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1.
J Pharm Pharmacol ; 76(1): 57-63, 2024 Jan 06.
Artículo en Inglés | MEDLINE | ID: mdl-37978932

RESUMEN

OBJECTIVES: To investigate the effect of blackseed oil (BSO) single dose on prednisolone pharmacokinetics via p-gp inhibition. METHODS: Three groups of rats (n = 5) were orally administered the vehicle, verapamil (50 mg/kg) or BSO (5 ml/kg) 15 min prior to prednisolone (5 mg/kg) administration. Blood samples were collected over 24 h and quantified. Non-compartmental analysis was employed to calculate maximum plasma concentration (Cmax), area under the curve (AUC0-last), time to reach Cmax (Tmax), apparent clearance (CL/F), and half-life (t1/2). Statistical significance was considered at p<0.05. RESULTS: Prednisolone Cmax and AUC0-last decreased by 65% and 25% in the BSO group compared to the negative control (P < .0001, .0029, respectively) while they increased by 1.75-folds and 8-folds in verapamil group (P < .0001). Tmax was achieved at 0.16, 0.5, and 0.25 h in the negative control, verapamil, and BSO-treated groups, respectively. CL/F in the treatment group was 1.3-fold and 10-fold higher compared to the negative and positive control, respectively, whereas the t1/2 remained comparable. CONCLUSION: Administration of BSO decreased prednisolone Cmax and AUC0-last in rats indicating that there is a herb-drug interaction; however, p-gp inhibition cannot be concluded. Patients relying on folk medicine in chronic illnesses treatment might need to avoid combining BSO with prednisolone.


Asunto(s)
Interacciones de Hierba-Droga , Prednisolona , Humanos , Ratas , Animales , Área Bajo la Curva , Verapamilo/farmacología , Aceites de Plantas/farmacología , Administración Oral
2.
Molecules ; 28(3)2023 Jan 30.
Artículo en Inglés | MEDLINE | ID: mdl-36770968

RESUMEN

Cisplatin (CP) is a platinum compound of the alkylating agent class that is used for the treatment of various types of cancer. However, CP treatments in cancer patients are accountable for nephrotoxicity, as it is a major adverse effect. Hence, this research study was proposed to investigate the nephroprotective effect of diosmin, a flavonoid glycoside of hesperidin derivatives against cisplatin-induced kidney damage. Wistar rats received a single intraperitoneal (i.p) injection of CP (7.5 mg/kg, i.p) to induce nephrotoxicity. The administration of CP significantly (p < 0.001) increased the markers of kidney function test (creatinine, blood urea nitrogen, and uric acid) and demonstrated histopathological changes in the kidney of the CP-treated nephrotoxic group. In addition, the CP-treated nephrotoxic group demonstrated a significant (p < 0.001) increase in lipid peroxidation (LPO) levels and depleted activities of reduced glutathione (GSH), glutathione peroxidase (GPx), glutathione reductase (GR), superoxide dismutase (SOD) and catalase (CAT).However, diosmin (100 and 200 mg/kg) treatments significantly reduced the elevated levels of kidney function test parameters and restored structural changes in the kidney (p < 0.001). The administration of diosmin (100 and 200 mg/kg) significantly (p < 0.001) reduced LPO levels, increased GSH content and showed improvements in the activities of GPx, GR, SOD and CAT. The markers of inflammatory cytokines such as IL-1ß, IL-6 and TNFα significantly (p < 0.001) increased in the CP-treated nephrotoxic group, whereas diosmin (100 and 200 mg/kg) treatments significantly (p < 0.001) reduced the elevated levels of these cytokines. The findings of this research demonstrate the nephroprotective effect of diosmin against CP-induced kidney damage. Therefore, we conclude that diosmin may be used as a supplement in the management of nephrotoxicity associated with CP treatments in cancer patients.


Asunto(s)
Diosmina , Enfermedades Renales , Ratas , Animales , Cisplatino/farmacología , Interleucina-6/metabolismo , Diosmina/farmacología , Factor de Necrosis Tumoral alfa/metabolismo , Ratas Wistar , Riñón , Enfermedades Renales/inducido químicamente , Enfermedades Renales/tratamiento farmacológico , Enfermedades Renales/prevención & control , Estrés Oxidativo , Antioxidantes/farmacología , Citocinas/metabolismo , Superóxido Dismutasa/metabolismo , Glutatión Peroxidasa/metabolismo
3.
Environ Res ; 220: 115169, 2023 03 01.
Artículo en Inglés | MEDLINE | ID: mdl-36587722

