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1.
Inflammopharmacology ; 31(6): 3047-3062, 2023 Dec.
Artigo em Inglês | MEDLINE | ID: mdl-37955785

RESUMO

Curcuma longa extract and its marker curcuminoids have potential use in inflammatory conditions. However, curcuminoids solubility and bioavailability are major hindrances to their bioactivity. The current study investigated green extraction-based curcuminoids-enriched extract (CRE) prepared from C. longa and its cyclodextrin inclusion complexes, i.e., binary inclusion complexes (BC) and ternary inclusion complexes (TC), in complete Freund's adjuvant (CFA)-induced mice for their comparative anti-arthritic efficacy. CRE, BC, and TC (2.5 and 5 mg/kg) with the standard drug diclofenac sodium (13.5 mg/kg) were orally administered to mice for 4 weeks. Variations in body weight, hematological and biochemical parameters, along with gene expression analysis of arthritis biomarkers, were studied in animals. The histopathological analysis and radiographic examination of joints were also performed. CRE, BC and TC treatment significantly restored the arthritic index, histopathology and body weight changes. The concentration of C-reactive protein, rheumatoid factor and other liver function parameters were significantly recovered by curcuminoids formulations. The pro-inflammatory cytokines (NF-κB, COX-2, IL-6, IL-1ß, and TNF-α) gene expression was considerably (p < 0.001) downregulated, while on the other side, the anti-inflammatory genes IL-4 and IL-10 were upregulated by the use of CRE and its complexes. The concentration of antioxidant enzymes was considerably (P < 0.001) recovered by CRE, BC and TC with marked decrease in lipid peroxidation, erosion of bone, inflammation of joints and pannus formation in comparison to arthritic control animals. Therefore, it is concluded that green CRE and its cyclodextrin formulations with enhanced solubility could be considered as an applicable therapeutic choice to treat chronic polyarthritis.


Assuntos
Artrite Experimental , Camundongos , Animais , Adjuvante de Freund , Artrite Experimental/metabolismo , Extratos Vegetais/farmacologia , Extratos Vegetais/uso terapêutico , Estresse Oxidativo , Citocinas/metabolismo , Biomarcadores/metabolismo , Peso Corporal
2.
Metab Brain Dis ; 38(7): 2255-2267, 2023 10.
Artigo em Inglês | MEDLINE | ID: mdl-37458892

RESUMO

Aggression, a highly prevalent behavior among all the psychological disorders having strong association with psychiatric imbalance, neuroendocrine changes and neurological disturbances (including oxidative stress & neuroinflammation) require both pharmacological and non-pharmacological treatments. Focusing the preclinical neuroendocrine determinants of aggression, this interventional study was designed to elucidate the curative effect of antioxidants on aggression in male mice. Adult albino male mice (n = 140) randomly divided into two main treatment groups for α-lipoic acid (ALA) and silymarin with 5 subgroups (n = 10) for each curative study, namely control, disease (aggression-induced), standard (diazepam, 2.5 mg/kg), low dose (100 mg/kg) and high dose (200 mg/kg) treatment groups of selected antioxidants. Resident-intruder paradigm and levodopa (L-dopa 375 mg/kg, p.o.) induced models were used for aggression. Effect of antioxidant treatment (i.e., 21 days bid) on aggression was assessed by evaluating the changes in aggressive behavior, oxidative stress biomarkers superoxide dismutase, catalase, glutathione, nitrite and malondialdehyde (SOD, CAT, GSH, nitrite & MDA), neurotransmitters (dopamine, nor-adrenaline and serotonin), pro-inflammatory cytokines tumor necrosis factor-α and interleukin- 6 (TNF-α & IL-6) along with serum testosterone examination. This study showed potential ameliorative effect on aggressive behavior with both low (100 mg/kg) and high (200 mg/kg) doses of antioxidants (ALA & silymarin). Resident-intruder or L-dopa induced aggression in male mice was more significantly tuned with ALA treatment than silymarin via down regulating both oxidative stress and inflammatory biomarkers. ALA also exhibited notable effects in managing aggression-induced disturbances on plasma testosterone levels. In conclusion, ALA is more effective than silymarin in attenuating aggression in mice.


Assuntos
Silimarina , Ácido Tióctico , Masculino , Camundongos , Animais , Ácido Tióctico/farmacologia , Ácido Tióctico/uso terapêutico , Antioxidantes/farmacologia , Antioxidantes/uso terapêutico , Antioxidantes/metabolismo , Silimarina/farmacologia , Silimarina/uso terapêutico , Levodopa/farmacologia , Nitritos/farmacologia , Estresse Oxidativo , Glutationa/metabolismo , Agressão , Biomarcadores/metabolismo , Testosterona
3.
Metab Brain Dis ; 38(3): 1051-1066, 2023 03.
Artigo em Inglês | MEDLINE | ID: mdl-36437394

