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1.
PLoS One ; 19(3): e0298986, 2024.
Artigo em Inglês | MEDLINE | ID: mdl-38551975

RESUMO

Syzygium heyneanum is a valuable source of flavonoids and phenols, known for their antioxidant and neuroprotective properties. This research aimed to explore the potential of Syzygium heyneanum ethanol extract (SHE) in countering Parkinson's disease. The presence of phenols and flavonoids results in SHE displaying an IC50 value of 42.13 when assessed in the DPPH scavenging assay. Rats' vital organs (lungs, heart, spleen, liver, and kidney) histopathology reveals little or almost no harmful effect. The study hypothesized that SHE possesses antioxidants that could mitigate Parkinson's symptoms by influencing α-synuclein, acetylcholinesterase (AChE), TNF-α, and IL-1ß. Both in silico and in vivo investigations were conducted. The Parkinson's rat model was established using paraquat (1 mg/kg, i.p.), with rats divided into control, disease control, standard, and SHE-treated groups (150, 300, and 600 mg/kg) for 21 days. According to the ELISA statistics, the SHE treated group had lowers levels of IL-6 and TNF-α than the disease control group, which is a sign of neuroprotection. Behavioral and biochemical assessments were performed, alongside mRNA expression analyses using RT-PCR to assess SHE's impact on α-synuclein, AChE, TNF-α, and interleukins in brain homogenates. Behavioral observations demonstrated dose-dependent improvements in rats treated with SHE (600 > 300 > 150 mg/kg). Antioxidant enzyme levels (catalase, superoxide dismutase, glutathione) were significantly restored, particularly at a high dose, with notable reduction in malondialdehyde. The high dose of SHE notably lowered acetylcholinesterase levels. qRT-PCR results indicated reduced mRNA expression of IL-1ß, α-synuclein, TNF-α, and AChE in SHE-treated groups compared to disease controls, suggesting neuroprotection. In conclusion, this study highlights Syzygium heyneanum potential to alleviate Parkinson's disease symptoms through its antioxidant and modulatory effects on relevant biomarkers.


Assuntos
Doença de Parkinson , Syzygium , Humanos , Ratos , Animais , Antioxidantes/farmacologia , Antioxidantes/uso terapêutico , Antioxidantes/metabolismo , Paraquat/toxicidade , Doença de Parkinson/tratamento farmacológico , alfa-Sinucleína/genética , alfa-Sinucleína/metabolismo , Syzygium/química , Acetilcolinesterase/metabolismo , China , Fator de Necrose Tumoral alfa/metabolismo , Roedores , Etnicidade , Extratos Vegetais/farmacologia , Extratos Vegetais/uso terapêutico , Extratos Vegetais/química , Fenóis/farmacologia , Flavonoides/farmacologia , RNA Mensageiro/metabolismo , Estresse Oxidativo
2.
Front Pharmacol ; 14: 1243742, 2023.
Artigo em Inglês | MEDLINE | ID: mdl-38239191

RESUMO

Panicum antidotale has traditionally been used as a poultice to alleviate local inflammation and painful diseases. This study aimed to evaluate the anti-inflammatory, wound-healing, analgesic, and antipyretic potential of its ethanol extract (PAAPEE) in vivo for the first time. In vitro antioxidant assays of Panicum antidotale using a 2,2-diphenyl-1-picrylhydrazyl assay revealed that it showed IC50 of 62.50 ± 6.85 µg/mL in contrast to standard, ascorbic acid, that showed IC50 of 85.51 ± 0.38 µg/mL. Administration of PAAPEE at a dose of 500 mg/kg (PAAPEE-500) displayed 78.44% and 75.13% inhibition of paw edema in carrageenen and histamine-induced edema models. respectively, 6 h post-treatment compared to that of the untreated group. Furthermore, it showed 68.78% inhibition of Freund's complete adjuvant-induced edema 21 days after treatment. It reduced the animal's rectal temperature in the yeast-induced fever model to 99.45 during the fourth h post-treatment. It significantly inhibited abnormal writhing by 44% in the acetic acid-induced pain model. PAE-500 also showed enhancement in wound closure by 72.52% with respect to that of the untreated group on the 10th day post-treatment using the excision healing of wound model. Histopathological examination of skin samples confirmed this improvement, showing enhanced tissue architecture with minimal infiltration of inflammatory cells. High-performance liquid chromatography (HPLC) of PAAPEE revealed the presence of quercetin, gallic, p-coumaric, benzoic, chlorogenic, syringic, ferulic, cinnamic, and sinapic acids. Molecular docking of 5-lipoxygenase and glycogen synthase kinase-3 ß protein indicated their potential interaction within the active sites of both enzymes. Thus, P. antidotale serves as an effective natural wound-healing, anti-inflammatory, analgesic, and antipyretic agent.

