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Sesamol (SM), a well-known component isolated from sesame seeds (Sesamum indicum), used in traditional medicines in treating numerous ailments. However, numerous molecular investigations revealed the various mechanisms behind its activity, emphasizing its antiproliferative, anti-inflammatory, and apoptosis-inducing properties, preventing cancer cell spread to distant organs. In several cells derived from various malignant tissues, SM-regulated signal transduction pathways and cellular targets have been identified. This review paper comprehensively describes the anticancer properties of SM and SM-viable anticancer drugs. Additionally, the interactions of this natural substance with standard anticancer drugs are examined, and the benefits of using nanotechnology in SM applications are explored. This makes SM a prime example of how ethnopharmacological knowledge can be applied to the development of contemporary drugs.
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Benzodioxóis , Fenóis , Humanos , Benzodioxóis/farmacologia , Fenóis/farmacologia , Fenóis/química , Animais , Neoplasias/tratamento farmacológico , Neoplasias/patologia , Neoplasias/metabolismo , Antineoplásicos Fitogênicos/farmacologia , Antineoplásicos Fitogênicos/isolamento & purificação , Antineoplásicos/farmacologia , Antineoplásicos/química , Apoptose/efeitos dos fármacosRESUMO
BACKGROUND: Prunella vulgaris , family Lamiaceae also known as self-heal, has been traditionally used as an expectorant, anti-inflammatory, anti-pyretic, and anti-rheumatic. Due to the widespread distribution of the plant, Vulgaris is also called 'vulgar' in Latin adjective meaning common. OBJECTIVE: The objective of this review was to describe the relevant aspects of phytochemistry and therapeutic uses of different fractions as well as isolated compounds from Prunella vulgaris . An attempt was also made to enumerate the possible leads, e.g . betulinic acid, oleanolic acid, ursolic acid, umbelliferone, scopoletin, esculetin, luteolin, homoorientin, Rosmarinic acid and cinaroside, for further development. METHOD: For peer-reviewed research literature, we undertook a structured search of bibliographic databases using a focused review question. Scientific databases such as PubMed, Scopus, Science Direct, and Google Scholar were searched. RESULTS: Phytochemistry of Prunella vulgaris (PV) after a thorough literature survey revealed varied and copious metabolites, such as triterpenoids, phenolic acid, sterols, carbohydrates, coumarins, fatty acids, and volatile oils. Many of these compounds have been found to possess a wide range of biological activities per se, including anti-microbial, immunosuppressive, anti-cancer, cardio- protective, anti-allergic and anti-inflammatory activities. CONCLUSION: Prunella vulgaris is a medicinal plant of immense medicinal importance having a variety of compounds, such as triterpenoids, phenolic acid, sterols, carbohydrates, coumarins, fatty acids, and volatile oils, and diversity in the pharmacological spectrum. The plant could be further exploited to isolate the various biologically active constituents responsible for its activity.
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Óleos Voláteis , Prunella , Triterpenos , Cumarínicos , Ácidos Graxos , Compostos Fitoquímicos/farmacologia , Compostos Fitoquímicos/uso terapêutico , Extratos Vegetais/farmacologia , Extratos Vegetais/uso terapêutico , Prunella/química , EsteróisRESUMO
Cancer is the leading cause of human disease and death worldwide, accounting for 7.6 million deaths per year and projected to reach 13.1 million by 2030. Many phytochemicals included in traditional medicine have been utilized in the management of cancer. Conventional chemotherapy is generally known to be the most effective treatment of metastatic cancer but these cancerous cells might grow resistant to numerous anticancer drugs over time that resulting in treatment failure. This review tried to portray the advancement in the anticancer and chemopreventive effects of several phytochemicals and some of its members encapsulated in the nano-based delivery system of the drug. It comprises the issue associated with limited use of each phytoconstituents in human cancer treatment are discussed, and the benefits of entrapment into nanocarriers are evaluated in terms of drug loading efficiency, nanocarrier size, release profile of the drug, and in vitro and/or in vivo research and treatment testing, such as cytotoxicity assays and cell inhibition/viability.
