comprising flavone derivatives such as (1⁻3) on all of seed germination characteristics. The allelopathic effect of flavone derivatives were more pronounced on seedling length and root length than the germination characteristics. The higher concentration of flavone derivatives showed stronger inhibitory effects, whereas the lower concentrations showed stimulatory effects in some cases.


Assuntos
Glicosídeos/toxicidade , Macrófagos/citologia , Oryza/química , Feromônios/farmacologia , Polifenóis/toxicidade , Animais , Compostos de Bifenilo/química , Espectroscopia de Ressonância Magnética Nuclear de Carbono-13 , Morte Celular/efeitos dos fármacos , Sobrevivência Celular/efeitos dos fármacos , Sequestradores de Radicais Livres/química , Germinação/efeitos dos fármacos , Glicosídeos/química , Macrófagos/efeitos dos fármacos , Macrófagos/metabolismo , Camundongos , Feromônios/química , Picratos/química , Raízes de Plantas/anatomia & histologia , Raízes de Plantas/efeitos dos fármacos , Brotos de Planta/anatomia & histologia , Brotos de Planta/efeitos dos fármacos , Polifenóis/química , Espectroscopia de Prótons por Ressonância Magnética , Células RAW 264.7 , Sementes/crescimento & desenvolvimento
20.
Saudi Pharm J ; 26(3): 375-387, 2018 Mar.
Artigo em Inglês | MEDLINE | ID: mdl-29556129

RESUMO

Five new flavonoids namely, 5-hydroxy-6-isoprenyl-7,4'-dimethoxyflavonol-3-O-ß-d-arabinofuranoside (1), 5,7-dihydroxy-4'-methoxyflavone-7-O-ß-d-arabinopyranosyl-2''-n-decan-1'''-oate (2), 3-butanoyl-5,6,8-trihydroxy-7,4'-dimethoxyflavonol--5-O-ß-d-glucopyranoside (3), 7, 4'-dimethoxy-5-hydroxyflavone-5-O-α-d-arabinopyranosyl-(2'' → 1''')-O-α-d-arabinopyranoside (4), and 5,6-dihydroxy-7, 4'-dimethoxyflavone-5-O-α-d-glucopyranoside (5), together with two known compounds, were isolated from the methanol extract of Oryza sativa leaves and straw. Their structures of new compounds were elucidated by 1D and 2D NMR spectral methods, viz: COSY, HMBC and HSQC aided by mass techniques and IR spectroscopy. The cytotoxicity of these compounds (1-7) were assessed by using (RAW 264.7) mouse macrophages cell line, and allelopathic effects of compounds (1-7) on the germination characteristics of barnyardgrass (Echinochloa oryzicola) and pigweed (Chenopodium album L.) were also evaluated. The compounds 1, 6 and 7 showed cytotoxicity and compounds 1-7 exhibited significant inhibitory activity on the seed germination of two weed species.

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