3.
Molecules ; 27(17)2022 Aug 26.
Artigo em Inglês | MEDLINE | ID: mdl-36080247

RESUMO

Combretaceae, an immense family involving species (500) or genera (20), originates in tropical and subtropical regions. This family has evinced medicinal values such as anti-leishmanial, cytotoxic, antibacterial, antidiabetic, antiprotozoal, and antifungal properties. Conocarpus lancifolius (C. lancifolius) methanol extract (CLM) was prepared, then compound isolation performed by open column chromatography, and compound structure was determined by spectroscopic techniques (13C NMR, IR spectroscopy, 1H-NMR, mass spectrometry UV-visible, and 2D correlation techniques). Molecular docking studies of ligand were performed on transcriptional regulators 4EY7 and 2GV9 to observe possible interactions. Phytochemical screening revealed the presence of secondary metabolites including steroids, cardiac glycosides, saponins, anthraquinones, and flavonoids. The isolated compound was distinguished as lancifolamide (LFD). It showed cytotoxic activity against human breast cancer, murine lymphocytic leukemia, and normal cells, human embryonic kidney cells, and rat glioma cells with IC50 values of 0.72 µg/mL, 2.01 µg/mL, 1.55 µg/mL, and 2.40 µg/mL, respectively. Although no cytotoxic activity was noticed against human colon cancer and human lung cancer, LFD showed 24.04% inhibition against BChE and 60.30% inhibition against AChE and is therefore beneficial for Alzheimer's disease (AD). AChE and LFD interact mechanistically in a way that is optimum for neurodegenerative disorders, according to molecular docking studies. Methanol and dichloromethane extract of C. lancifolius and LFD shows antibacterial and antifungal activity against antibiotic resistance Bacillus subtilis, Streptococcus mutans, Brevibacillus laterosporus, Salmonella Typhi, Candida albicans, and Cryptococcus neoformans, respectively. LFD shows antiviral activity against HSV-1 with 26% inhibition IP. The outcomes of this study support the use of LFD for cognitive disorders and highlight its underlying mechanism, targeting AChE, DNA-POL, NF-KB, and TNF-α, etc., for the first time.


Assuntos
Inibidores da Colinesterase , Combretaceae , Herpes Simples , Herpesvirus Humano 1 , Acetilcolinesterase/metabolismo , Animais , Inibidores da Colinesterase/química , Combretaceae/química , Herpesvirus Humano 1/efeitos dos fármacos , Humanos , Metanol , Camundongos , Simulação de Acoplamento Molecular , Extratos Vegetais/química , Ratos
4.
Molecules ; 27(8)2022 Apr 18.
Artigo em Inglês | MEDLINE | ID: mdl-35458792

RESUMO

Breynia distachia is a plant of genus Breynia belonging to family Phyllanthaceae. This study was conducted to isolate and examine the anti-inflammatory attributes of the roots of Breynia distachia. Methanol extract from roots were prepared by simple maceration. For phytochemical studies, isolation, purification, structure elucidation, metal analysis, total phenolic content, and solubility test were done by chromatographic and spectroscopic techniques. Anti-inflammatory activity was evaluated by cotton pallet edema model and carrageenan paw edema model, and antioxidant potential was evaluated by DPPH, FRAP, and ABTS antioxidants assays. Metal analysis of BD.Me revealed the presence of Na > Mg > K > Mn > Fe = Zn in respective order. Four phytochemicals such as gallic acid, quercetin, sinapic acid, and p-coumaric acid are found in Breynia distachia. Quercetin is present in relatively larger quantity, and shows antioxidant activity by reducing the ferric iron to ferrous iron. Novel distachionate shows high antioxidant activity in ABTS assay by reducing reactive oxygen species. Quantitative or qualitative analysis performed by HPLC indicates the ascending peaks or presence of secondary products (metabolites) respectively. Histopathology analysis of liver, spleen, heart, and kidney was done, revealing mild inflammations in spleen and liver, and no cytotoxicity in heart and kidney. Oral administration of BD.Me and ditachionate significantly inhibits the carrageenan and cotton pellet-induced paw edema in 1st and 2nd h with (ns = p > 0.05) than control. After 3rd, 4th, 5th, and 6th h, BD.Me and ditachionate showed inhibition of paw edema in a highly significant (*** = p < 0.001) manner as compared to control. In cotton-pellet edema model, distachionate shows a %inhibition of 57.3% at a dose level of 5 mg/kg. Docking values obtained from distachionate-COX-2 complex suggest a potent inhibitor evaluated for this protein. The distachionate shows effective anti-inflammatory activity. Methanol extracts of roots showed significant lipoxygenase inhibitory activity by IC50 values of 155.7 ± 0.55 and 132.9 ± 0.33 µg/mL. Data from various in vitro and in vivo models suggest that novel distachionate isolated from Breynia distachia shows strong antioxidant and anti-inflammatory activities; it should be further studied for the exploration of its medicinal potential.