RESUMO

Parkinson's disease (PD) is slowly developing neurodegenerative disorder associated with gradual decline in cerebration and laboriousness to perform routine piece of work. PD imposed a social burden on society through higher medical cost and by loss of social productivity in current era. The available treatment options are expensive and associated with serious adverse effect after long term use. Therefore, there is a critical clinical need to develop alternative pharmacotherapies from natural sources to prevent and cure the pathological hall marks of PD with minimal cost. Our study aimed to scrutinize the antiparkinsonian potential of curcuminoids-rich extract and its binary and ternary inclusion complexes. In healthy rats, 1 mg/kg haloperidol daily intraperitoneally, for 3 weeks was used to provoke Parkinsonism like symptoms except control group. Curcuminoids rich extract, binary and ternary inclusion complexes formulations 15-30 mg/kg, L-dopa and carbidopa (100 + 25 mg/kg) were orally administered on each day for 3 weeks. Biochemical, histopathological and RT-qPCR analyses were conducted after neurobehavioral observations. Findings of current study indicated that all curcuminoids formulations markedly mitigated the behavioral abnormalities, recovered the level of antioxidant enzymes, acetylcholinesterase inhibitory activity and neurotransmitters. Histological analysis revealed that curcuminoids supplements stabilized the neuronal loss, pigmentation and Lewy bodies' formation. The mRNA expressions of neuro-inflammatory and specific PD pathological biomarkers were downregulated by treatment with curcuminoids formulations. Therefore, it is suggested that these curcuminoids rich extract, binary and ternary supplements should be considered as promising therapeutic agents in development of modern anti-Parkinson's disease medications.


Assuntos
Diarileptanoides , Doença de Parkinson , Ratos , Animais , Diarileptanoides/uso terapêutico , Haloperidol/farmacologia , Haloperidol/uso terapêutico , Acetilcolinesterase , Modelos Animais de Doenças , Doença de Parkinson/tratamento farmacológico
4.
Metab Brain Dis ; 38(2): 483-505, 2023 Feb.
Artigo em Inglês | MEDLINE | ID: mdl-35344129

RESUMO

Mangifera indica L., also known as mango, is a tropical fruit that belongs to the Anacardiaceae family and is prized for its juiciness, unique flavour, and worldwide popularity. The current study aimed to probe into antidepressant power (ADP) of MIS in animals and confirmation of ADP with in silico induced-fit molecular docking. The depression model was prepared by exposing mice to various stressors from 9:00 am to 2:00 pm during 42 days study period. MIS extract and fluoxetine were given daily for 30 min before exposing animals to stressors. ADP was evaluated by various behavioural tests and biochemical analysis. Results showed increased physical activity in mice under behavioural tests, plasma nitrite and malondialdehyde (MDA) levels and monoamine oxidase A (MAO-A) activity decreased dose-dependently in MIS treated mice and superoxide dismutases (SOD) levels increased in treated groups as compared to disease control. With the peculiar behaviour and significant interactions of the functional residues of target proteins with selected ligands along with the best absorption, distribution, metabolism, excretion, and toxicity (ADMET) properties, it is concluded that catechin could be the best MAO-A inhibitor at a binding energy of -8.85 kcal/mol, and two hydrogen bonds were generated with Cys406 (A) and Gly443 (A) residues of the active binding site of MAO-A enzyme. While catechin at -6.86 kcal/mol generated three hydrogen bonds with Ala263 (A) and Gly434 (A) residues of the active site of monoamine oxidase B (MAO-B) enzyme and stabilized the best conformation. Therefore, it is highly recommended to test the selected lead-like compound catechin in the laboratory with biological system analysis to confirm its activity as MAO-A and MAO-B inhibitors so it can be declared as one of the novel therapeutic options with anti-depressant activity. Our findings concluded that M. indica seeds could be a significant and alternative anti-depressant therapy.


Assuntos
Catequina , Mangifera , Camundongos , Animais , Antidepressivos/farmacologia , Antidepressivos/uso terapêutico , Antidepressivos/química , Mangifera/metabolismo , Extratos Vegetais/farmacologia , Extratos Vegetais/uso terapêutico , Extratos Vegetais/química , Simulação de Acoplamento Molecular , Catequina/análise , Inibidores da Monoaminoxidase/farmacologia , Monoaminoxidase/metabolismo , Sementes/química , Compostos Fitoquímicos/farmacologia , Compostos Fitoquímicos/uso terapêutico
5.
Molecules ; 27(21)2022 Oct 23.
Artigo em Inglês | MEDLINE | ID: mdl-36364001

