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1.
Clin Exp Hypertens ; 43(1): 69-76, 2021 Jan 02.
Artigo em Inglês | MEDLINE | ID: mdl-32799699

RESUMO

BACKGROUND: High blood pressure effects heart and vessels. Development of pathogenesis is the result of oxidative stress. We aimed to investigate the antioxidant effects of propolis, caffeic acid phenethyl ester (CAPE), and pollen on the hearts of rats which chronic nitric oxide synthase (NOS) inhibited through Nω-nitro-L-arginine methyl ester (L-NAME). Paraoxonase 1 (PON1), total antioxidant status (TAS), total oxidant status (TOS), oxidative stress index (OSI), asymmetric dimethylarginine (ADMA), and nuclear factor-κB (NF-κB) were analyzed on the heart. MATERIAL AND METHODS: Sprague-Dawley rats were divided five groups of seven rats in every group; Group I: Control, Group II: L-NAME, Group III: L-NAME+propolis, Group IV: L-NAME+CAPE and Group V: L-NAME+pollen. L-NAME become dissolved in regular saline (0.9% NaCl w/v). The ethanolic extract of propolis (200 mg/kg/days, gavage), pollen (100 mg/kg/days, by gavage), CAPE (50 µM/kg/days, intraperitoneally), and the NOS inhibitor L-NAME (40 mg/kg, intraperitoneally) had been administered. RESULTS: Blood pressure (BP) of rats treated with propolis, CAP,E and pollen statistically significant decreased. Decreasing in BP of the rats of pollen group was more than CAPE and propolis groups (P < .05). PON1 and TAS levels decreased in L-NAME-treated groups (P < .05), but ranges have been better in propolis, CAPE and pollen groups. TOS, ADMA and NF-κB levels increased (P < .05) in L-NAME group; however, these parameters were lower (P < .05) in propolis and CAPE groups (P < .05). CONCLUSIONS: Vasorelaxant properties and free radical scavenging actions of propolis, CAPE, and pollen may reduce the oxidative stress and blood pressure in the rats chronic NOS inhibited through L-NAME.


Assuntos
Pressão Sanguínea/efeitos dos fármacos , Ácidos Cafeicos/farmacologia , Sequestradores de Radicais Livres/farmacologia , Miocárdio/metabolismo , Álcool Feniletílico/análogos & derivados , Pólen , Própole/farmacologia , Animais , Anti-Inflamatórios/farmacologia , Antioxidantes/metabolismo , Arginina/análogos & derivados , Arginina/metabolismo , Arildialquilfosfatase/metabolismo , Masculino , NF-kappa B/metabolismo , NG-Nitroarginina Metil Éster , Óxido Nítrico Sintase/antagonistas & inibidores , Oxidantes/metabolismo , Estresse Oxidativo/efeitos dos fármacos , Álcool Feniletílico/farmacologia , Ratos , Ratos Sprague-Dawley
2.
Cell Mol Biol (Noisy-le-grand) ; 66(4): 78-103, 2020 Jun 25.
Artigo em Inglês | MEDLINE | ID: mdl-32583790

RESUMO

The genus Achillea genus houses more than 100 species, a number of them are popularly used in traditional medicine for spasmodic gastrointestinal, gynecological and hepatobiliary disorders, hemorrhages, pneumonia, rheumatic pain, inflammation, wounds healing etc. Members of the genus contain a wide variety of volatile and non-volatile secondary metabolites, including terpenes, polyphenols, flavonoids and others. Multiple studies have assessed the biological effects and other aspects of Achillea spp. In a number of preclinical studies, Achillea plants and their essential oils have demonstrated promising antibacterial properties against a number of human and plant pathogens. Besides, the plants have displayed strong antioxidative and potent anti-proliferative and anticancer properties in various cellular and animal models. Achillea plants have widely been used as food preservative in food industry. Clinical studies have indicated its potential against multiple sclerosis (MS), irritable bowel syndrome (IBS), ulcerative colitis, episiotomy wound, primary dysmenorrhea, oral mucositis etc. The present work focuses to provide a brief overview on folk knowledge, phytochemistry, biological activity and applications of Achillea plants. There is a close relationship between the traditional ethnobotanical usage and pharmacological and clinical data from different Achillea spp. The application of Achillea plants and their extracts seems to be a promising alternative for antimicrobial and antioxidant purposes in food, pharmaceutical and cosmetic industries.