Assuntos
Antioxidantes , Malpighiales , Animais , Anti-Inflamatórios/química , Antioxidantes/química , Carragenina/efeitos adversos , Ciclo-Oxigenase 2 , Citocinas , Edema/induzido quimicamente , Edema/tratamento farmacológico , Inflamação/induzido quimicamente , Inflamação/tratamento farmacológico , Ferro/efeitos adversos , Fígado , Metanol/química , Compostos Fitoquímicos/farmacologia , Extratos Vegetais/química , Quercetina/uso terapêutico , Ratos
5.
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
6.
Curr Pharm Biotechnol ; 23(5): 728-739, 2022.
Artigo em Inglês | MEDLINE | ID: mdl-34225619

RESUMO

BACKGROUND: Raphanus sativus is traditionally used as an anti-inflammatory agent. OBJECTIVES: The current study was designed to explore the in vivo anti-inflammatory and antiangiogenic properties of Raphanus sativus seeds oil. METHODS: Cold press method was used for the extraction of oil (RsSO) and was characterised by using GC-MS techniques. Three in vitro antioxidant assays (DPPH, ABTS and FRAP) were performed to explore the antioxidant potential of RsSO. Disc diffusion methods were used to study in vitro antimicrobial properties. In vivo anti-inflammatory properties were studied in both acute and chronic inflammation models. In vivo chicken chorioallantoic membrane assay was performed to study antiangiogenic effects. Molecular mechanisms were identified using TNF-α ELISA kit and docking tools. RESULTS: GC-MS analysis of RsSO revealed the presence of hexadecanoic and octadecanoic acid. Findings of DPPH, ABTS, and FRAP models indicated relatively moderate radical scavenging properties of RsSO. Oil showed antimicrobial activity against a variety of bacterial and fungal strains tested. Data of inflammation models showed significant (p < 0.05) anti-inflammatory effects of RsSO in both acute and chronic models. 500 mg/kg RsSO halted inflammation development significantly better (p < 0.05) as compared with lower doses. Histopathological evaluations of paws showed minimal infiltration of inflammatory cells in RsSO-treated animals. Findings of TNF-α ELSIA and docking studies showed that RsSO has the potential to down-regulate the expression of TNF-α, iNOS, ROS, and NF-κB respectively. Moreover, RsSO showed in vivo antiangiogenic effects. CONCLUSION: Data of the current study highlight that Raphanus sativus seeds oil has anti-inflammatory, and antiangiogenic properties and can be used as an adjunct to standard NSAIDs therapy which may reduce the dose and related side effects.


Assuntos
Raphanus , Fator de Necrose Tumoral alfa , Animais , Regulação para Baixo , Inflamação/tratamento farmacológico , Extratos Vegetais , Raphanus/metabolismo , Fator de Necrose Tumoral alfa/metabolismo
7.
Future Microbiol ; 16: 1289-1301, 2021 11.
Artigo em Inglês | MEDLINE | ID: mdl-34689597

RESUMO

COVID-19, caused by the SARS-CoV-2 outbreak, has resulted in a massive global health crisis. Bioactive molecules extracted or synthesized using starting material obtained from marine species, including griffithsin, plitidepsin and fingolimod are in clinical trials to evaluate their anti-SARS-CoV-2 and anti-HIV efficacies. The current review highlights the anti-SARS-CoV-2 potential of marine-derived phytochemicals explored using in silico, in vitro and in vivo models. The current literature suggests that these molecules have the potential to bind with various key drug targets of SARS-CoV-2. In addition, many of these agents have anti-inflammatory and immunomodulatory potentials and thus could play a role in the attenuation of COVID-19 complications. Overall, these agents may play a role in the management of COVID-19, but further preclinical and clinical studies are still required to establish their role in the mitigation of the current viral pandemic.