RESUMO

Polydatin or 3-O-ß-d-resveratrol-glucopyranoside (PD), a stilbenoid component of Polygonum cuspicadum (Polygonaceae), has a variety of biological roles. In traditional Chinese medicine, P. cuspicadum extracts are used for the treatment of infections, inflammation, and cardiovascular disorders. Polydatin possesses a broad range of biological activities including antioxidant, anti-inflammatory, anticancer, and hepatoprotective, neuroprotective, and immunostimulatory effects. Currently, a major proportion of the population is victimized with cervical lung cancer, ovarian cancer and breast cancer. PD has been recognized as a potent anticancer agent. PD could effectively inhibit the migration and proliferation of ovarian cancer cells, as well as the expression of the PI3K protein. The malignancy of lung cancer cells was reduced after PD treatments via targeting caspase 3, arresting cancer cells at the S phase and inhibiting NLRP3 inflammasome by downregulation of the NF-κB pathway. This ceases cell cycle, inhibits VEGF, and counteracts ROS in breast cancer. It also prevents cervical cancer by regulating epithelial-to-mesenchymal transition (EMT), apoptosis, and the C-Myc gene. The objective of this review is thus to unveil the polydatin anticancer potential for the treatment of various tumors, as well as to examine the mechanisms of action of this compound.


Assuntos
Neoplasias da Mama , Estilbenos , Humanos , Feminino , Transdução de Sinais , Estilbenos/farmacologia , Glucosídeos/farmacologia
6.
J Food Biochem ; 46(12): e14389, 2022 12.
Artigo em Inglês | MEDLINE | ID: mdl-36121315

RESUMO

Berberine-rich extract (BRE) prepared from Berberis lycium root bark using green extraction approach and its marker compound berberine has a broad spectrum of clinical applications. Berberine's potential pharmacological effects include anticancer, antidiarrheal, antidiabetic, antimicrobial and anti-inflammatory activities. In current work, BRE and berberine were evaluated for their therapeutic prospects in inflammation models. The comparative effect of BRE and berberine against inflammation was determined through in vitro chemiluminescence technique. The in vivo anti-inflammatory evaluation of BRE and berberine (25, 75, and 125 mg/kg) compared to diclofenac (10 mg/kg) was performed in carrageenan and formaldehyde-induced inflammation in Wistar rats. Histopathological and biochemical studies were conducted to find the comparative anti-inflammatory potential of BRE and berberine on pathological hallmarks induced by formaldehyde. Moreover, the modulatory effects on inflammatory biomarkers were also investigated through qPCR. ELISA (enzyme-linked immunoassay test assay) was performed to investigate the expression of pathological protein biomarkers like TNF-α and IL-6 and levels of antioxidant enzymes were estimated in liver homogenates. Both BRE and berberine markedly (p < .001) reduced paw diameter and inflammation in carrageenan and formaldehyde-induced inflammation. The levels of antioxidant enzymes were recovered (p < .001) by BRE and berberine treatments, and compared to the formaldehyde-treated inflammation model. Both BRE and berberine remarkably downregulated the mRNA and protein expression of inflammatory biomarkers. BRE similar to berberine mitigated the level of antioxidant enzymes in liver homogenate. The undertaken study suggests that BRE, a natural, green, and therapeutically bioequivalent to berberine could be used as an economical phytomedicine in the treatment of inflammatory disorders. PRACTICAL APPLICATIONS: Anti-inflammatory drugs like NSAIDS are associated with serious adverse effects like gastrointestinal ulcer, worsening of preexisting cardiovascular disorders, and renal failure. Therefore, there is a constant demand to develop novel, inexpensive therapeutic strategies to treat the inflammatory disorder with the least harmful effects. Pure phytochemicals with anti-inflammatory potential are costly and hard to isolate, therefore green microwave-assisted extraction technique is developed to get the rich bioequivalent extract. Berberis lycium a medicinal plant with berberine as a major bioactive constituent, has wide acceptance in traditionally used medicine and as food. Pharmacological studies revealed its hepatoprotective, anticancer, antidiabetic, and antihypertensive activities. BRE was prepared by green microwave-assisted extraction and enrichment by resin column to get a higher yield of berberine. The comparative anti-inflammatory effect of BRE and berberine was determined by in vitro and in vivo studies. Results obtained from this experimental work contribute beneficial guidance that reinforces the use of the BRE to treat inflammatory disorders.


Assuntos
Berberina , Extratos Vegetais , Ratos , Animais , Carragenina/efeitos adversos , Extratos Vegetais/química , Antioxidantes/química , Berberina/farmacologia , Ratos Wistar , Anti-Inflamatórios/farmacologia , Inflamação/tratamento farmacológico , Hipoglicemiantes/farmacologia , Formaldeído
7.
Curr Pharm Des ; 28(19): 1523-1542, 2022.
Artigo em Inglês | MEDLINE | ID: mdl-35762558

RESUMO

Obesity-associated diabetes mellitus, a chronic metabolic affliction accounting for 90% of all diabetic patients, has been affecting humanity extremely badly and escalating the risk of developing other serious disorders. It is observed that 0.4 billion people globally have diabetes, whose major cause is obesity. Currently, innumerable synthetic drugs like alogliptin and rosiglitazone are being used to get through diabetes, but they have certain complications, restrictions with severe side effects, and toxicity issues. Recently, the frequency of plant-derived phytochemicals as advantageous substitutes against diabesity is increasing progressively due to their unparalleled benefit of producing less side effects and toxicity. Of these phytochemicals, dietary polyphenols have been accepted as potent agents against the dual sword "diabesity". These polyphenols target certain genes and molecular pathways through dual mechanisms such as adiponectin upregulation, cannabinoid receptor antagonism, free fatty acid oxidation, ghrelin antagonism, glucocorticoid inhibition, sodium-glucose cotransporter inhibition, oxidative stress and inflammation inhibition etc. which sequentially help to combat both diabetes and obesity. In this review, we have summarized the most beneficial natural polyphenols along with their complex molecular pathways during diabesity.