RESUMEN

To date, the development of renewable fuels has become a normal phenomenon to solve the problem of diesel fuel emissions and the scarcity of fossil fuels. Biodiesel production has some limitations, such as two-step processes requiring high free fatty acids (FFAs), oil feedstocks and gum formation. Hydrotreated vegetable oil (HVO) is a newly developed international renewable diesel that uses renewable feedstocks via the hydrotreatment process. Unlike FAME, FFAs percentage doesn't affect the HVO production and sustains a higher yield. The improved characteristics of HVO, such as a higher cetane value, better cold flow properties, lower emissions and excellent oxidation stability for storage, stand out from FAME biodiesel. Moreover, HVO is a hydrocarbon without oxygen content, but FAME is an ester with 11% oxygen content which makes it differ in oxidation stability. Waste sludge palm oil (SPO), an abundant non-edible industrial waste, was reused and selected as the feedstock for HVO production. Techno-economical and energy analyses were conducted for HVO production using Aspen HYSYS with a plant capacity of 25,000 kg/h. Alternatively, hydrogen has been recycled to reduce the hydrogen feed. With a capital investment of RM 65.86 million and an annual production cost of RM 332.56 million, the base case of the SPO-HVO production process was more desirable after consideration of all economic indicators and HVO purity. The base case of SPO-HVO production could achieve a return on investment (ROI) of 89.03% with a payback period (PBP) of 1.68 years. The SPO-HVO production in this study has observed a reduction in the primary greenhouse gas, carbon dioxide (CO2) emission by up to 90% and the total annual production cost by nearly RM 450 million. Therefore, SPO-HVO production is a potential and alternative process to produce biobased diesel fuels with waste oil.


Asunto(s)
Aceites de Plantas , Aguas del Alcantarillado , Aceite de Palma , Emisiones de Vehículos , Biocombustibles/análisis , Gasolina/análisis , Hidrógeno , Oxígeno
4.
Antioxidants (Basel) ; 12(1)2023 Jan 05.
Artículo en Inglés | MEDLINE | ID: mdl-36670996

RESUMEN

Gymnema sylvestre (GS) is a perennial woody vine native to tropical Asia, China, the Arabian Peninsula, Africa and Australia. GS has been used as a medicinal plant with potential anti-microbial, anti-inflammatory and anti-oxidant properties. This study was conceptualized to evaluate the cytotoxicity potential of Gymnema sylvestre saponin rich fraction (GSSRF) on breast cancer cell lines (MCF-7 and MDA-MB-468) by SRB assay. The anti-tumor activity of GSSRF was assessed in tumor-bearing Elrich ascites carcinoma (EAC) and Dalton's lymphoma ascites (DLA) mouse models. The anti-oxidant potential of GSSRF was assessed by DPPH radical scavenging assay. The acute toxicity of GSSRF was carried out according to OECD guideline 425. The yield of GSSRF was around 1.4% and the presence of saponin content in GSSRF was confirmed by qualitative and Fourier transform infrared spectroscopic (FTIR) analysis. The in vitro cytotoxic effects of GSSRF on breast cancer cell lines were promising and found to be dose-dependent. An acute toxicity study of GSSRF was found to be safe at 2000 mg/kg body weight. GSSRF treatment has shown a significant increase in the body weight and the life span of EAC-bearing mice in a dose-dependent manner when compared with the control group. In the solid tumor model, the doses of 100 and 200 mg/kg body weight per day have shown about 46.70% and 60.80% reduction in tumor weight and controlled the tumor weight until the 30th day when compared with the control group. The activity of GSSRF in both models was similar to the cisplatin, a standard anticancer agent used in the study. Together, these results open the door for detailed investigations of anti-tumor potentials of GSSRF in specific tumor models, mechanistic studies and clinical trials leading to promising novel therapeutics for cancer therapy.