Assuntos
Antivirais/farmacologia , Antivirais/uso terapêutico , Tratamento Farmacológico da COVID-19 , Oceanos e Mares , SARS-CoV-2/efeitos dos fármacos , Alcaloides/farmacologia , Anti-Inflamatórios , Antivirais/química , Depsipeptídeos , Cloridrato de Fingolimode/química , Cloridrato de Fingolimode/farmacologia , Humanos , Lectinas , Biologia Marinha , Simulação de Acoplamento Molecular , Peptídeos Cíclicos/química , Peptídeos Cíclicos/farmacologia , Ficocianina/farmacologia , Compostos Fitoquímicos , Lectinas de Plantas/química , Lectinas de Plantas/farmacologia , Polifenóis/farmacologia , Polissacarídeos/farmacologia , Alga Marinha , Sesquiterpenos/farmacologia
8.
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
9.
Molecules ; 26(9)2021 Apr 24.
Artigo em Inglês | MEDLINE | ID: mdl-33923335

RESUMO

Wound-healing is complicated process that is affected by many factors, especially bacterial infiltration at the site and not only the need for the regeneration of damaged tissues but also the requirement for antibacterial, anti-inflammatory, and analgesic activity at the injured site. The objective of the present study was to develop and evaluate the natural essential oil-containing nanofiber (NF) mat with enhanced antibacterial activity, regenerative, non-cytotoxic, and wound-healing potential. Clove essential oil (CEO) encapsulated in chitosan and poly-ethylene oxide (PEO) polymers to form NFs and their morphology was analyzed using scanning electron microscopy (SEM) that confirmed the finest NFs prepared with a diameter of 154 ± 35 nm. The successful incorporation of CEO was characterized by Fourier transform infra-red spectroscopy (FTIR) and X-ray diffractometry (XRD). The 87.6 ± 13.1% encapsulation efficiency and 8.9 ± 0.98% loading of CEO was observed. A total of 79% release of CEO was observed in acidic pH 5.5 with 117% high degree of swelling. The prepared NF mat showed good antibacterial activity against Staphylococcus aureus and Escherichia coli and non-cytotoxic behavior against human fibroblast cell lines and showed good wound-healing potential.


Assuntos
Quitosana/farmacologia , Óleo de Cravo/farmacologia , Syzygium/química , Cicatrização/efeitos dos fármacos , Antibacterianos/química , Antibacterianos/farmacologia , Infecções Bacterianas/tratamento farmacológico , Infecções Bacterianas/microbiologia , Linhagem Celular , Quitosana/química , Óleo de Cravo/química , Escherichia coli/efeitos dos fármacos , Escherichia coli/patogenicidade , Fibroblastos/efeitos dos fármacos , Humanos , Nanofibras/química , Staphylococcus aureus/efeitos dos fármacos , Staphylococcus aureus/patogenicidade
11.
Molecules ; 27(1)2021 Dec 31.
Artigo em Inglês | MEDLINE | ID: mdl-35011482

RESUMO

Plumeria rubra (L.) is a traditional folkloric medicinal herb used to treat cardiovascular disorders. The present investigation was methodically planned to investigate the pharmacological foundations for the therapeutic effectiveness of P. rubra in cardiovascular illnesses and its underlying mechanisms. Ex vivo vaso-relaxant effects of crude leaf extract of P. rubra were observed in rabbit aorta ring preparations. Hypotensive effects were measured using pressure and force transducers connected to the Power Lab data acquisition system. Furthermore, P. rubra displayed cardioprotective properties in rabbits when they were exposed to adrenaline-induced myocardial infarction. In comparison to the intoxicated group, the myocardial infarction model showed decreased troponin levels, CK-MB, LDH, ALT, ALP, AST, and CRP, as well as necrosis, apoptosis, oedema, and inflammatory cell enrollment. P. rubra has revealed good antioxidant properties and prolonged the noradrenaline intoxicated platelet adhesion. Its anticoagulant, vasorelaxant, and cardioprotective effects in both in vivo and ex vivo investigations are enabled by blocking L-type calcium channels, lowering adrenaline, induced oxidative stress, and tissue tear, justifying its therapeutic utility in cardiovascular disorders.