Assuntos
Diabetes Mellitus Tipo 2 , Diabetes Mellitus , Diabetes Mellitus/tratamento farmacológico , Diabetes Mellitus Tipo 2/tratamento farmacológico , Humanos , Obesidade/metabolismo , Polifenóis/farmacologia , Polifenóis/uso terapêutico
8.
Environ Sci Pollut Res Int ; 29(45): 67981-67996, 2022 Sep.
Artigo em Inglês | MEDLINE | ID: mdl-35525893

RESUMO

Alzheimer's disease (AD) is a slowly progressive brain degenerative disorder which gradually impairs memory, thinking, and ability to perform easy routine tasks. This degenerative disorder mainly targets the elderly people and has imposed an endemic burden on society. Hence, there is a crucial need to investigate the efficacious herbal pharmacotherapies that can effectively mitigate and prevent the pathological hallmarks of AD. The current study aims to explore the potential efficacy of curcuminoid-rich extract (CRE) and its ternary complex (TC). Experimental rodents were administered with AlCl3 (300 mg/kg) to induce AD and treated with rivastigmine, curcuminoid crude extract, CRE, and TC orally for three consecutive weeks. Neurobehavioral, biochemical, and histopathological studies were performed from the last week of the study period. The mRNA expression of different pathological biomarkers was estimated by RT-qPCR analysis. The results of the study suggested that CRE and TC significantly improved the behavioral, biochemical parameters and acetylcholinesterase inhibitory activity in treatment groups. Histological analysis was also carried out indicating that the neurodegenerative changes and neuronal loss were stabilized by CRE and TC supplementation. CRE and TC supplementation remarkably downregulated the interleukin-1α, tumor necrosis factor-α, interleukin-1ß, acetylcholinesterase, and ß-secretase pathological gene expression. Hence, it was concluded that CRE and TC may act as promising candidates in the prevention of AD via numerous underlying signaling pathways.


Assuntos
Doença de Alzheimer , Fármacos Neuroprotetores , Acetilcolinesterase/metabolismo , Cloreto de Alumínio/toxicidade , Doença de Alzheimer/tratamento farmacológico , Secretases da Proteína Precursora do Amiloide/metabolismo , Secretases da Proteína Precursora do Amiloide/uso terapêutico , Animais , Biomarcadores/metabolismo , Misturas Complexas/uso terapêutico , Misturas Complexas/toxicidade , Diarileptanoides/uso terapêutico , Diarileptanoides/toxicidade , Modelos Animais de Doenças , Humanos , Interleucina-1alfa/uso terapêutico , Interleucina-1alfa/toxicidade , Interleucina-1beta/metabolismo , Fármacos Neuroprotetores/uso terapêutico , RNA Mensageiro , Rivastigmina/uso terapêutico , Rivastigmina/toxicidade , Fator de Necrose Tumoral alfa/metabolismo
9.
Inflammopharmacology ; 30(2): 579-597, 2022 Apr.
Artigo em Inglês | MEDLINE | ID: mdl-35218463

RESUMO

Sarcococca saligna plant is commonly used as traditional therapy for arthritis especially in Asian countries. The current study is designed to explore the anti-arthritic potential of S. saligna aqueous methanolic extract (SSME). Preliminary proximate study and HPLC analysis were performed to investigate the phytochemical characterization and quality control. The safety of the SSME was evaluated by performing an acute oral toxicity study (OECD guidelines 425). The anti-arthritic potential of SSME was explored by in vivo formaldehyde-induced arthritis model. The antiarthritic effect of the SSME was determined through paw diameter, arthritic index, body weight, biochemical and haematological parameters. Radiographic and histopathological studies were also carried out to evaluate the results. qRT-PCR was performed to determine the upregulation and downregulation of anti- and pro-inflammatory cytokines in rats while ELISA was done to determine the concentration of HSP-70, IL-6 and TNF-α in the serum. Results of acute oral toxicity showed no abnormality and mortality. There was no noticeable change in haematological and biochemical parameters. Histopathological examination exhibited the normal structure of vital organs. So, SSME might be safe at a 2000 mg/kg dose, proposing that LD50 was higher than 2000 mg/kg body weight. Gallic acid, catechin, hydroxyl benzoic acid, sinapic acid, caffeic acid, ferulic acid and p-cumaric acid were identified by HPLC. The outcomes of in vivo formaldehyde-induced arthritic model showed that SSME significantly reduced paw inflammation and arthritic index and improved haematological and biochemical parameters. Moreover, the SSME influentially down-regulated the gene expression of IL-1ß, IL-6, COX-2, PGE2, TNF-α and NF-κB, and up-regulated the expression of IL-4, and IL-10. The results of the undertaken study suggest that S. saligna have strong anti-arthritic activity supporting its conventional application as the remedy of rheumatoid arthritis.