5.
Sci Rep ; 12(1): 18698, 2022 11 04.
Artículo en Inglés | MEDLINE | ID: mdl-36333525

RESUMEN

The presence of metal with microwave irradiation has always invited controversial arguments as the metal will catch on fire easily. But interestingly, researchers found that arc discharge phenomena provide a promising way for molecule cracking to synthesize nanomaterials. This study developed a single-step yet affordable synthesis approach that combines microwave heating and arcing in transforming crude palm oil into magnetic nanocarbon (MNC), which can be considered a new alternative for the palm oil sectors. It involves synthesizing the medium at a partial inert condition with constant coiled stainless steel metal wire (dielectric media) and ferrocene (catalyst). This approach successfully demonstrates heating at a temperature ranging from 190.9 to 472.0 °C with different synthesis times (10-20 min). The produced MNC shows formations of spheres with average sizes of 20.38-31.04 nm, mesoporous structure (SBET: 14.83-151.95 m2/g), and high content of fixed carbon (52.79-71.24wt%), and the ratio of the D and G bands (ID/IG) is 0.98-0.99. The formation of new peaks in the FTIR spectra (522.29-588.48 cm-1) supports the appearance of the FeO compounds from the ferrocene. The magnetometer shows high magnetization saturation (22.32-26.84 emu/g) in ferromagnetic materials. The application of the MNC in wastewater treatment has been demonstrated by evaluating their adsorbent capability with Methylene Blue (MB) adsorption test at a different concentrations varying between 5 and 20 ppm. The MNC produced at synthesis time (20 min) shows the highest adsorption efficiency (10.36 mg/g) compared to others, with 87.79% removal of MB dye. As a result, the value for Langmuir is not promising compared to Freundlich, with R2 being around 0.80, 0.98, and 0.99 for MNC synthesized at 10 min (MNC10), 15 min (MNC15), and 20 min (MNC20), respectively. Hence, the adsorption system is in a heterogeneous condition. The microwave-assisted arcing thereby presents a promising approach to transforming CPO into MNC that could remove the hazardous dye.


Asunto(s)
Contaminantes Químicos del Agua , Purificación del Agua , Aceite de Palma/química , Metalocenos , Microondas , Adsorción , Contaminantes Químicos del Agua/química
6.
Biomed Res Int ; 2022: 5347224, 2022.
Artículo en Inglés | MEDLINE | ID: mdl-35928915

RESUMEN

Phytopathogenic fungi are serious threats in the agriculture sector especially in fruit and vegetable production. The use of plant essential oil as antifungal agents has been in practice from many years. Plant essential oils (PEOs) of Cuminum cyminum, Trachyspermum ammi, Azadirachta indica, Syzygium aromaticum, Moringa oleifera, Mentha spicata, Eucalyptus grandis, Allium sativum, and Citrus sinensis were tested against Fusarium oxysporum. Three phase trials consist of lab testing (MIC and MFC), field testing (seed treatment and foliar spray), and computer-aided fungicide design (CAFD). Two concentrations (25 and 50 µl/ml) have been used to asses MIC while MFC was assessed at four concentrations (25, 50, 75, and 100 µl/ml). C. sinensis showed the largest inhibition zone (47.5 and 46.3 m2) for both concentrations. The lowest disease incidence and disease severity were recorded in treatments with C. sinensis PEO. Citrus sinensis that qualified in laboratory and field trials was selected for CAFD. The chemical compounds of C. sinensis PEO were docked with polyketide synthase beta-ketoacyl synthase domain of F. oxysporum by AutoDock Vina. The best docked complex was formed by nootkatone with -6.0 kcal/mol binding affinity. Pharmacophore of the top seven C. sinensis PEO compounds was used for merged pharmacophore generation. The best pharmacophore model with 0.8492 score was screened against the CMNP database. Top hit compounds from screening were selected and docked with polyketide synthase beta-ketoacyl synthase domain. Four compounds with the highest binding affinity and hydrogen bonding were selected for confirmation of lead molecule by doing MD simulation. The polyketide synthase-CMNPD24498 showed the highest stability throughout 80 ns run of MD simulation. CMNPD24498 (FW054-1) from Verrucosispora was selected as the lead compound against F. oxysporum.


Asunto(s)
Fungicidas Industriales , Fusarium , Aceites Volátiles , Antifúngicos/farmacología , Fungicidas Industriales/farmacología , Pruebas de Sensibilidad Microbiana , Aceites Volátiles/química , Aceites Volátiles/farmacología , Aceites de Plantas/química , Aceites de Plantas/farmacología , Sintasas Poliquetidas
7.
Environ Res ; 214(Pt 4): 114149, 2022 11.
Artículo en Inglés | MEDLINE | ID: mdl-36007570