Assuntos
Apocynaceae/química , Extratos Vegetais/química , Extratos Vegetais/farmacologia , Plantas Medicinais/química , Animais , Antioxidantes/química , Antioxidantes/farmacologia , Aorta/efeitos dos fármacos , Aorta/metabolismo , Cardiotônicos/química , Cardiotônicos/farmacologia , Doenças Cardiovasculares/tratamento farmacológico , Doenças Cardiovasculares/etiologia , Doenças Cardiovasculares/metabolismo , Cromatografia Líquida de Alta Pressão , Relação Dose-Resposta a Droga , Coração/efeitos dos fármacos , Miocárdio/metabolismo , Miocárdio/patologia , Coelhos , Vasodilatadores/química , Vasodilatadores/farmacologia
12.
Anticancer Agents Med Chem ; 21(11): 1460-1471, 2021.
Artigo em Inglês | MEDLINE | ID: mdl-33019940

RESUMO

INTRODUCTION: Inflammation is a vital reaction of the natural immune system that protects against encroaching agents. However, uncontrolled inflammation can lead to complications. Trigonella foenumgraecum is traditionally used as an anti-inflammatory herb. OBJECTIVES: The current study was conducted to explore the antioxidant, anti-inflammatory, and antiangiogenic potentials of Trigonella foenum-graecum seeds oil. METHODS: Oil was extracted from seeds of Trigonella foenum-graecum by cold press method and labelled as TgSO. Phytochemical (GC-MS, Folin-Ciocalteu method) and metal analyses were conducted to evaluate the metalo-chemical profile of TgSO. In vitro antioxidant assays (2,2-diphenyl-1-picrylhydrazyl, 2,2'-azino-bis-3- ethylbenzothiazoline-6-sulfonic acid and ferric reducing antioxidant power) were performed to assess its antioxidant potential. In vitro antimicrobial activity was evaluated using agar disc diffusion method and the safety profile of TgSO was assessed in acute toxicological studies following OECD 425 guidelines. In vivo antiinflammatory activities of TgSO were assessed in carrageenan, serotonin, histamine, formalin, and cotton pelletinduced oedema models. Serum TNF-α, Superoxide Dismutase (SOD) and, Catalases (CAT) levels were assessed by ELISA kits. In vivo antiangiogenic activity of TgSO was screened in chick Chorioallantoic Membrane (CAM) assay. Histopathological studies using excised paws were conducted to observe the effects of TgSO treatment at the tissue level. In silico docking studies were conducted to screen the binding potentials of identified compounds with TNF-α. RESULTS: Extraction by cold press method yielded 16% of TgSO. Phytochemical analysis of TgSO through GCMS showed the presence of eugenol, dihydrocoumairn, heptadecanoic acid, tri- and tetradecanoic acid, and hexadecanoic acid, respectively. Total phenolic contents of TgSO were found to be 0.30±0.01mg/g gallic acid equivalent in Folin-Ciocalteu method. Metal analysis indicated the presence of different metals in TgSO. Findings of antioxidant models showed the moderate antioxidant potential of TgSO. Findings of antimicrobial assays showed that TgSO was active against bacterial (S. aureus, S. epidermidis) and fungal (C. albicans, and A. niger) strains. In vivo toxicity study data showed that TgSO was safe up to the dose of 5000 mg/kg. Data of oedema models showed a significant (p<0.05) reduction in oedema development in TgSO treated animals in both acute and chronic models. Histopathological evaluations of paws showed minimum tissue infiltration with inflammatory cells in TgSO-treated animals. Treatment with TgSO also significantly (p<0.05) down-regulated TNF-α in serum while levels of SOD and CAT were up-regulated. Findings of the CAM assay revealed the antiangiogenic activity of TgSO. Findings of in silico docking studies showed that identified phytoconstituents can bind with culprit cytokine (TNF-α). CONCLUSION: Data obtained from the current study conclude that TgSO has antioxidant, anti-inflammatory, and antiangiogenic effects that validate its traditional uses. Synergistic actions of different phytoconstituents are proposed to be responsible for the observed effects.


Assuntos
Inibidores da Angiogênese/farmacologia , Antibacterianos/farmacologia , Anti-Inflamatórios/farmacologia , Antifúngicos/farmacologia , Granuloma/tratamento farmacológico , Compostos Fitoquímicos/farmacologia , Óleos de Plantas/farmacologia , Inibidores da Angiogênese/química , Inibidores da Angiogênese/isolamento & purificação , Animais , Antibacterianos/química , Antibacterianos/isolamento & purificação , Anti-Inflamatórios/química , Anti-Inflamatórios/isolamento & purificação , Antifúngicos/química , Antifúngicos/isolamento & purificação , Aspergillus niger/efeitos dos fármacos , Candida albicans/efeitos dos fármacos , Relação Dose-Resposta a Droga , Regulação para Baixo/efeitos dos fármacos , Edema/induzido quimicamente , Edema/tratamento farmacológico , Feminino , Inflamação/tratamento farmacológico , Masculino , Testes de Sensibilidade Microbiana , Estrutura Molecular , Neovascularização Patológica/tratamento farmacológico , Compostos Fitoquímicos/química , Compostos Fitoquímicos/isolamento & purificação , Óleos de Plantas/química , Óleos de Plantas/isolamento & purificação , Ratos , Sementes/química , Staphylococcus aureus/efeitos dos fármacos , Staphylococcus epidermidis/efeitos dos fármacos , Relação Estrutura-Atividade , Trigonella/química , Fator de Necrose Tumoral alfa/antagonistas & inibidores
13.
Inflammopharmacology ; 29(1): 281-293, 2021 Feb.
Artigo em Inglês | MEDLINE | ID: mdl-32297069