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Antineoplásicos/uso terapêutico , Sistemas de Liberação de Fármacos por Nanopartículas/química , Nanopartículas/química , Neoplasias/tratamento farmacológico , Compostos Fitoquímicos/química , Animais , Antineoplásicos/farmacologia , Linhagem Celular Tumoral , Humanos , Lipossomos/química , Nanocápsulas/química , Nanosferas/químicaRESUMO
Individuals with calcium oxalate (CaOx) kidney stones can have secondarily infected calculi which may play a role in the development of recurrent urinary tract infection (UTI). Uropathogenic Escherichia coli (UPEC) is the most common causative pathogen of UTIs. Macrophages play a critical role in host immune defense against bacterial infections. Our previous study demonstrated that oxalate, an important component of the most common type of kidney stone, impairs monocyte cellular bioenergetics and redox homeostasis. The objective of this study was to investigate whether oxalate compromises macrophage metabolism, redox status, anti-bacterial response, and immune response. Monocytes (THP-1, a human monocytic cell line) were exposed to sodium oxalate (soluble oxalate; 50 µM) for 48 hours prior to being differentiated into macrophages. Macrophages were subsequently exposed to calcium oxalate crystals (50 µM) for 48 hours followed by UPEC (MOI 1:2 or 1:5) for 2 hours. Peritoneal macrophages and bone marrow-derived macrophages (BMDM) from C57BL/6 mice were also exposed to oxalate. THP-1 macrophages treated with oxalate had decreased cellular bioenergetics, mitochondrial complex I and IV activity, and ATP levels compared to control cells. In addition, these cells had a significant increase in mitochondrial and total reactive oxygen species levels, mitochondrial gene expression, and pro-inflammatory cytokine (i.e. Interleukin-1ß, IL-1ß and Interleukin-6, IL-6) mRNA levels and secretion. In contrast, oxalate significantly decreased the mRNA levels and secretion of the anti-inflammatory cytokine, Interleukin-10 (IL-10). Further, oxalate increased the bacterial burden of primary macrophages. Our findings demonstrate that oxalate compromises macrophage metabolism, redox homeostasis, and cytokine signaling leading to a reduction in anti-bacterial response and increased infection. These data highlight a novel role of oxalate on macrophage function.
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Metabolismo Energético/efeitos dos fármacos , Homeostase/efeitos dos fármacos , Macrófagos/efeitos dos fármacos , Oxalatos/farmacologia , Trifosfato de Adenosina/biossíntese , Animais , Infecções Bacterianas/imunologia , Citocinas/biossíntese , Humanos , Macrófagos/imunologia , Macrófagos/metabolismo , Masculino , Camundongos , Camundongos Endogâmicos C57BL , Oxirredução , Células THP-1RESUMO
Diet has been associated with several metabolic diseases and may impact immunity. Increased consumption of meals with high oxalate content may stimulate urinary calcium oxalate (CaOx) crystals, which are precursors to CaOx kidney stones. We previously reported that CaOx stone formers have decreased monocyte cellular bioenergetics compared to healthy participants and oxalate reduces monocyte metabolism and redox status in vitro. The purpose of this study was to investigate whether dietary oxalate loading impacts monocyte cellular bioenergetics, mitochondrial complex activity, and inflammatory signaling in humans. Healthy participants (n = 40; 31.1 ± 1.3 years) with a BMI of 24.9 ± 0.6 kg/m2 consumed a controlled low oxalate diet for 3 days before drinking a blended preparation of fruits and vegetables containing a large amount of oxalate. Blood and urine were collected before (pre-oxalate) and for 5 h after the oxalate load to assess urinary oxalate levels, monocyte cellular bioenergetics and mitochondrial complex activity, and plasma cytokine/chemokine levels. Urinary oxalate levels significantly increased in post-oxalate samples compared to pre-oxalate samples. Monocyte cellular bioenergetics, mitochondrial complex I activity, and plasma cytokine and chemokine levels were altered to varying degrees within the study cohort. We demonstrate for the first time that dietary oxalate loading may impact monocyte metabolism and immune response in a cohort of healthy adults, but these response are variable. Further studies are warranted to understand oxalate mediated mechanisms on circulating monocytes and how this potentially influences CaOx kidney stone formation. Clinical Trial Registration: ClinicalTrials.gov, identifier NCT03877276.
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Suplementos Nutricionais , Metabolismo Energético/efeitos dos fármacos , Monócitos/efeitos dos fármacos , Monócitos/metabolismo , Oxalatos/administração & dosagem , Transdução de Sinais/efeitos dos fármacos , Adulto , Biomarcadores , Complexo de Proteínas da Cadeia de Transporte de Elétrons/metabolismo , Feminino , Humanos , Inflamação/etiologia , Inflamação/metabolismo , Inflamação/patologia , Contagem de Leucócitos , Masculino , Mitocôndrias/efeitos dos fármacos , Mitocôndrias/metabolismo , UrináliseRESUMO
BACKGROUND: Inflammation involves a dynamic network that is highly regulated by signals that initiate the inflammation process as well as signals that downregulate it. However, an imbalance between the two leads to tissue damage. Throughout the world, inflammatory disease becomes common in the aging society. The drugs which are used clinically have serious side effects. Natural products or compounds derived from natural products show diversity in structure and play an important role in drug discovery and development. OBJECTIVE: Oreganum Vulgare is used in traditional medicine for various ailments including respiratory and rheumatic disorders, severe cold, suppression of tumors. The current study aims to evaluate the anti-inflammatory potential by evaluating various in vitro parameters. METHODS: Inflammation-induced in macrophages via LPS is the most accepted model for evaluating the antiinflammatory activity of various plant extracts and lead compounds. RESULTS: The extracts (OVEE, OVEAF) as well as the isolated compound(OVRA)of Oreganum Vulgare inhibit the pro-inflammatory cytokines (IL-6 and TNF-α) and NO without affecting cell viability. CONCLUSION: Our study established that the leaf extracts of Oreganum vulgare L. exhibit anti-inflammatory activity and thus confirm its importance in traditional medicine.