Assuntos
Artrite Experimental , Buxaceae , Animais , Anti-Inflamatórios/uso terapêutico , Artrite Experimental/induzido quimicamente , Artrite Experimental/tratamento farmacológico , Artrite Experimental/metabolismo , Biomarcadores/metabolismo , Citocinas/metabolismo , Formaldeído , Extratos Vegetais/uso terapêutico , Ratos , Ratos Wistar
10.
Comb Chem High Throughput Screen ; 25(7): 1181-1186, 2022.
Artigo em Inglês | MEDLINE | ID: mdl-34391377

RESUMO

Oxalis corniculata (Oxalidaceae) is a small decumbent and delicate appearing medicinal herb flourishing in warm temperate and tropical domains such as Pakistan and India. Main bioactive chemical constituents of Oxalis plant include several alkaloids, flavonoids, terpenoids, cardiac glycosides, saponins, and phlobatannins, along with steroids. Due to its polyphenolic, glycosides and flavonoid profile, it is proved to be protective in numerous ailments and exhibit various biological activities such as anti-fungal, anti-cancer, anti-oxidant, antibacterial, anti-diabetic, and cardioprotective. Moreover, bioactive phytochemicals from this plant possess significant wound healing potential. Our current effort intends to emphasize on the immense significance of this plant species, which have not been the subject matter of clinical trials and effective pharmacological studies, even though its favored usage has been stated. This review proposes that Oxalis corniculata possess a potential for the cure of various diseases. However, further researches on isolation and characterization of bioactive compounds along with pre-clinical trials are compulsory to figure out its pharmacological applications.


Assuntos
Oxalidaceae , Plantas Medicinais , Antibacterianos/farmacologia , Antioxidantes , Flavonoides/farmacologia , Oxalidaceae/química , Compostos Fitoquímicos , Extratos Vegetais/química , Plantas Medicinais/química
11.
Anticancer Agents Med Chem ; 22(1): 40-52, 2022.
Artigo em Inglês | MEDLINE | ID: mdl-33622231

RESUMO

Radiations are an efficient treatment modality in cancer therapy. Besides the treatment effects of radiations, the ionizing radiations interact with biological systems and generate reactive oxygen species that interfere with the normal cellular process. Previous investigations have been conducted only on few synthetic radioprotectors, mainly owing to some limiting effects. The nutraceuticals act as efficient radioprotectors to protect the tissues from the deleterious effects of radiation. The main radioprotection mechanism of nutraceuticals is the scavenging of free radicals while other strategies involve modulation of signaling transduction pathways like MAPK (JNK, ERK1/2, ERK5, and P38), NF-kB, cytokines, and their protein regulatory gene expression. The current review is focused on the radioprotective effects of nutraceuticals including vitamin E, -C, organosulphur compounds, phenylpropanoids, and polysaccharides. These natural entities protect against radiation-induced DNA damage. The review mainly entails the antioxidant perspective and radioprotective molecular mechanism of nutraceuticals, DNA repair pathway, anti-inflammation, immunomodulatory effects and regeneration of hematopoietic cells.


Assuntos
Antineoplásicos/uso terapêutico , Antioxidantes/uso terapêutico , Suplementos Nutricionais , Neoplasias/prevenção & controle , Animais , Humanos , Radiação Ionizante
12.
Front Biosci (Landmark Ed) ; 26(11): 1031-1051, 2021 11 30.
Artigo em Inglês | MEDLINE | ID: mdl-34856751

RESUMO

Background: Parkinson's disease (PD) is associated with progressive neuronal damage and dysfunction. Oxidative stress helps to regulate neurodegenerative and neuronal dysfunction. Natural compounds could attenuate oxidative stress in a variety of neurological disorders. B. juncea is a rich source of antioxidants. The present study aimed to evaluate the therapeutic potential of B. juncea leaves for the treatment of PD by applying behavioral, in vivo and in silico studies. For in vivo studies rats were divided into six groups (n = 6). Group-I served as normal control (vehicle control). Group-II was disease control (haloperidol 1 mg/kg). Group-III was kept as a standard group (L-Dopa 100 mg/kg + carbidopa 25 mg/kg). Groups (IV-VI) were the treatment groups, receiving extract at 200-, 400- and 600 mg/kg doses respectively, for 21 days orally. Results: In vivo study results showed that the extract was found to improve muscles strength, motor coordination, and balance in PD. These behavioral outcomes were consistent with the recovery of endogenous antioxidant defence in biochemical analysis which was further corroborated with histopathological ameliorations. Dopamine levels increased and monoamine oxidase B (MAO-B) levels decreased dose-dependently in the brain during the study. Herein, we performed molecular docking analysis of the proposed extracted phytochemicals has explained that four putative phytochemicals (sinapic acid, rutin, ferulic acid, and caffeic acid) have presented very good results in terms of protein-ligand binding interactions as well as absorption, distribution, metabolism, excretion & toxicity (ADMET) profile estimations. Conclusion: The undertaken study concluded the anti-Parkinson activity of B. juncea and further suggests developments on its isolated compounds in PD therapeutics.