RESUMO

Inflammation and angiogenesis are two major contributors to tumourigenesis. Melilotus indicus is traditionally used as an anti-inflammatory agent. The current study was designed to investigate the anti-inflammatory and anti-angiogenic properties of ethanolic extract of M. indicus (Miet) whole plant and its marker compound (coumarin) using a series of in vivo methods. Extraction by maceration was adopted to prepare ethanolic extract. Phytochemical compounds present in Miet were investigated using both qualitative and quantitative methods. In vivo safety profile of Miet was investigated in behavioural studies. Four acute oedema models such as carrageenan, serotonin, histamine-induced paw oedema and xylene-induced ear oedema, and chronic formaldehyde-induced paw oedema model were employed to explore the anti-inflammatory potential of Miet. Chorioallantoic chick membrane assay (CAM) was performed to explore anti-angiogenic potential of Miet. Histopathological evaluations were conducted to access improvement in skin texture of paws. TNF-α ELISA kit was used to study effects of treatment on serum levels of TNF-α. Extraction by maceration resulted in formation of greenish coloured semisolid extract with a high coumarin content. In vivo toxicological studies revealed LD50 of Miet was greater than 8000 mg/kg. Data of acute inflammatory models depicted significant (p < 0.05) inhibition of oedema in Miet, coumarin and standard (piroxicam/indomethacin) treated groups. 750 mg/kg of Miet induced comparable (p > 0.05) anti-inflammatory effects to that of standard-treated groups. Coumarin showed better anti-inflammatory effects in carrageenan-induced paw oedema model as compared with histamine- and serotonin-induced oedema models. Data of chronic inflammatory models also depicted dose-dependent anti-inflammatory attributes of Miet which were comparable with standard treated groups. Significant (p > 0.05) downregulation of TNF-α in serum samples of animals treated with Miet and piroxicam was observed as compared with control group. Furthermore, Miet significantly halted blood vessels formation in CAM assay. Overall, data of the current study highlight that M. indicus has anti-inflammatory and anti-angiogenic potentials, and, thus, can potentially be used as an adjuvant therapy in solid tumours management.


Assuntos
Inibidores da Angiogênese/farmacologia , Anti-Inflamatórios/farmacologia , Cumarínicos/farmacologia , Melilotus/química , Inibidores da Angiogênese/administração & dosagem , Inibidores da Angiogênese/isolamento & purificação , Animais , Anti-Inflamatórios/administração & dosagem , Anti-Inflamatórios/isolamento & purificação , Cumarínicos/isolamento & purificação , Modelos Animais de Doenças , Relação Dose-Resposta a Droga , Edema/tratamento farmacológico , Etanol/química , Feminino , Indometacina/farmacologia , Inflamação/tratamento farmacológico , Dose Letal Mediana , Piroxicam/farmacologia , Extratos Vegetais/administração & dosagem , Extratos Vegetais/farmacologia , Extratos Vegetais/toxicidade , Ratos
14.
Inflammopharmacology ; 28(5): 1153-1161, 2020 Oct.
Artigo em Inglês | MEDLINE | ID: mdl-32803479

RESUMO

Coronavirus disease of 2019 (COVID-19) has emerged as a global health threat. Unfortunately, there are very limited approved drugs available with established efficacy against the SARs-CoV-2 virus and its inflammatory complications. Vaccine development is actively being researched, but it may take over a year to become available to general public. Certain medications, for example, dexamethasone, antimalarials (chloroquine/hydroxychloroquine), antiviral (remdesivir), and IL-6 receptor blocking monoclonal antibodies (tocilizumab), are used in various combinations as off-label medications to treat COVID-19. Essential oils (EOs) have long been known to have anti-inflammatory, immunomodulatory, bronchodilatory, and antiviral properties and are being proposed to have activity against SARC-CoV-2 virus. Owing to their lipophilic nature, EOs are advocated to penetrate viral membranes easily leading to membrane disruption. Moreover, EOs contain multiple active phytochemicals that can act synergistically on multiple stages of viral replication and also induce positive effects on host respiratory system including bronchodilation and mucus lysis. At present, only computer-aided docking and few in vitro studies are available which show anti-SARC-CoV-2 activities of EOs. In this review, role of EOs in the prevention and treatment of COVID-19 is discussed. A discussion on possible side effects associated with EOs as well as anti-corona virus claims made by EOs manufacturers are also highlighted. Based on the current knowledge a chemo-herbal (EOs) combination of the drugs could be a more feasible and effective approach to combat this viral pandemic.