Assuntos
Achillea/química , Etnobotânica , Indústrias , Compostos Fitoquímicos/análise , Fitoterapia , Achillea/classificação , Animais , Humanos , Medicina Tradicional , Compostos Fitoquímicos/química
3.
J Asian Nat Prod Res ; 22(1): 1-16, 2020 Jan.
Artigo em Inglês | MEDLINE | ID: mdl-29973097

RESUMO

Eupatilin (5,7-dihydroxy-3',4',6-trimethoxyflavone) is a pharmacologically active flavone which has been isolated from a variety of medicinal plants. Eupatilin is known to possess various pharmacological properties such as anti-cancer, anti-oxidant, and anti-inflammatory. It is speculated that eupatilin could be subjected to structural optimization for the synthesis of derivative analogs to reinforce its efficacy, to minimize toxicity, and to optimize absorption profiles, which will ultimately lead towards potent drug candidates. Although, reported data acclaim multiple pharmacological activities of eupatilin but further experimentations on its molecular mechanism of action are yet mandatory to elucidate full spectrum of its pharmacological activities.


Assuntos
Medicamentos de Ervas Chinesas , Flavonas , Flavonoides , Estrutura Molecular
4.
Cell Physiol Biochem ; 53(2): 301-322, 2019.
Artigo em Inglês | MEDLINE | ID: mdl-31343125

RESUMO

BACKGROUND/AIMS: Propolis is one of the most promising natural products, exhibiting not only therapeutic but also prophylactic actions. Propolis has several biological and pharmacological properties, including hepatoprotective activities. The present study aimed to investigate the underlying molecular mechanisms of propolis against CCl4-mediated liver fibrosis. METHODS: Three groups of male BALB/c mice (n=15/ group) were used: group 1 comprised control mice; groups 2 and 3 were injected with CCl4 for the induction of liver fibrosis. Group 3 was then orally supplemented with propolis (100 mg/kg body weight) for four weeks. Different techniques were used to monitor the antifibrotic effects of propolis, including histopathological investigations using H&E, Masson's trichrome and Sirius red staining; Western blotting; flow cytometry; and ELISA. RESULTS: We found that the induction of liver fibrosis by CCl4 was associated with a significant increase in hepatic collagen and α-smooth muscle actin (α-SMA) expression. Moreover, CCl4-treated mice also exhibited histopathological alterations in the liver architecture. Additionally, the liver of CCl4-treated mice exhibited a marked increase in proinflammatory signals, such as increased expression of HSP70 and increased levels of proinflammatory cytokines and ROS. Mechanistically, the liver of CCl4-treated mice exhibited a significant increase in the phosphorylation of AKT and mTOR; upregulation of the expression of BAX and cytochrome C; downregulation of the expression of Bcl2; a significant elevation in the levels of TGF-ß followed by increased phosphorylation of SMAD2; and a marked increase in the expression of P53 and iNOS. Interestingly, oral supplementation of CCl4-treated mice with propolis significantly abolished hepatic collagen deposition, abrogated inflammatory signals and oxidative stress, restored CCl4-mediated alterations in the signaling cascades, and hence repaired the hepatic architecture nearly to the normal architecture observed in the control mice. CONCLUSION: Our findings revealed the therapeutic potential and the underlying mechanisms of propolis against liver fibrosis.


