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1.
Pak J Pharm Sci ; 36(6): 1695-1707, 2023 Nov.
Artigo em Inglês | MEDLINE | ID: mdl-38124409

RESUMO

Diabetes mellitus (DM), a prevalent metabolic condition that impairs glucose metabolism, causes morbidity and hospitalization. Thus, there is need to establish novel therapeutics against DM. The current study examined the phytochemical analysis and antidiabetic effects of Carissa grandiflora leave extracts (CGLE) on streptozotocin (STZ)-induced DM in mice. CGLE (n-hexane, chloroform, ethanol) was extracted and phytochemically examined for primary and secondary metabolites. Fourier transformed infrared spectroscopy (FTIR) detected functional groups, while 2,2-diphenyl-1-picrylhydrazyl (DPPH) test assessed antioxidant capacity. Later, antidiabetic potential of CGLE extract was investigated in vivo in STZ induced diabetic mice. Phytochemical investigation revealed sugars, ketones, alkaloids, triterpenoids, and glycosides. FTIR indicated phenol, aldehyde, ketone, alkene, alkyne, alcohol, benzene ring and amines, while DPPH assay demonstrated antioxidant potential of extract. Oral CGLE treatment significantly improved body weight (P<0.05), polyphagia and polydipsia (P<0.05) and FBG (P<0.001). Moreover, CGLE extract reversed histopathological alterations in the pancreas, liver, and kidney of diabetic mice. These outcomes highlighted that C. grandiflora extract could be effective therapeutic approach against DM.


Assuntos
Diabetes Mellitus Experimental , Hipoglicemiantes , Camundongos , Animais , Hipoglicemiantes/uso terapêutico , Estreptozocina , Antioxidantes/farmacologia , Antioxidantes/uso terapêutico , Glicemia/metabolismo , Diabetes Mellitus Experimental/induzido quimicamente , Diabetes Mellitus Experimental/tratamento farmacológico , Diabetes Mellitus Experimental/metabolismo , Extratos Vegetais/química , Etanol/uso terapêutico
2.
ACS Omega ; 8(18): 15920-15931, 2023 May 09.
Artigo em Inglês | MEDLINE | ID: mdl-37179630

RESUMO

Cancer treatment development is hampered by chemotherapy side effects, drug resistance, and tumor metastasis, giving cancer patients a gloomy prognosis. Nanoparticles (NPs) have developed as a promising medicinal delivery technique in the last 10 years. The zinc oxide (ZnO) NPs can precisely and captivatingly promote the apoptosis of cancer cells in cancer treatment. There is also an urgent need to discover novel anti-cancer therapies, and current research suggests that ZnO NPs hold significant promise. ZnO NPs have been tested for phytochemical screening and in vitro chemical efficiency. The green synthesis method was employed for the preparation of ZnO NPs from Sisymbrium irio (L.) (Khakshi). An alcoholic and aqueous extract of S. irio was prepared using the Soxhlet method. Various chemical compounds were revealed in the methanolic extract through qualitative analysis. The results of quantitative analysis showed that the total phenolic content has the highest amount (42.7861 mgGAE/g), while the resultant amounts of (5.72175 mgAAE/g) and (15.20725 mgAAE/g) were obtained in total flavonoid content and antioxidant property, respectively. ZnO NPs were prepared using a 1:1 ratio. The synthesized ZnO NPs were identified to have a hexagonal wurtzite crystal arrangement. The nanomaterial was characterized by scanning electron microscopy, transmission electron microscopy, and UV-visible spectroscopy. The ZnO-NPs' morphology exhibited an absorbance at 350-380 nm. Furthermore, different fractions were prepared and assessed for anticancer activity. As a result of this anticancer activity, all fractions exhibited cytotoxic activity against both BHK and HepG2 human cancer cell lines. The methanol fraction showed the highest activity of 90% (IC50 = 0.4769 mg/mL), followed by the hexane fraction that showed 86.72%, ethyl acetate showed 85%, and chloroform fraction showed 84% against BHK and HepG2 cell lines. These findings suggested that synthesized ZnO-NPs have anticancer potential.