Assuntos
Anti-Inflamatórios não Esteroides/uso terapêutico , Antivirais/uso terapêutico , Infecções por Coronavirus/tratamento farmacológico , Fatores Imunológicos/uso terapêutico , Óleos Voláteis/uso terapêutico , Pneumonia Viral/tratamento farmacológico , Anti-Inflamatórios não Esteroides/efeitos adversos , Antivirais/efeitos adversos , COVID-19 , Humanos , Fatores Imunológicos/efeitos adversos , Óleos Voláteis/efeitos adversos , Pandemias , Plantas Medicinais/química
15.
Inflammopharmacology ; 28(6): 1691-1704, 2020 Dec.
Artigo em Inglês | MEDLINE | ID: mdl-32385747

RESUMO

Chronic wounds may lead to the development of various pathological conditions such as diabetic foot ulcers and pressure sores. The current study evaluated wound healing and anti-inflammatory potentials of methanolic extract of Ephedra ciliata using series of in vivo models. Methanolic extract of Ephedra ciliata was prepared by maceration (Ec.Me). Qualitative and quantitative (HPLC) phytochemical and metal analyses were conducted to explore the chemical and metal profiles of Ec.Me. Safety profile (behavioural) and, antimicrobial, antioxidant, wound healing, anti-inflammatory and anti-angiogenic potentials of Ec.Me were evaluated using well-established in vitro and in vivo models. ELISA assay was performed to estimate the effects of Ec.Me treatment on serum levels of TNF-α. HPLC analysis identified quercetin as one of the major compounds in Ec.Me. Safety study data showed that Ec.Me was safe up to the dose of 2000 mg/kg. Antimicrobial assay data showed that Ec.Me was active against bacterial (Staphylococcus aureus) as well as fungal (Candida albicans and Aspergillus niger) strains. Ec.Me showed modertate antioxidant potential in in vitro and in vivo models. Data of excision and burn wound healing models showed that Ec.Me, promoted wound closure in a dose and time-dependent manner. Treatment with 20% Ec.Me cream and heparin showed almost the same effects with no statistical differences (p > 0.05). Ec.Me also showed time-dependent anti-inflammatory activities in both acute and chronic models. In carrageenan model, treatment with 200 mg/kg of Ec.Me showed comparable anti-inflammatory effects (p > 0.05) with quercetin and indomethacin throughout the study. In cotton pellet granuloma model treatment with 200 mg/kg of Ec.Me and indomethacin inhibited granuloma formation significantly better (p < 0.05) as compared with the rest of the treatment groups. Histopathological examination of skin samples showed marked improvement in architecture with minimal infiltration of inflammatory cells. Data of in vivo angiogenesis assay showed marked improvement in vessels length, density, branching points, total segments and total nets after treatment with Ec.Me, indicating no toxic effects towards vasculature development. Significant (p < 0.05) downregulation of TNF-α was observed in serum samples of animals treated with Ec.Me. Based on data of the current study, it is concluded that quercetin-rich extract of Ephedra ciliata has wound healing and anti-inflammatory potentials via downregulation of TNF-α. Moreover, it is suggested that the antimicrobial activity of Ec.Me prevented microbial invasion, thus promoted natural wound healing mechanisms as well.


Assuntos
Anti-Inflamatórios/farmacologia , Regulação para Baixo/efeitos dos fármacos , Ephedra/química , Inflamação/tratamento farmacológico , Extratos Vegetais/farmacologia , Fator de Necrose Tumoral alfa/metabolismo , Cicatrização/efeitos dos fármacos , Animais , Anti-Infecciosos/farmacologia , Antioxidantes/farmacologia , Aspergillus niger/efeitos dos fármacos , Candida albicans/efeitos dos fármacos , Feminino , Indometacina/farmacologia , Inflamação/metabolismo , Masculino , Metanol/química , Testes de Sensibilidade Microbiana/métodos , Folhas de Planta/química , Quercetina/farmacologia , Ratos , Pele/efeitos dos fármacos , Pele/metabolismo , Staphylococcus aureus/efeitos dos fármacos
16.
Inflammopharmacology ; 28(4): 993-1008, 2020 Aug.
Artigo em Inglês | MEDLINE | ID: mdl-32172496