RESUMEN

Biodiesel is renewable, biodegradable, biocompatible (non-toxic) and environmentally friendly, which emits less pollution than traditional fossil-based diesel, making it the most promising and ideal option. However, biodiesel is facing many current issues, mostly related to the utilisation of homogeneous catalytic technology, and this circumstance obstructs its potential development and advancement. Therefore, new pathways for biodiesel production need to be explored, and the aforementioned issues need to be addressed. Recently, a study was conducted on the impregnated magnetic biochar derived from a waste palm kernel shell (PKS) catalyst that can replace conventional catalysts due to its reusability property. Nevertheless, the environmental impacts of impregnated magnetic biochar derived from waste PKS catalyst for biodiesel production are yet to be studied. This study focuses on the evaluation of the life cycle assessment (LCA) of palm-based cooking oil for biodiesel production catalysed by impregnated magnetic biochar derived from waste PKS. Simapro was used in this study to evaluate the impact assessment methodologies. Case 1 (6.64 × 102 Pt) has contributed less to environmental impacts than Case 2 (1.83 × 103 Pt). This indicates purchasing refined palm oil for biodiesel production may reduce environmental impacts by 64% compared to producing biodiesel from raw fruit bunches. In the midpoint assessment, the transesterification process was identified as the hotspot and marine aquatic ecotoxicity as the highest impact category with a value of 1.00 × 106 kg 1,4-DB eq for 1 tonne of biodiesel produced. The endpoint results showed that Case 1 revealed the greatest impact on the transesterification process, with cumulative damage of 461 Pt. Scenario without processing the raw palm fruit bunches to obtained palm oil was better than Case 2. Further research should be conducted on life cycle cost and sensitivity analysis to evaluate the economic feasibility and promote sustainable biodiesel production.


Asunto(s)
Biocombustibles , Aceites de Plantas , Animales , Catálisis , Carbón Orgánico , Estadios del Ciclo de Vida , Fenómenos Magnéticos , Aceite de Palma
8.
Artículo en Inglés | MEDLINE | ID: mdl-35722152

RESUMEN

Diabetes mellitus (DM) is a very common metabolic disorder/disease. The deterioration of ß-cells by autoimmune system is the hallmark of this disease. Thioredoxin-Interacting Protein (TXNIP) is responsible for ß-cells degradation by T-cells in the pancreas. This protein had been declared a good drug target for controlling DM. Lots of side effects have been reported as a result of long-time consumption of conventional antidiabetic drugs. The development of new and effective drugs with the minimal side effects needs time. TXNIP was selected as a target for Computer-Aided Drug Design. The antidiabetic fungal metabolite compounds were selected from the literature. The compounds were screened for their drug-likeness properties by DruLiTo and DataWarior tools. Twenty-two drug-like fungal compounds were subjected to Quantitative Structure-Activity Relationship (QSAR) analysis by using CheS-Mapper 2.0. The lowest (0.01) activity cliff was found for three compounds: Pinazaphilone A, Pinazaphilone B, and Chermesinone A. The highest value for apol (81.76) was shown by Asperphenamate, while Albonoursin and Sterenin L showed highest score (40.66) for bpol. The lowest value (0.46) for fractional molecular frame (FMF) was calculated for Pinazaphilone A and Pinazaphilone B. TPSA for Pinazaphilone A and Pinazaphilone B was 130.51 Å2. log P < 5 was observed for all the twenty-two compounds. Molecular docking of fungal compounds with TXNIP was done by AutoDock Vina. The binding energy for complexes ranged between -9.2 and -4.6 kcal/mol. Four complexes, TXNIP-Pinazaphilone A, TXNIP-Pinazaphilone B, TXNIP-Asperphenamate, and TXNIP-Sterenin L, were selected for MD simulation to find out the best lead molecule. Only one complex, TXNIP-Pinazaphilone B, showed a stable conformation throughout the 80 ns run of MD simulation. Pinazaphilone B derived from the Penicillium species fungi was selected as the lead molecule for development of antidiabetic drug having the least side effects.

9.
Biomed Res Int ; 2022: 8263999, 2022.
Artículo en Inglés | MEDLINE | ID: mdl-35528161

RESUMEN

Terpenoids and phenols from Trachyspermum ammi (T. ammi) have reported some pharmacological actions. The objective of the work was to isolate the active constituent, its identification by spectroscopic techniques, and evaluation of the antidiabetic and neuroprotective activity from T. ammi on STZ Wistar rats. The dried fruits of T ammi were kept in a hydrodistillation apparatus to collect essential oil. The isolated fraction went through TLC, UV, FTIR, HPLC, HRMS, C13, and 1H NMR for characterization. Two dosage concentrations from the isolated compound were prepared as 10 and 20 mg/kg for treatment groups. The groups were tested for thermal and mechanical hyperalgesia, writhing, grip strength, spontaneous locomotor test, neuromuscular coordination tests, and histopathological and lipid profile analysis. Diabetes was induced by streptozotocin (45 mg/kg i.p.) and 12 weeks of treatment-induced diabetic neuropathy in Wistar rats. Biomarkers were evaluated to understand the neuropathic protection of thymol on STZ-treated Wistar rats. The biomarker studies (SOD, NO, LPO, Na+K+ATPase, and TNF-α) further confirmed thymol's diabetic neuropathy protective action. This study suggests that isolated compound thymol was antidiabetic and neuroprotective as it has shown controlled glucose levels defensive nerve damage in STZ Wistar rats. P < 0.05 level of significance was observed in the levels of endogenous biomarkers, fasting blood glucose levels, actophotometer response, and response latency in treated groups compared to the diabetic group, whereas P < 0.001 level of significance during lipid profile levels, thermal algesia, and neuromuscular comparison tests was noted in treated groups compared to the diabetic group.