Assuntos
Apoptose/efeitos dos fármacos , Cirrose Hepática Experimental/patologia , Própole/farmacologia , Transdução de Sinais/efeitos dos fármacos , Animais , Tetracloreto de Carbono/toxicidade , Citocinas/metabolismo , Células Estreladas do Fígado/citologia , Células Estreladas do Fígado/efeitos dos fármacos , Células Estreladas do Fígado/metabolismo , Fígado/metabolismo , Fígado/patologia , Cirrose Hepática Experimental/induzido quimicamente , Cirrose Hepática Experimental/metabolismo , Masculino , Camundongos , Camundongos Endogâmicos BALB C , Óxido Nítrico Sintase Tipo II/metabolismo , Fosfatidilinositol 3-Quinases/metabolismo , Proteínas Proto-Oncogênicas c-akt/metabolismo , Proteínas Proto-Oncogênicas c-bcl-2/metabolismo , Espécies Reativas de Oxigênio/metabolismo , Proteína Smad2/metabolismo , Serina-Treonina Quinases TOR/metabolismo , Fator de Crescimento Transformador beta/metabolismo , Proteína Supressora de Tumor p53/metabolismo , Proteína X Associada a bcl-2/metabolismo
5.
IUBMB Life ; 71(10): 1418-1427, 2019 10.
Artigo em Inglês | MEDLINE | ID: mdl-31169978

RESUMO

Altered enzymatic machineries are a substantial biochemical characteristic of tumor cell metabolism that switch metabolic profile from oxidative phosphorylation to amplified glycolysis as well as increased lactate production under hypoxia conditions. Reprogrammed metabolic profile is an emerging hallmark of cancer. Overexpression of several glycolytic enzymes and glucose transporters has been reported in 24 different types of cancers that represent approximately 70% of all the cancer cases around the globe. Thus, targeting glycolytic enzymes could serve as tempting avenue for drug design against cancer. Phosphoglycerate mutase 1 (PGAM1) is an important glycolytic enzyme that catalyzes the conversion of 3-phosphoglycerate to 2-phosphoglycerate. Recent investigations have revealed the overexpression of PGAM1 in several human cancers that is linked with tumor growth, survival, and invasion. The aim of this review is to update scientific research network with cancer-specific role of PGAM1 to elucidate its capability as bonafide therapeutic target for cancer therapy. Moreover, we have also summarized the reported genetic and pharmacological inhibitors of PGAM1. This study suggests that further investigations on PGAM1 should focus on the exploration of molecular mechanisms of PGAM1 overexpression in development of cancer, assessment of biosafety profiles of known inhibitors of PGAM1, and utilization of PGAM1 inhibitors in combinatorial therapies. These future studies will surely support the unbiased strategies for the development of novel PGAM1 inhibitors for cancer therapies.


Assuntos
Terapia de Alvo Molecular , Neoplasias/genética , Neoplasias/terapia , Fosfoglicerato Mutase/genética , Proliferação de Células/genética , Ácidos Glicéricos/metabolismo , Glicólise/genética , Humanos , Neoplasias/diagnóstico
6.
Molecules ; 24(10)2019 May 14.
Artigo em Inglês | MEDLINE | ID: mdl-31091784

RESUMO

Cucurbita genus has received a renowned interest in the last years. This plant species, native to the Americas, has served worldwide folk medicine for treating gastrointestinal diseases and intestinal parasites, among other clinical conditions. These pharmacological effects have been increasingly correlated with their nutritional and phytochemical composition. Among those chemical constituents, carotenoids, tocopherols, phenols, terpenoids, saponins, sterols, fatty acids, and functional carbohydrates and polysaccharides are those occurring in higher abundance. However, more recently, a huge interest in a class of triterpenoids, cucurbitacins, has been stated, given its renowned biological attributes. In this sense, the present review aims to provide a detailed overview to the folk medicinal uses of Cucurbita plants, and even an in-depth insight on the latest advances with regards to its antimicrobial, antioxidant and anticancer effects. A special emphasis was also given to its clinical effectiveness in humans, specifically in blood glucose levels control in diabetic patients and pharmacotherapeutic effects in low urinary tract diseases.