RESUMO

Launaea spinosa is used as an anti-inflammatory agent traditionally. This study was conducted to evaluate anti-inflammatory and anti-angiogenic activities of methanol extract of Launaea spinosa. Extraction was performed by maceration and the resultant green coloured extract was labelled as Ls.Me. Solubility analysis showed that Ls.Me was miscible with distilled water, normal saline, ethanol and methanol. Metal analysis following acid digestion method exhibited the presence of copper, magnesium, manganese, iron, zinc and calcium. Phytochemical analysis confirmed the presence of different classes of secondary metabolites in Ls.Me. HPLC analysis showed the presence of quercetin, gallic acid, caffeic acid, benzoic acid and sinapic acid in Ls.Me. Data of in vitro antioxidant assays showed moderate antioxidant potential of Ls.Me which was also confirmed by data of in vivo enzymes (SOD, CAT, and TSP) assays. Antimicrobial assays data showed that Ls.Me was active against S.aureus and S.epidermidis (bacterial) as well as C.albicans and A.niger (fungal) strains. Data of acute physio-pathological studies showed no abnormalities in Albino rats up to the dose of 2000 mg/kg of Ls.Me. Acute and chronic inflammatory models were used to evaluate anti-inflammatory effects of Ls.Me. Data of acute studies showed that Ls.Me has the potential to arrest inflammation produced by different mediators in a dose-dependent manner. 200 mg/kg of Ls.Me was found to produce significantly (p < 0.05) better anti-inflammatory effects than 100 mg/kg of Ls.Me. Ls.Me also significantly (p < 0.05) inhibited ear edema induced by xylene. Ls.Me showed profound anti-inflammatory responses in paw edema induced by formalin and also inhibited granuloma development in cotton pellet-induced granuloma model. Histopathological and biochemical investigations showed marked reduction in the number of inflammatory cells. TNF-α and IL-6 ELSIA kits were used to study effects of Ls.Me treatment on serum levels of TNF-α and IL-6. Data obtained showed significant (p < 0.05) reduction in TNF-α and IL-6 levels in serum of animals treated with Ls.Me. Data of in vivo angiogenesis assay showed that 200 µg/ml of Ls.Me significantly halted vasculature development indicating its potent anti-angiogenic potential. On the basis of findings of the current study, it is concluded that multiple phytochemicals present in Ls.Me act synergistically to produce anti-inflammatory and anti-angiogenic effects. Further studies are required to standardize the plant extract and explore its safety profile.


Assuntos
Inibidores da Angiogênese/farmacologia , Anti-Inflamatórios/farmacologia , Asteraceae/química , Extratos Vegetais/farmacologia , Inibidores da Angiogênese/química , Inibidores da Angiogênese/isolamento & purificação , Animais , Antibacterianos/química , Antibacterianos/farmacologia , Anti-Inflamatórios/química , Anti-Inflamatórios/isolamento & purificação , Embrião de Galinha , Cromatografia Líquida de Alta Pressão , Cromatografia em Camada Fina , Edema/tratamento farmacológico , Feminino , Masculino , Metanol/química , Extratos Vegetais/química , Extratos Vegetais/isolamento & purificação , Ratos
17.
Acta Pol Pharm ; 72(5): 821-7, 2015.
Artigo em Inglês | MEDLINE | ID: mdl-26665388

RESUMO

Ruellia is a genus of flowering plants commonly known as Ruellias or Wild Petunias which belongs to the family Acanthaceae. It contains about 250 genera and 2500 species. Most of these are shrubs, or twining vines; some are epiphytes. Only a few species are distributed in temperate regions. They are distributed in Indonesia and Malaysia, Africa, Brazil, Central America and Pakistan. Some of these are used as medicinal plants. Many species of the genus has antinociceptive, antioxidant, analgesic, antispasmolytic, antiulcer, antidiabetic and anti-inflammatory properties. The phytochemicals constituents: glycosides, alkaloids, flavonoids and triterpenoids are present. The genus has been traditionally claimed to be used for the treatment of flu, asthma, fever, bronchitis, high blood pressure, eczema, and diabetes. The objective of this review article is to summarize all the pharmacological and phytochemical evaluations or investigations to find area of gap and endorse this genus a step towards commercial drug. Hence, further work required is to isolate and characterize the active compounds responsible for these activities in this plant and bring this genus plants to commercial health market to serve community with their potential benefits.


Assuntos
Acanthaceae/química , Etnofarmacologia , Extratos Vegetais/farmacologia , Animais , Humanos , Compostos Fitoquímicos/análise , Fitoterapia
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