3.
Drug Dev Res ; 82(8): 1169-1181, 2021 12.
Artigo em Inglês | MEDLINE | ID: mdl-33983647

RESUMO

Urease plays a significant role in the pathogenesis of urolithiasis pyelonephritis, urinary catheter encrustation, hepatic coma, hepatic encephalopathy, and peptic acid duodenal ulcers. Salvinia molesta was explored to identify new bioactive compounds with particular emphasis on urease inhibitors. The aqueous methanol extract was fractionated using solvents of increasing polarity. A series of column chromatography and later HPLC were performed on butanol extract. The structures of the resulting pure compounds were resolved using NMR (1D and 2D), infrared, and mass spectroscopy. The novel isolate was evaluated for antioxidant activity (using DPPH, superoxide anion radical scavenging, oxidative burst, and Fe+2 chelation assays), anti-glycation behavior, anticancer activity, carbonic anhydrase inhibition, phosphodiesterase inhibition, and urease inhibition. One new glucopyranose derivative 6'-O-(3,4-dihydroxybenzoyl)-4'-O-(4-hydroxybenzoyl)-α/ß-D-glucopyranoside (1) and four known glycosides were identified. Glycoside 1 demonstrated promising antioxidant potential with IC50 values of 48.2 ± 0.3, 60.3 ± 0.6, and 42.1 ± 1.8 µM against DPPH, superoxide radical, and oxidative burst, respectively. Its IC50 in the Jack bean urease inhibition assay was 99.1 ± 0.8 µM. The mechanism-based kinetic studies presented that compound 1 is a mixed-type inhibitor of urease with a Ki value of 91.8 ± 0.1 µM. Finally, molecular dynamic simulations exploring the binding mode of compound 1 with urease provided quantitative agreement between estimated binding free energies and the experimental results. The studies corroborate the use of compound 1 as a lead for QSAR studies as an antioxidant and urease inhibitor. Moreover, it needs to be further evaluated through the animal model, that is, in vivo or tissue culture-based ex-vivo studies, to establish their therapeutic potential against oxidative stress phosphodiesterase-II and urease-induced pathologies.


Assuntos
Antioxidantes/isolamento & purificação , Extratos Vegetais/análise , Traqueófitas/química , Urease/antagonistas & inibidores , Antioxidantes/farmacologia , Inibidores Enzimáticos/isolamento & purificação , Medições Luminescentes , Simulação de Acoplamento Molecular , Inibidores de Fosfodiesterase/isolamento & purificação , Urease/química
4.
Sci Rep ; 11(1): 1708, 2021 01 18.
Artigo em Inglês | MEDLINE | ID: mdl-33462261

RESUMO

Ifosfamide is a widely used chemotherapeutic agent having broad-spectrum efficacy against several tumors. However, nephro, hepato, neuro cardio, and hematological toxicities associated with ifosfamide render its use limited. These side effects could range from organ failure to life-threatening situations. The present study aimed to evaluate the attenuating efficiency of Berberis vulgaris root extract (BvRE), a potent nephroprotective, hepatoprotective, and lipid-lowering agent, against ifosfamide-induced toxicities. The study design comprised eight groups of Swiss albino rats to assess different dose regimes of BvRE and ifosfamide. Biochemical analysis of serum (serum albumin, blood urea nitrogen, creatinine, alanine transaminase, aspartate transaminase, alkaline phosphatase, lactate dehydrogenase, total cholesterol, and triglycerides) along with complete blood count was performed. Kidney, liver, brain, and heart tissue homogenates were used to find malondialdehyde, catalase, and glutathione S-transferase levels in addition to the acetylcholinesterase of brain tissue. The results were further validated with the help of the histopathology of the selected organs. HeLa cells were used to assess the effect of BvRE on ifosfamide cytotoxicity in MTT assay. The results revealed that pre- and post-treatment regimens of BvRE, as well as the combination therapy exhibited marked protective effects against ifosfamide-induced nephro, hepato, neuro, and cardiotoxicity. Moreover, ifosfamide depicted a synergistic in vitro cytotoxic effect on HeLa cells in the presence of BvRE. These results corroborate that the combination therapy of ifosfamide with BvRE in cancer treatment can potentiate the anticancer effects of ifosfamide along with the amelioration of its conspicuous side effects.