Assuntos
Cucurbita/química , Cucurbitacinas/química , Cucurbitacinas/farmacologia , Anti-Infecciosos/química , Anti-Infecciosos/farmacologia , Antineoplásicos Fitogênicos/química , Antineoplásicos Fitogênicos/farmacologia , Antioxidantes/química , Antioxidantes/farmacologia , Glicemia/efeitos dos fármacos , Etnofarmacologia , Humanos , Medicina Tradicional , Extratos Vegetais/química
7.
Pak J Pharm Sci ; 32(4(Supplementary)): 1761-1766, 2019 Jul.
Artigo em Inglês | MEDLINE | ID: mdl-31680070

RESUMO

Peripheral nerve injury is a complex condition which results in restricted physical activity. Despite the tremendous efforts to figure out effective remedies, the complete functional retrieval is still a goal to be achieved. So, the need of hour is the exploration of potential natural compounds to recover this functional loss. Here, we have investigated the role of a local plant "Neurada procumbens" in ameliorating the functional recovery after an induced nerve compression injury in a mouse model. A dose of N. procumbens (50mg/kg of body weight) was administered orally from the day of injury to onwards. The motor functional recovery was assessed by evaluating muscle grip strength and sciatic functional index; while the sensory functions were gauged by the hotplate test. The serological parameters were carried out to analyze the effect of N. procumbens on oxidative stress level. The recovery of sensory and motor functions was significantly improved and perceived earlier in the treatment group. Moreover, the elevated antioxidant level was statistically significant in the treatment group. These results indicate that the supplementation of N. procumbens accelerates functional recovery after sciatic nerve crush injury.


Assuntos
Traumatismos dos Nervos Periféricos/tratamento farmacológico , Preparações de Plantas/farmacologia , Recuperação de Função Fisiológica/efeitos dos fármacos , Nervo Isquiático/efeitos dos fármacos , Neuropatia Ciática/tratamento farmacológico , Animais , Antioxidantes/farmacologia , Modelos Animais de Doenças , Camundongos , Atividade Motora/efeitos dos fármacos , Regeneração Nervosa/efeitos dos fármacos , Estresse Oxidativo/efeitos dos fármacos
8.
IUBMB Life ; 70(11): 1076-1083, 2018 11.
Artigo em Inglês | MEDLINE | ID: mdl-30160039

RESUMO

Reprogrammed metabolic profile is a biochemical fingerprint of cancerous cells, which represents one of the "hallmarks of cancer." The aberrant expression pattern of enzymatic machineries orchestrates metabolic activities into a platform that ultimately promotes cellular growth, survival, and proliferation. The NADP(+)-dependent mitochondrial malic enzyme 2 (ME2) has been widely appreciated due to its function as a provider of pyruvate and reducing power to the cell for biosynthesis of fatty acids and nucleotides along with maintenance of redox balance. Multiple lines of evidences have indicated that ME2 is a bonafide therapeutic target and novel biomarker which plays critical role during tumorigenesis. The objective of this review is to provide an update on the cancer-specific role of ME2 in order to explore its potential for therapeutic opportunities. Furthermore, we have discussed the potential of genetic and pharmacological inhibitors of ME2 in the light of previous research work for therapeutic advancements in cancer treatment. It is contemplated that additional investigations should focus on the use of ME2 inhibitors in combinational therapies as rational combinations of metabolic inhibitors and chemotherapy may have the ability to cure cancer. © 2018 IUBMB Life, 70(11):1076-1083, 2018.


Assuntos
Antineoplásicos/uso terapêutico , Malato Desidrogenase/antagonistas & inibidores , Neoplasias/tratamento farmacológico , Neoplasias/enzimologia , Humanos , Neoplasias/patologia , Prognóstico
9.
Pak J Pharm Sci ; 31(5(Supplementary)): 2163-2168, 2018 Sep.
Artigo em Inglês | MEDLINE | ID: mdl-30393228