Assuntos
Levodopa , Mostardeira , Animais , Simulação de Acoplamento Molecular , Compostos Fitoquímicos/farmacologia , Extratos Vegetais/farmacologia , Ratos
13.
Phytother Res ; 35(12): 6530-6551, 2021 Dec.
Artigo em Inglês | MEDLINE | ID: mdl-34396612

RESUMO

The flare-up in severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2) that emerged in December 2019 in Wuhan, China, and spread expeditiously worldwide has become a health challenge globally. The rapid transmission, absence of anti-SARS-CoV-2 drugs, and inexistence of vaccine are further exacerbating the situation. Several drugs, including chloroquine, remdesivir, and favipiravir, are presently undergoing clinical investigation to further scrutinize their effectiveness and validity in the management of COVID-19. Natural products (NPs) in general, and plants constituents specifically, are unique sources for various effective and novel drugs. Immunostimulants, including vitamins, iron, zinc, chrysin, caffeic acid, and gallic acid, act as potent weapons against COVID-19 by reinvigorating the defensive mechanisms of the immune system. Immunity boosters prevent COVID-19 by stimulating the proliferation of T-cells, B-cells, and neutrophils, neutralizing the free radicals, inhibiting the immunosuppressive agents, and promoting cytokine production. Presently, antiviral therapy includes several lead compounds, such as baicalin, glycyrrhizin, theaflavin, and herbacetin, all of which seem to act against SARS-CoV-2 via particular targets, such as blocking virus entry, attachment to host cell receptor, inhibiting viral replication, and assembly and release.


Assuntos
Antivirais , COVID-19 , Antivirais/farmacologia , Humanos , SARS-CoV-2 , Replicação Viral , Vitaminas
14.
Pak J Pharm Sci ; 34(1(Special)): 473-479, 2021 Jan.
Artigo em Inglês | MEDLINE | ID: mdl-34275796

RESUMO

Herbal medicines are gaining importance due to more advantages and less toxic effects. Withania coagulans is natural plant that possesses multiple activities. Its main constituents are withaferin and withanolide. The purpose of present study is to identify main constituent of Withania coagulans and preparation of extract loaded micro emulsions. Withania coagulans fruit extract in methanol/chloroform (1:1) was collected in semisolid form and LCMS was done to identify active compound, and then micro emulsions were prepared using Tween 80: Transcutol (1:1) Frankincense oil, and water to enhance its stability for topical application. Five formulations were prepared by Pseudo ternary phase diagram and evaluated for pH, conductivity, viscosity, drug contents, particle size analysis, and polydispersity. Withania coagulans extract was evaluated for anti-bacterial activity against (Staphylococcus aureus, E. coli, and S. typhi) and anti-fungal activity against (Candida albicans and Aspergillus niger). Anti-inflammatory activity was checked for both extract and Extract based micro emulsion. Among all five formulations F5 shows best physiochemical properties with small globule size, good stability and high anti-inflammatory activity. Based on these results it was concluded that Withania coagulans extract loaded micro emulsions can be used for topical application with promising anti-inflammatory activities. Data for in-vivo studies for checking the topical effect of Withania coagulans is provided elsewhere.


Assuntos
Anti-Infecciosos/farmacologia , Anti-Inflamatórios/farmacologia , Extratos Vegetais/farmacologia , Withania , Administração Tópica , Aspergillus niger/efeitos dos fármacos , Candida albicans/efeitos dos fármacos , Emulsões , Escherichia coli/efeitos dos fármacos , Salmonella typhi/efeitos dos fármacos , Staphylococcus aureus/efeitos dos fármacos , Vitanolídeos
15.
Pak J Pharm Sci ; 34(2(Supplementary)): 693-698, 2021 Mar.
Artigo em Inglês | MEDLINE | ID: mdl-34275804

RESUMO

The study was carried out to evaluate the hepatoprotective potential of aqueous methanolic extract of Heliotropium strigosum (HSME) against paracetamol induced hepatotoxicity in Swiss albino mice. The plant powder (1.5Kg) was macerated in aqueous methanol (30:70) for 7 days. The extract was evaluated for the presence of different phytochemicals and High-performance liquid chromatography (HPLC) analysis. HSME was orally administered to mice at 125, 250 and 500mg/kg for 8 days followed by paracetamol intoxication (500mg/kg orally) on the 8th day using silymarin as standard control. All the therapy was administered by oral gavage. The liver biochemical parameters and histopathological evaluation were carried out to assess changes in liver function and histology. HPLC analysis confirmed the presence of quercetin, kaempferol, and other phenolic compounds. Treatment with the extract resulted in notable (p<0.05) reduction in liver parameters in dose dependent manner. The action of HSME 500mg/kg dose was comparable to silymarin. The effect of HSME against paracetamol induced hepatotoxicity was demonstrated by protective changes in the liver histopathological which proved the traditional uses of the plant.