Asunto(s)
Ammi , Apiaceae , Diabetes Mellitus Experimental , Neuropatías Diabéticas , Aceites Volátiles , Animales , Biomarcadores , Glucemia , Diabetes Mellitus Experimental/patología , Neuropatías Diabéticas/tratamiento farmacológico , Frutas , Hipoglucemiantes/farmacología , Hipoglucemiantes/uso terapéutico , Aceites Volátiles/uso terapéutico , Ratas , Ratas Wistar , Estreptozocina , Timol
10.
Plants (Basel) ; 11(5)2022 Mar 06.
Artículo en Inglés | MEDLINE | ID: mdl-35270176

RESUMEN

The increase in the use of herbal medicines has led to the implementation of more stern regulations in terms of quality variation and standardization. As medicinal plants are prone to quality variation acquired due to differences in geographical origin, collection, storage, and processing, it is essential to ensure the quality, efficacy, and biological activity of medicinal plants. This study aims to standardize the widely used fruit, i.e., Prunus domestica Linn., using evaluation techniques (microscopic, macroscopic, and physicochemical analyses), advanced instrumental (HPLC, HPTLC, and GC-MS for phytochemical, aflatoxins, pesticides, and heavy metals), biological, and toxicological techniques (microbial load and antioxidant activities). The results revealed a 6-8 cm fruit with smooth surface, delicious odor, and acidic taste (macroscopy), thin-walled epidermis devoid of cuticle and any kind of excrescences with the existence of xylem and phloem (microscopy), LOD (15.46 ± 2.24%), moisture content (13.27 ± 1.75%), the high extractive value of 24.71 ± 4.94% in water:methanol (1:1; v/v) and with ash values in the allowed limits (physicochemical properties), and the presence of numerous phytochemical classes such as alkaloids, flavonoids, carbohydrates, glycosides, saponins, etc. (phytochemical screening). Furthermore, no heavy metals (Pb, Hg, Cd, Ar), pesticides, ad microbial limits were detected beyond the permissible limits specified, as determined with AAS, GC-MS analysis, and microbial tests. The HPTLC was developed to characterize a complete phytochemical behavior for the components present in P. domestica fruit extract. The parameters utilized with the method used and the results observed for the prunus herein may render this method an effective tool for quality evaluation, standardization, and quality control of P. domestica fruit in research, industries, and market available food products of prunus.

11.
Artículo en Inglés | MEDLINE | ID: mdl-35300069

RESUMEN

Neurodegeneration is the final event after a cascade of pathogenic mechanisms in several brain disorders that lead to cognitive and neurological loss. Quinolinic acid (QA) is an excitotoxin derived from the tryptophan metabolism pathway and is implicated in several ailments, such as Alzheimer's, Parkinson's, Huntington's, and psychosis disease. Diosmin (DSM) is a natural flavonoid possessing such properties that may halt the course of neurodegenerative progression. In past studies, free radical scavenging, along with properties, such as antihyperglycemic, anti-inflammatory, and vasoactive properties, of DSM were pragmatic. Hence, in the current experimentations, the neuroprotective activity of DSM was investigated in the QA rat prototype. QA was administered through the intracerebroventricular route (QA-ICV) in rats on day one, and DSM (50 and 100 mg/kg, intraperitoneal route) was given from day 1 to 21. Memory, gait, sensorimotor functions, and biomarkers of oxidative mutilation and mitochondrial functions were evaluated in the whole brain. Results showed significant deterioration of sensorimotor performance, gait, and working- and long-term memory in rats by QA-ICV. These behavioral anomalies were significantly attenuated by DSM (50 and 100 mg/kg) and donepezil (standard drug). QA-ICV-induced decrease in body mass (g), diet, and water ingestion were also attenuated by DSM or donepezil treatments. QA-ICV inhibited mitochondrial complex I and II activities that caused an increase in oxidative and nitrosative stress along with a reduction in endogenous antioxidants in the brain. DSM dose-dependently ameliorated mitochondrial functions and decreased oxidative stress in QA-ICV-treated rats. DSM can be a possible alternative in treating neurodegenerative disorders with underlying mitochondrial dysfunction pathology.