RESUMO

Mushrooms, a treasure of diverse bioactive scaffolds, have been widely admired due to their nutritional and medicinal significance all over the world. The current study intended to evaluate the therapeutic potentiality of an edible mushroom, Leucoagaricus leucothites (Vittad.) Wasser. Thus, anti-oxidant potential of L. leucothites was determined using DPPH assay and for the determination of anti-microbial potential agar dilution procedure was followed. TOS (total oxidant status), TAS (total anti-oxidant status), and OSI (oxidative stress index) values were evaluated utilizing Rel Assay Kits. For the assessment of heavy metal contents, wet decomposition approach with atomic absorption spectrophotometry was adopted. Screening of phytochemicals present in ethanolic extract of L. leucothites were determined by HPLC. TAS, TOS and OSI values were found to be 8.291mmol/L, 10.797µmol/L and 0.130 respectively. Our results declared that heavy metal contents are generally in the safe range. Phytochemical analysis of L. leucothites has affirmed the presence of important phenolics such as gallic acid, catechin, and hesperidin. Investigations on anti-oxidant and anti-microbial potential of L. leucothites has uncovered the fact that this naturally occurring, biologically active, and therapeutically effective mushroom specie has natural borne anti-oxidant and anti-microbial potential and it would be worthwhile to use it for nutritional as well as medicinal purpose.


Assuntos
Agaricales , Anti-Infecciosos/farmacologia , Antioxidantes/farmacologia , Metais Pesados , Estresse Oxidativo/efeitos dos fármacos , Agaricales/química , Anti-Infecciosos/isolamento & purificação , Antioxidantes/isolamento & purificação , Candida albicans/efeitos dos fármacos , Candida albicans/crescimento & desenvolvimento , Escherichia coli/efeitos dos fármacos , Escherichia coli/fisiologia , Humanos , Metais Pesados/isolamento & purificação , Estresse Oxidativo/fisiologia
10.
Cell Biochem Funct ; 35(6): 304-314, 2017 Aug.
Artigo em Inglês | MEDLINE | ID: mdl-28833317

RESUMO

The objective of this study was to evaluate the antioxidant effects of propolis, caffeic acid phenethyl ester (CAPE; active compound in propolis), and pollen on biochemical oxidative stress biomarkers in rat kidney tissue inhibited by Nω -nitro-L-arginine methyl ester (L-NAME). The biomarkers evaluated were paraoxonase (PON1), oxidative stress index (OSI), total antioxidant status (TAS), total oxidant status (TOS), asymmetric dimethylarginine (ADMA), and nuclear factor kappa B (NF-κB). TAS levels and PON1 activity were significantly decreased in kidney tissue samples in the L-NAME-treated group (P < 0.05). The levels of TAS and PONI were higher in the L-NAME plus propolis, CAPE, and pollen groups compared with the L-NAME-treated group. TOS, ADMA, and NF-κB levels were significantly increased in the kidney tissue samples of the L-NAME-treated group (P < 0.05). However, these parameters were significantly lower in the L-NAME plus propolis, CAPE, and pollen groups (P < 0.05) compared with rats administered L-NAME alone (P < 0.05). Furthermore, the binding energy of CAPE within catalytic domain of glutathione reductase (GR) enzyme as well as its inhibitory mechanism was determined using molecular modeling approaches. In conclusion, experimental and theoretical data suggested that oxidative alterations occurring in the kidney tissue of chronic hypertensive rats may be prevented via active compound of propolis, CAPE administration.


Assuntos
Ácidos Cafeicos/farmacologia , Nefropatias/etiologia , Simulação de Dinâmica Molecular , Estresse Oxidativo/efeitos dos fármacos , Álcool Feniletílico/análogos & derivados , Própole/farmacologia , Animais , Antioxidantes , Arginina/análogos & derivados , Arginina/metabolismo , Arginina/toxicidade , Arildialquilfosfatase/metabolismo , Sítios de Ligação , Ácidos Cafeicos/química , Ácidos Cafeicos/metabolismo , Glutationa Redutase/química , Glutationa Redutase/metabolismo , Meia-Vida , Hipertensão/metabolismo , Hipertensão/patologia , Nefropatias/metabolismo , Masculino , Simulação de Acoplamento Molecular , NF-kappa B/metabolismo , Álcool Feniletílico/química , Álcool Feniletílico/metabolismo , Álcool Feniletílico/farmacologia , Pólen/química , Pólen/metabolismo , Própole/metabolismo , Estrutura Terciária de Proteína , Ratos , Ratos Sprague-Dawley
11.
Cureus ; 16(3): e57064, 2024 Mar.
Artigo em Inglês | MEDLINE | ID: mdl-38681260