Assuntos
Acetaminofen/antagonistas & inibidores , Doença Hepática Induzida por Substâncias e Drogas/prevenção & controle , Heliotropium/química , Extratos Vegetais/farmacologia , Acetaminofen/toxicidade , Animais , Doença Hepática Induzida por Substâncias e Drogas/tratamento farmacológico , Doença Hepática Induzida por Substâncias e Drogas/patologia , Cromatografia Líquida de Alta Pressão , Feminino , Fígado/efeitos dos fármacos , Fígado/patologia , Masculino , Metanol , Camundongos , Extratos Vegetais/uso terapêutico , Silimarina/farmacologia , Silimarina/uso terapêutico
16.
Metab Brain Dis ; 36(6): 1231-1251, 2021 08.
Artigo em Inglês | MEDLINE | ID: mdl-33759084

RESUMO

Cucurbita pepo is used as a vegetable in Pakistan and its seeds are also rich in tocopherol. Data showed the pivotal role of tocopherol in the treatment of Parkinson's disease (PD). The current study was designed to probe into the antiparkinson activity of methanolic extract of C. pepo (MECP) seeds in the haloperidol-induced Parkinson rat model. Behavioral studies showed improvement in motor functions. The increase in catalase, superoxide dismutase, glutathione levels whereas the decreases in the malondialdehyde and nitrite levels were noted in a dose-dependent manner. Acetylcholine-esterase (AchE) activity was increased. Molecular docking results revealed significant binding interaction of selected phytoconstituents within an active site of target protein AchE (PDB ID: 4EY7). Furthermore, α-synuclein was up regulated with down regulation of TNF-α and IL-1ß in the qRT-PCR study. Subsequently, ADMET results on the basis of structure to activity predictions in terms of pharmacokinetics and toxicity estimations show that selected phytochemicals exhibited moderately acceptable properties. These properties add knowledge towards the structural features which could improve the bioavailability of selected phytochemicals before moving towards the initial phase of the drug development. Our integrated drug discovery scheme concluded that C. pepo seeds could ameliorate symptoms of PD and may prove a lead remedy for the treatment of PD.


Assuntos
Antiparkinsonianos/farmacologia , Cucurbita/química , Doença de Parkinson/tratamento farmacológico , Extratos Vegetais/farmacologia , Animais , Antioxidantes/farmacologia , Cucurbita/metabolismo , Malondialdeído/metabolismo , Ratos , Superóxido Dismutase/metabolismo
17.
Metab Brain Dis ; 36(5): 889-900, 2021 06.
Artigo em Inglês | MEDLINE | ID: mdl-33570733

RESUMO

Alzheimer's disease affects daily routine due to loss of memory and decline in cognition. In vitro data showed acetylcholine esterase inhibition activity of Malva neglecta but no in vivo evidence is available. The current study aims to investigate the anti-Alzheimer's activity of Malva neglecta methanolic extract in the AlCl3-induced Alzheimer disease rats' model. Thirty Wistar rats were divided into six groups and respective doses were given orally for 21 days. Behavioural observations were recorded and biochemical analysis was performed on brain homogenate. Improvement in memory and cognition was noted in treated rats as compared to disease control. A dose-dependent decrease (0.530 ± 0.009 at 200 mg/kg, 0.212 ± 0.007 at 400 mg/kg, 0.173 ± 0.005 at 600 mg/kg) in AChE activity was noted in the treatment groups with reference to disease control value (1.572 ± 0.013). This decrease in AChE activity is linked with an increase in acetylcholine in the brain which plays a key role in retaining memory. Oxidative stress biomarkers; GSH (66.77 ± 0.01 at 600 mg/kg), SOD (26.60 ± 0.10 at 600 mg/kg), CAT (21.46 ± 0.01 at 600 mg/kg) levels were increased with a decrease in MDA (103.33 ±0.49 at 600 mg/kg) level in a dose-dependently manner in the treatment groups as compared to disease control respective values. It is concluded that Malva neglecta could ameliorate Alzheimer's symptoms possibly by decreasing AChE activity and oxidative stress.