12.
Plants (Basel) ; 11(4)2022 Feb 21.
Artículo en Inglés | MEDLINE | ID: mdl-35214895

RESUMEN

Spondias mangifera is a drupaceous fruit popular for its flavour and health advantages. There is little scientific knowledge about S. mangifera, despite its widespread usage in traditional medicine, in the North-Eastern region of India. Inhibiting the key carbohydrate hydrolysing enzymes is one of the strategies for managing diabetes. Therefore, this study studied the antioxidant and anti-diabetic properties of different fraction S. mangifera fruit extract (SMFFs) from Indian geographical origin by in vitro experimental assays and silico docking simulation studies. The ADMET prediction for active substances was also investigated using the AdmetSAR database. Based on the binding affinity/molecular interactions between phytocompounds and target enzymes, in silico investigations were done to confirm the in vitro enzymatic inhibitory capability. ß-sitosterol in EtOH-F was analysed using RP-HPLC with RP-C18 column as stationary phase and photo diode array detector. The percentage of ß-sitosterol was found to be 1.21% ± 0.17% of total weight of extract (w/w). S. mangifera fruit ethanolic extract had a significant inhibitory concentration of 50% against free radicals produced by ABTS (89.71 ± 2.73%) and lipid peroxidation assay (88.26 ± 2.17%) tests. Similarly, the in vitro antidiabetic test findings indicated that S. mangifera inhibited alpha-amylase (73.42 ± 2.01%) and alpha-glucosidase (79.23 ± 1.98%) enzymes dose-dependently. The maximum glycosylated Hb percentage inhibitory activity shown in the ethanolic fraction was (83.97 ± 2.88%) at 500 µg/mL. The glucose uptake of the ethanolic fraction by the yeast cell showed significant (p < 0.05) at 500 µg/mL when compared with metformin (91.37 ± 1.59%), whereas the other fraction did not show the uptake of glucose by the yeast cell at the same concentration. In the docking study, the main phytoconstituents of S. mangifera fruit, such as oleanolic acid, beta-sitosterol, and beta amyrin, show strong affinity for pancreatic α-amylase. These results imply that S. mangifera has α-amylase and α-glucosidase inhibitory properties and may be used as antidiabetic with antioxidant characteristics.

13.
Artículo en Inglés | MEDLINE | ID: mdl-35096118

RESUMEN

OBJECTIVE: Medicinal plants and essentials oils are well known for diverse biological activities including antidiabetic potential. This study was designed to isolate essential oils from the leaves of Persicaria hydropiper L. (P. hydropiper), perform its phytochemical analysis, and explore its in vitro antidiabetic effects. MATERIALS AND METHODS: P. hydropiper leaves essential oils (Ph.Los) were extracted using a hydrodistillation apparatus and were subjected to phytochemical analysis using the gas chromatography mass spectrometry (GC-MS) technique. Ph.Lo was tested against two vital enzymes including α-glucosidase and α-amylase which are important targets in type-2 diabetes. The identified compounds were tested using in silico approaches for their binding affinities against the enzyme targets using MOE-Dock software. RESULTS: GC-MS analysis revealed the presence of 141 compounds among which dihydro-alpha-ionone, cis-geranylacetone, α-bulnesene, nerolidol, ß-caryophyllene epoxide, and decahydronaphthalene were the most abundant compounds. Ph.Lo exhibited considerable inhibitory potential against α-glucosidase enzyme with 70% inhibition at 1000 µg mL-1 which was the highest tested concentration. The inhibitory activity of positive control acarbose was 77.30 ± 0.61% at the same tested concentration. Ph.Lo and acarbose exhibited IC50 of 170 and 18 µg mL-1 correspondingly. Furthermore, dose-dependent inhibitions were observed for Ph.Lo against α-amylase enzyme with an IC50 of 890 µg mL-1. The top-ranked docking conformation was observed for ß-caryophyllene epoxide with a docking score of -8.3182 against α-glucosidase, and it has established seven hydrogen bonds and one H-pi interaction at the active site residues (Phe 177, Glu 276, Arg 312, Asp 349, Gln 350, Asp 408, and Arg 439). Majority of the identified compounds fit well in the binding pocket of Tyr 62, Asp 197, Glu 233, Asp 300, His 305, and Ala 307 active residues of α-amylase. ß-Caryophyllene epoxide was found to be the most active inhibitor with a docking score of -8.3050 and formed five hydrogen bonds at the active site residues of α-amylase. Asp 197, Glu 233, and Asp 300 active residues were observed to be making polar interactions with the ligand. CONCLUSIONS: The current study revealed that Ph.Lo is rich in bioactive metabolites which might contribute to its enzyme inhibitory potential. Inhibition of these enzymes is the key target in reducing postprandial hyperglycemia. However, further detailed in vivo studies are required for their biological and therapeutic activities.