RESUMO

We aim to evaluate the bond strength between resin composite and primary demineralized dentin, pretreated with silver diamine fluoride (SDF) and simultaneous SDF with potassium iodide (KI) after thermal aging. In this in vitro study, human carious-free primary molars were randomly assigned into three groups and prepared by exposing the superficial dentin. The primary dentin of each molar was demineralized. The first group (the control) received saline treatment before bond application. SDF was pretreated for the second group, whereas SDF and KI were used for the third. After that, the pretreated dentin was immediately built with resin composite bonded with a universal adhesive and kept wet for 24 hours. Then, the pretreated molars were prepared into beam specimens for microtensile bond strength (µTBS), 16 for each group, and subjected to thermal aging. Lastly, they were tested using a universal testing machine, and the resulting data were analyzed using one-way analysis of variance (ANOVA) followed by Tukey's post hoc test. It was found that the SDF-KI group had a significant difference with both the control and SDF groups (p < 0.05), while the control and SDF groups showed no significant differences (p = 0.310). The SDF-KI group had the highest mean value of 11.73 ± 4.39 megapascal (MPa). In contrast, the control group had the lowest mean value of 9.31 ± 3.41 MPa. Post hoc pairwise comparison results showed that SDF-KI pretreatment had a significantly higher strength value than the control and SDF groups. Pretreatment of demineralized primary dentin with SDF-KI does not negatively affect the immediate loading of resin composite. However, under the limitation of this study, KI application after SDF pretreatment is recommended to enhance the bond's durability of resin composite to demineralized dentin.

12.
Saudi J Biol Sci ; 29(5): 3372-3379, 2022 May.
Artigo em Inglês | MEDLINE | ID: mdl-35865797

RESUMO

Tumor metabolism, an emerging hallmark of cancer, is characterized by aberrant expression of enzymes from various metabolic pathways including glycolysis and PPP (pentose phosphate pathway). Glucose 6 phosphate dehydrogenase (G6PD) and 6-phosphogluconate dehydrogenase (6PGD), oxidative carboxylases of PPP, have been reported to accomplish different biosynthetic and energy requirements of cancer cells. G6PD and 6PGD have been proposed as potential therapeutic targets for cancer therapy during recent years due to their overexpression in various cancers. Here, we have employed enzymatic assay based screening using in-house G6PD and 6PGD assay protocols for the identification of mushroom extracts which could inhibit G6PD or 6PGD enzymatic activity for implications in cancer therapy. For the fulfillment of the objectives of present study, nine edible mushrooms were subjected to green extraction for preparation of ethanolic extracts. 6xhis-G6PD and pET-28a-h6PGD plasmids were expressed in BL21-DE3 E. coli cells for the expression and purification of protein of interests. Using purified proteins, in house enzymatic assay protocols were established. The preliminary screening identified two extracts (Macrolepiota procera and Terfezia boudieri) as potent and selective G6PD inhibitors, while no extract was found highly active against 6PGD. Further, evaluation of anticancer potential of mushroom extracts against lung cancer cells revealed Macrolepiota procera as potential inhibitor of cancer cell proliferation with IC50 value of 6.18 µg/ml. Finally, screening of M. procera-derived compounds against G6PD via molecular docking has identified paraben, quercetin and syringic acid as virtual hit compounds possessing good binding affinity with G6PD. The result of present study provides novel findings for possible mechanism of action of M. procera extract against A549 via G6PD inhibition suggesting that M. procera might be of therapeutic interest for lung cancer treatment.