Assuntos
Berberis/química , Encéfalo/efeitos dos fármacos , Ifosfamida/farmacologia , Rim/efeitos dos fármacos , Fígado/efeitos dos fármacos , Extratos Vegetais/farmacologia , Animais , Berberis/metabolismo , Contagem de Células Sanguíneas , Encéfalo/metabolismo , Encéfalo/patologia , Sobrevivência Celular/efeitos dos fármacos , Células HeLa , Humanos , Rim/metabolismo , Rim/patologia , Fígado/metabolismo , Fígado/patologia , Masculino , Estresse Oxidativo/efeitos dos fármacos , Extratos Vegetais/química , Raízes de Plantas/química , Raízes de Plantas/metabolismo , Ratos
5.
Biology (Basel) ; 9(8)2020 Jul 30.
Artigo em Inglês | MEDLINE | ID: mdl-32751610

RESUMO

Withania coagulans (W. coagulans) is well-known in herbal medicinal systems for its high biological potential. Different parts of the plant are used against insomnia, liver complications, asthma, and biliousness, as well as it is reported to be sedative, emetic, diuretic, antidiabetic antimicrobial, anti-inflammatory, antitumor, hepatoprotective, antihyperglycemic, cardiovascular, immuno-suppressive and central nervous system depressant. Withanolides present in W. coagulans have attracted an immense interest in the scientific field due to their diverse therapeutic applications. The current study deals with chemical and biological evaluation of chloroform, and n-butanol fractions of W. coagulans. The activity-guided fractionation of both extracts via multiple chromatographic steps and structure elucidation of pure isolates using spectroscopies (NMR, mass spectrometry, FTIR and UV-Vis) led to the identification of a new withanolide glycoside, withacogulanoside-B (1) from n-butanol extract and five known withanolides from chloroform extract [withanolid J (2), coagulin E (3), withaperuvin C (4), 27-hydroxywithanolide I (5), and ajugin E (6)]. Among the tested compounds, compound 5 was the most potent α-glucosidase inhibitor with IC50 = 66.7 ± 3.6 µM, followed by compound 4 (IC50: 407 ± 4.5 µM) and compound 2 (IC50: 683 ± 0.94 µM), while no antiglycation activity was observed with the six isolated compounds. Molecular docking was used to predict the binding potential and binding site interactions of these compounds as α-glucosidase inhibitors. Consequently, this study provides basis to discover specific antidiabetic compounds from W. coagulans.

6.
Artigo em Inglês | MEDLINE | ID: mdl-28331912

RESUMO

BACKGROUND: Escherichia coli is the agent responsible for a range of clinical diseases. With emerging antimicrobial resistance, other treatment options including solar/photo-therapy are becoming increasingly common. Visible Range Radiation Therapy/Colour Therapy is an emerging technique in the field of energy/vibrational medicine that uses visible spectrum of Electromagnetic Radiations to cure different diseases. In this study, our goal was to understand the effect of Visible Range Electromagnetic Radiations on E. coli (in vitro) and therefore find out the most appropriate visible range radiation for the treatment of diseases caused by E. coli. MATERIALS AND METHODS: A total of 6 non-repetitive E. coli isolates were obtained from urine samples obtained from hospitalized patients with UTI. Single colony of E. coli was inoculated in 3 ml of Lysogeny Broth (LB) and 40 µl of this E. coli suspension was poured into each of the plastic tubes which were then irradiated with six different wavelengths in the visible region (Table. 1) after 18 hours with one acting as a control. The Optical Densities of these irradiated samples were then measured. Furthermore, scanning electron microscopy (TEFCAN ZEGA3) was carried out. RESULTS: The analysis of the microscopic and SEM images of irradiated E. coli samples with six different visible range radiations is representative of The fact that E. coli responded differently to every applied radiation in the visible region and the most profound inhibitory effects were that of 538nm Visible Range Radiation (Green) which proved to be bactericidal and 590nm Visible Range Radiation (yellow) which was bacteriostatic. The enhanced growth of E. coli with varying degrees was clearly observed in 610nm (orange), 644nm (red), 464nm (Purple) and 453nm (blue). CONCLUSION: It can be concluded that 538nm (Green) and 590nm (Yellow) can effectively be used for treating E. coli borne diseases.


Assuntos
Infecções por Escherichia coli/microbiologia , Escherichia coli/efeitos da radiação , Campos Eletromagnéticos , Escherichia coli/crescimento & desenvolvimento , Humanos , Luz
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