14.
Curr Neuropharmacol ; 19(11): 1884-1895, 2021.
Artículo en Inglés | MEDLINE | ID: mdl-33588732

RESUMEN

BACKGROUND: Alzheimer's disease (AD) affects several people worldwide and has devastating impacts on society with a limited number of approaches for its pharmacological treatment. The main causes of AD are not clear yet. However, the formation of senile plaques, neurofibrillary tangles, hyper-phosphorylation of tau protein, and disruption of redox homeostasis may cause AD. These causes have a positive correlation with oxidative stress, producing reactive ions, which are responsible for altering the physiological condition of the body. CONCLUSION: Ongoing research recommended the use of phytochemicals as acetylcholinesterase inhibitors to hinder the onset and progression of AD. The natural compound structures, including lignans, flavonoids, tannins, polyphenols, triterpenes, sterols, and alkaloids have anti-inflammatory, antioxidant, and anti-amyloidogenic properties. The purpose of this article is to provide a brief introduction to AD along with the use of natural compounds as new therapeutic approaches for its management.


Asunto(s)
Enfermedad de Alzheimer , Acetilcolinesterasa , Enfermedad de Alzheimer/tratamiento farmacológico , Suplementos Dietéticos , Humanos , Ovillos Neurofibrilares , Fitoquímicos/uso terapéutico
15.
Waste Manag ; 118: 626-636, 2020 Dec.
Artículo en Inglés | MEDLINE | ID: mdl-33011540

RESUMEN

Due to its environment-friendly and replenishable characteristics, biodiesel has the potential to substitute fossil fuels as an alternative source of energy. Although biodiesel has many benefits to offer, manufacturing biodiesel on an industrial scale is uneconomical as a high cost of feedstock is required. A novel sulfonated and magnetic catalyst synthesised from a palm kernel shell (PMB-SO3H) was first introduced in this study for methyl ester or biodiesel production to reduce capital costs. The wasted palm kernel shell (PKS) biochar impregnated with ferrite Fe3O4 was synthesised with concentrated sulphuric acid through the sulfonation process. The SEM, EDX, FTIR, VSM and TGA characterization of the catalysts were presented. Then, the optimisation of biodiesel synthesis was catalysed by PMB-SO3H via the Response Surface Methodology (RSM). It was found that the maximum biodiesel yield of 90.2% was achieved under these optimum operating conditions: 65 °C, 102 min, methanol to oil ratio of 13:1 and the catalyst loading of 3.66 wt%. Overall, PMB-SO3H demonstrated acceptable catalysing capability on its first cycle, which subsequently showed a reduction of the reusability performance after 4 cycles. An important practical implication is that PMB-SO3H can be established as a promising heterogeneous catalyst by incorporating an iron layer which can substantially improve the catalyst separation performance in biodiesel production.


Asunto(s)
Biocombustibles , Aceites de Plantas , Carbón Orgánico , Esterificación , Fenómenos Magnéticos
16.
J Ayurveda Integr Med ; 11(4): 448-454, 2020.
Artículo en Inglés | MEDLINE | ID: mdl-32912644

RESUMEN

BACKGROUND: Myrica esculenta is a notable therapeutic plant widely utilized in Indian system of medicine. Ayurvedic literature reported fruit and bark of this plant is used in gulma, jvara, arsa, grahani, pandu roga, hrillasa, mukha roga, kasa, svasa, agnimandhya, aruchi, meha, and kantharoga. OBJECTIVE: The present study aimed to investigate the neuroprotective potential of "Himalayan Bayberry" (Myrica esculenta Buch.-Ham. ex D. Don) leaves methanol extract in Parkinson's disease induced by haloperidol. MATERIALS AND METHODS: The present investigation was completed in wistar rats, in which Parkinson's disease (PD) was induced with haloperidol 1 mg/kg, intraperitoneally. The rats were randomly divided into six gatherings and the test animals received the methanolic extract of M. esculenta (MEME) at a dose of 50, 100 and 200 mg/kg, orally for one week. Various behavioural, biochemical and histopathological parameters were estimated in haloperidol exposed rats. RESULTS: MEME demonstrated significant and dose-dependent increment in behavioural activity and improved muscle coordination. The significant diminution in malonaldehyde level while improved the level of antioxidant enzymes like catalase, superoxide dismutase and reduced glutathione in extract treated group were observed as compared to the control group. Histopathological changes revealed MEME significantly reduced haloperidol-induced damage in the substantia nigra and there was very little neuronal atrophy. CONCLUSION: The outcomes showed the defensive role of M. esculenta against PD. The mechanism of protection may be due to an escalation of cellular antioxidants.