13.
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
14.
Curr Pharm Des ; 27(4): 456-466, 2021.
Artigo em Inglês | MEDLINE | ID: mdl-32348212

RESUMO

Nature always remains an inexhaustible source of treasures for mankind. It remains a mystery for every challenge until the completion of the challenge. While we talk about the complicated health issues, nature offers us a great variety of chemical scaffolds and their various moieties packed in the form of natural products e.g., plants, microorganisms (fungi, algae, protozoa), and terrestrial vertebrates and invertebrates. This review article is an update about jaceosidin, a bioactive flavone, from genus Artemisia. This potentially active compound exhibits a variety of pharmacological activities including anti-inflammatory, anti-oxidant, anti-bacterial, antiallergic and anti-cancer activities. The bioactivities and the therapeutic action of jaceosidin, especially the modulation of different cell signaling pathways (ERK1/2, NF-κB, PI3K/Akt and ATM-Chk1/2) which become deregulated in various pathological disorders, have been focused here. The reported data suggest that the bioavailability of this anti-cancer compound should be enhanced by utilizing various chemical, biological and computational techniques. Moreover, it is recommended that researchers and scientists should work on exploring the mode of action of this particular flavone to precede it further as a potent anti-cancer compound.


Assuntos
Artemisia , Flavonas , Animais , Flavonas/farmacologia , Flavonoides , Fosfatidilinositol 3-Quinases
15.
Oxid Med Cell Longev ; 2021: 2713511, 2021.
Artigo em Inglês | MEDLINE | ID: mdl-34840666

RESUMO

As an antioxidant, lycopene has acquired importance as it prevents autoxidation of fats and related products. Tomatoes are an important agricultural product that is a great source of lycopene. It contains many vitamins and minerals, fiber, and carbohydrates and is associated with various positive effects on health. The antioxidant potential of tomatoes is substantially explained with lycopene compounds. Diet is a major risk factor for heart diseases which is shown as the most important cause of death in the world. It has been observed that the lycopene taken in the diet has positive effects in many stages of atherosclerosis. The serum lipid levels, endothelial dysfunction, inflammation, blood pressure, and antioxidative potential are mainly affected by lycopene. These natural antioxidants, which can also enhance the nutritional value of foods, may lead to new ways if used in food preservation. In this review study, the antioxidant potential and cardiovascular protection mechanism of lycopene are discussed.


Assuntos
Antioxidantes/farmacologia , Doenças Cardiovasculares/prevenção & controle , Licopeno/farmacologia , Animais , Antioxidantes/administração & dosagem , Doenças Cardiovasculares/metabolismo , Doenças Cardiovasculares/patologia , Manipulação de Alimentos , Humanos , Licopeno/administração & dosagem
16.
Antibiotics (Basel) ; 10(8)2021 Aug 20.
Artigo em Inglês | MEDLINE | ID: mdl-34439061

RESUMO

The SARS CoV-2 pandemic has affected millions of people around the globe. Despite many efforts to find some effective medicines against SARS CoV-2, no established therapeutics are available yet. The use of phytochemicals as antiviral agents provides hope against the proliferation of SARS-CoV-2. Several natural compounds were analyzed by virtual screening against six SARS CoV-2 protein targets using molecular docking simulations in the present study. More than a hundred plant-derived secondary metabolites have been docked, including alkaloids, flavonoids, coumarins, and steroids. SARS CoV-2 protein targets include Main protease (MPro), Papain-like protease (PLpro), RNA-dependent RNA polymerase (RdRp), Spike glycoprotein (S), Helicase (Nsp13), and E-Channel protein. Phytochemicals were evaluated by molecular docking, and MD simulations were performed using the YASARA structure using a modified genetic algorithm and AMBER03 force field. Binding energies and dissociation constants allowed the identification of potentially active compounds. Ligand-protein interactions provide an insight into the mechanism and potential of identified compounds. Glycyrrhizin and its metabolite 18-ß-glycyrrhetinic acid have shown a strong binding affinity for MPro, helicase, RdRp, spike, and E-channel proteins, while a flavonoid Baicalin also strongly binds against PLpro and RdRp. The use of identified phytochemicals may help to speed up the drug development and provide natural protection against SARS-CoV-2.