Assuntos
Doença de Alzheimer/metabolismo , Colinesterases/metabolismo , Fármacos Neuroprotetores/farmacologia , Estresse Oxidativo/efeitos dos fármacos , Extratos Vegetais/farmacologia , Doença de Alzheimer/tratamento farmacológico , Animais , Cognição/efeitos dos fármacos , Regulação para Baixo/efeitos dos fármacos , Feminino , Glutationa/metabolismo , Masculino , Malva , Aprendizagem em Labirinto/efeitos dos fármacos , Fármacos Neuroprotetores/uso terapêutico , Estresse Oxidativo/fisiologia , Extratos Vegetais/uso terapêutico , Ratos , Ratos Wistar , Superóxido Dismutase/metabolismo
18.
Microsc Res Tech ; 84(4): 608-617, 2021 Apr.
Artigo em Inglês | MEDLINE | ID: mdl-33064896

RESUMO

The present study aimed to investigate the palyno-morphological features of species of family Vitaceae from Pakistan. A total of nine species, belonging to four genera were collected, pressed, identified, and then analyzed microscopically. Both quantitative and qualitative characters of the pollen grains were recorded including polar and equatorial diameter, P/E ratio, number of colpi and pores, exine thickness and shapes of the pollen in both polar and equatorial view, and exine sculpturing using Leica microscope fitted with camera Meiji Infinity 1 and then analyzed statistically using software IBM SPSS Statistics 20. The results of the present study demonstrated the variations in polar and equatorial diameter, exine thickness, P/E ratio, pollen shape, and exine sculpturing of the studied species and highlighted the significance of pollen morphology as an identification tool. The present study may contribute to better understand the classification at genus level, which will support the future phylogenetic characterization of the family.


Assuntos
Vitaceae , Microscopia Eletrônica de Varredura , Paquistão , Filogenia , Pólen
19.
Mini Rev Med Chem ; 21(18): 2747-2763, 2021.
Artigo em Inglês | MEDLINE | ID: mdl-32646359

RESUMO

Nature has always proved to be a significant reservoir of bioactive scaffolds that have been used for the discovery of drugs since times. Medicinal plants continue to be a solid niche for biologically active and therapeutically effective chemical entities, opening up new avenues for the successful treatment of several human diseases. The contribution of plant-derived compounds to drug discovery, either in their original or in the semi-synthetic derivative form, extends far back in time. This review aims to focus on the sources, biological, and pharmacological profile of a pharmacologically active plant-derived coumarin, osthole, which is an important component of numerous remedial plants such as Cnidium monnieri. Several studies have revealed that osthole possess pharmacological properties such as anticancer, antioxidant, anti-hyperglycemic, neuroprotective, and antiplatelet. Osthole has been reported to regulate various signaling pathways, which in turn modulate several apoptosis-related proteins, cell cycle regulators, protein kinases, transcriptional factors, cytokines, and growth receptors affiliated with inflammation, proliferation and several other ailments. Osthole is known to halt proliferation and metastasis of cancerous cells by arresting the cell cycle and inducing apoptosis. The data in this review paper supports the pharmacological potential of osthole but further experimentation, biosafety profiling and synergistic effects of this compound need to be focused by the researchers to understand the full spectrum of pharmacological potential of this therapeutically potent compound.


Assuntos
Anti-Inflamatórios , Antineoplásicos , Antioxidantes , Cumarínicos/farmacologia , Animais , Anti-Inflamatórios/farmacologia , Antineoplásicos/farmacologia , Antioxidantes/farmacologia , Produtos Biológicos/farmacologia , Cnidium/química , Humanos
20.
Infect Drug Resist ; 13: 4367-4378, 2020.
Artigo em Inglês | MEDLINE | ID: mdl-33304102

RESUMO

BACKGROUND AND AIM: Bacillus species are widely distributed microorganisms in nature that are responsible for outbreaks of food poisoning and a common cause of food spoilage. This study aimed to isolate and identify foodborne Bacillus species from meat and to determine the antimicrobial activities of commercial essential oils and spices powder extracted from certain medicinal plants. METHODS: Sixty meat samples were collected in Assiut city and subdivided into raw meat and processed meat. Bacillus spp were isolated and identified according to their cultural characters, biochemical reactions, serological typing, and 16S rRNA gene sequencing. The antibacterial activity of essential oils and spices powder was measured by using well-diffusion and microbial count techniques. RESULTS: The prevalence of Bacillus spp. in the examined raw meat samples and processed meat samples was 13.34%, and 26.67%, respectively. There was a marked decrease in the total Bacillus species count after treatment of minced beef with essential oils and spices powder compared to the untreated one. Black seed oil was the most potent antibacterial essential oil among the tested oils present in this study. CONCLUSION: Essential oils and spices powder of certain medicinal plants (cumin: Cuminum cyminum, black seeds: Nigella sativa, cloves: Syzygium aromaicum, cinnamon: Cinnamomum zeylanicum, and Marjoram: Origanum majorana) have a potential in vitro antimicrobial activity against Bacillus spp. Furthermore, Nigella sativa oil exhibited the most potent antibacterial activity against Bacillus spp.

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