17.
J Diet Suppl ; 17(1): 97-109, 2020.
Artículo en Inglés | MEDLINE | ID: mdl-30289011

RESUMEN

Berberis aristata is used for the treatment of diabetes, piles, and liver diseases. As the drug is broadly used in Indigenous systems of medicine, it was designed to set the quality standards and antimicrobial potential for the stem bark of Berberis aristata. Botanical, physicochemical, pharmacotoxicological, fluorescence, microbial load, and phytochemical parameters of the stem bark were determined. High-performance thin-layer chromatography (HPTLC) was carried out by the CAMAG-HPTLC system. Berberine, total phenolics, and flavonoids were estimated. The antimicrobial potential was determined against the bacteria Bacillus subtilis and Escherichia coli and fungi Penicillium citrinum and Aspergillus terreus. The foreign matter, foaming index, swelling index, bitterness value, resin content, loss on drying, total ash, acid-insoluble ash, water-soluble ash, heavy metals, microbial load, berberine content, total phenolic content, and total flavonoid content were found to be 0, 0, 5, 1.34, 0.86%, 2.07%, 4.33%, 0.28%, 2.66%, within limits, 6 colonies in 1/100 dilution, 0.032 mg/g, 144.04 µg/ml, and 85.61 µg/ml, respectively. Phytochemicals such as phenolics, flavonoids, and sterols were present in the methanolic extract. The fluorescences observed in UV light were of different colors in different solvents. The methanolic extract and standards exhibited antimicrobial activity at the tested concentrations against the microbial strains. Results confirmed the quality and purity of the drug B. aristata. Results also confirmed that methanolic extract of B. aristata stem bark possesses potent antimicrobial activity. Thus, the use of this quality-controlled plant-derived drug with established antimicrobial property could be of great significance in quality-control standardization and preventive and therapeutic approaches to infectious diseases.


Asunto(s)
Antibacterianos/farmacología , Antifúngicos/farmacología , Bacterias/efectos de los fármacos , Berberis/química , Hongos/efectos de los fármacos , Extractos Vegetales/farmacología , Aspergillus/efectos de los fármacos , Bacillus subtilis/efectos de los fármacos , Berberina/análisis , Berberina/farmacología , Cromatografía Líquida de Alta Presión , Escherichia coli/efectos de los fármacos , Flavonoides/análisis , Flavonoides/farmacología , Humanos , Penicillium/efectos de los fármacos , Fenoles/análisis , Fenoles/farmacología , Corteza de la Planta/química , Extractos Vegetales/química , Extractos Vegetales/normas , Tallos de la Planta/química , Control de Calidad
18.
Integr Med Res ; 5(4): 267-275, 2016 Dec.
Artículo en Inglés | MEDLINE | ID: mdl-28462128

RESUMEN

BACKGROUND: Traditional systems of medicine use herbal drugs for hepatoprotection. Thus, the study was designed to evaluate the hepatoprotective and antioxidant effects of Spondias pinnata bark extracts against ethanol-induced liver injury in Wistar rats. METHODS: Group I animals were treated with 1 mL/kg 0.3% carboxymethyl cellulose and Group II with 12 mL/kg 50% ethanol for 8 consecutive days. Groups III-VII animals were first treated with 400 mg/kg petroleum ether extract, chloroform extract, acetone extract (AE), ethanol extract (EE), and 100 mg/kg silymarin, and then 12 mL/kg 50% ethanol orally after 2 hours pretreatment each day for 8 consecutive days. Six hours after the last dose, blood was withdrawn. The hepatoprotective activity was assessed by several biochemical and antioxidant parameters. It was accomplished by the histopathology and DNA fragmentation study of liver tissues. RESULTS: Treatment with S. pinnata extracts, mainly AE and EE significantly (p < 0.05-0.01) and dose-dependently prevented the ethanol-induced increase in serum levels of aspartate aminotransferase, alanine aminotransferase, alkaline phosphatase, lactate dehydrogenase, cholesterol, bilirubin, and malondialdehyde, and decrease in reduced glutathione, catalase, superoxide dismutase, and albumin. They also attenuated the ethanol-induced DNA damage. Hepatoprotective potential of the extract was less than that of standard drug silymarin. Results of the study were well supported by the histopathological observations. CONCLUSION: S. pinnata extracts AE and EE possess a potent hepatoprotective effect against ethanol-induced liver injury in Wistar rats, and protect them from hepatotoxicity by prevention of ethanol-induced oxidative stress, DNA-damage and altered biochemical markers.

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