17.
Artigo em Inglês | MEDLINE | ID: mdl-34795782

RESUMO

Citrus fruits such as oranges, grapefruits, lemons, limes, tangerines, and mandarins, whose production is increasing every year with the rise of consumer demand, are among the most popular fruits cultivated throughout the globe. Citrus genus belongs to the Rutaceae family and is known for its beneficial effects on health for centuries. These plant groups contain many beneficial nutrients and bioactive compounds. These compounds have antimicrobial, anticancer, antidiabetic, antiplatelet aggregation, and anti-inflammatory activities. Citrus waste, generated by citrus-processing industries in large amounts every year, has an important economic value due to richness of bioactive compounds. The present review paper has summarized the application and properties of Citrus and its waste in some fields such as food and drinks, traditional medicine practices, and recent advances in modern approaches towards pharmaceutical and nutraceutical formulations.

18.
Curr Drug Targets ; 22(5): 488-504, 2021.
Artigo em Inglês | MEDLINE | ID: mdl-33050858

RESUMO

Nature has provided prodigious reservoirs of pharmacologically active compounds for drug development since times. Physcion and physcion 8-O-ß-D-glucopyranoside (PG) are bioactive natural anthraquinones which exert anti-inflammatory and anticancer properties with minimum or no adverse effects. Moreover, physcion also exhibits anti-microbial and hepatoprotective properties, while PG is known to have anti-sepsis as well as ameliorative activities against dementia. This review aims to highlight the natural sources and anticancer activities of physcion and PG, along with associated mechanisms of actions. On the basis of the literature, physcion and PG regulate multitudinous cell signaling pathways through the modulation of various regulators of cell cycle, protein kinases, microRNAs, transcriptional factors, and apoptosis linked proteins resulting in the effective killing of cancerous cells in vitro as well as in vivo. Both compounds effectively suppress metastasis, furthermore, physcion acts as an inhibitor of 6PGD and also plays an important role in chemosensitization. This review article suggests that physcion and PG are potent anticancer drug candidates, but further investigations on their mechanism of action and pre-clinical trials are mandatory in order to comprehend the full potential of these natural cancer killers in anticancer remedies.


Assuntos
Antineoplásicos/farmacologia , Emodina , Neoplasias , Emodina/análogos & derivados , Emodina/farmacologia , Glucosídeos , Humanos , Neoplasias/tratamento farmacológico , Transdução de Sinais
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.
Mycology ; 12(2): 128-138, 2020 Dec 02.
Artigo em Inglês | MEDLINE | ID: mdl-34035978

RESUMO

Octaviania asterosperma (hypogeous Basidiomycota) We investigated the phenolic composition, and antioxidant, antimicrobial and antigenotoxic effects of methanol extracts of fruiting bodies from Octaviania asterosperma. The total phenolic content (ppm) of O. asterosperma was found to be catechin (54.73 ± 4.68), epicatechin (123.90 ± 8.52), caffeic acid (4.23 ± 0.97), p-hydroxybenzoic acid (37.72 ± 3.84), cinnamic acid (58.07 ± 5.40), gallic acid (56.64 ± 6.39), clorogenic acid (80.76 ± 4.92) and coumaric acid (2.45 ± 0.15). The total antioxidant status (TAS), total oxidant status (TOS) and oxidative stress index (OSI) were 3.410 ± 0.099 mmol/L, 7.548 ± 0.147 µmol/L and 0.221 ± 0.005 respectively. O. asterosperma showed some promising antimicrobial activity. The extract showed no genotoxic potential and attenuated hydrogen peroxide (H2O2)-induced oxidative DNA damage in neurons. Pre-treatment with O. asterosperma maintained mitochondrial function, reduced expression levels of cleaved-caspase-3 and apoptosis-inducing factor (AIF) when HT22 cells were exposed to pathophysiological concentrations of GLU (25 mM) and modulated protein kinase B (Akt), the mammalian target of rapamycin (mTOR), and the phosphotase and tensin homolog on chromosome ten (PTEN). O. asterosperma is an important food for the treatment or management of neurodegenerative disorders due to its phenolic content and potent antioxidant and anti-excitotoxic effects.

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