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Anti-Inflamatórios/farmacologia , Antioxidantes/farmacologia , Origanum/química , Animais , Anti-Inflamatórios/química , Antioxidantes/química , Sobrevivência Celular/efeitos dos fármacos , Cinamatos/química , Cinamatos/metabolismo , Citocinas/metabolismo , Depsídeos/química , Depsídeos/metabolismo , Dexametasona/química , Dexametasona/metabolismo , Avaliação Pré-Clínica de Medicamentos , Interleucina-1beta/química , Interleucina-1beta/metabolismo , Lipopolissacarídeos/farmacologia , Camundongos , Simulação de Acoplamento Molecular , Óxido Nítrico/metabolismo , Extratos Vegetais/química , Extratos Vegetais/farmacologia , Folhas de Planta/química , Células RAW 264.7 , Fator de Necrose Tumoral alfa/química , Fator de Necrose Tumoral alfa/metabolismo , Ácido RosmarínicoRESUMO
INTRODUCTION: There is significant variation in practices concerning Roux-en-Y gastric bypass (RYGB) among bariatric surgeons, but there is currently a lack of robust data on the nature and extent of these variations. The purpose of this study was to understand global variations in practices concerning RYGB. METHODS: A questionnaire-based survey on Survey Monkey® was created, and the link was shared freely on various social media platforms. The link was also distributed through a personnel email network of authors. RESULTS: A total of 657 surgeons from 65 countries completed the survey. Crohn's disease and liver cirrhosis were considered absolute contraindications for RYGB by 427 surgeons (64.98%) and 347 surgeons (53.30%), respectively. More than 68.5% of surgeons performed routine upper GI endoscopy while 64.17% performed routine ultrasound of abdomen preoperatively. The majority of surgeons (77.70%) used the perigastric technique for Gastric pouch creation. Approximately, 79.5% used orogastric bougie. More than 70% of the respondents did not use any staple line reinforcement routinely. Only 17.67% of surgeons measured the whole small bowel length, and the majority of surgeons (86.5%) used constant length of BP limb. Approximately, 89% used constant length of alimentary limb. Approximately, 95% of surgeons preferred antecolic bypass, and more than 86% routinely closed the Petersen defect. Marginal ulcer prophylaxis was used by the majority (91.17%). Almost 95% of surgeons recommended lifelong vitamin and mineral supplements. CONCLUSION: This survey identifies global variations in practices concerning RYGB. It identifies several areas for future research and consensus building.
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Derivação Gástrica , Obesidade Mórbida , Cirurgiões , Humanos , Obesidade Mórbida/cirurgia , Estômago/cirurgia , Inquéritos e QuestionáriosRESUMO
Heat stress hampers nutrient utilisation and production of animals, and dietary betaine supplementation can mitigate the adverse effects of heat stress on animals and improve their productivity. The present study was conducted to explore the effects of betaine supplementation on the growth performance of eighteen growing Karan Fries (KF) heifers having similar age and body conditions. The experiment was carried out on three groups (nâ¯=â¯6) of KF heifers viz. control, treatment I (betaine supplemented at 25â¯â¯g/d/animal), and treatment II (betaine supplemented at 50â¯â¯g/d/animal). The experiment lasted for eight months covering the three major seasons of Indian tropical conditions viz. hot-dry (temperature humidity index, THIâ¯=â¯83), hot-humid (THIâ¯=â¯85) and thermoneutral season (THIâ¯=â¯73). Blood samples were collected at fortnightly intervals and analysed for plasma growth hormone (GH; competitive ELISA) and total insulin-like growth factor 1 (IGF-1; Sandwich ELISA), as well as expression of IGF-I in peripheral blood mononuclear cells (PBMC) using real-time polymerase chain reaction. Betaine supplementation resulted in significant (pâ¯<â¯0.05) increase in dry matter intake, feed conversion efficiency, body weight gain, plasma GH and IGF-1 levels during all seasons. The concentrations of plasma IGF-1 and the mRNA expression of IGF-1 were higher (pâ¯<â¯0.01) in treatment I as compared to other groups during all seasons. Betaine supplementation at 25â¯â¯g/d/animal was more cost-effective in improving growth performance of heat-stressed heifers as compared to 50â¯â¯g/d/animal. The study suggests that the betaine protects intestinal integrity, enhances nutrient utilisation during heat stress and improves growth performance of growing heifers.
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Betaína/administração & dosagem , Bovinos , Ingestão de Energia/efeitos dos fármacos , Transtornos de Estresse por Calor/dietoterapia , Resposta ao Choque Térmico/efeitos dos fármacos , Fator de Crescimento Insulin-Like I/genética , Aumento de Peso/efeitos dos fármacos , Fenômenos Fisiológicos da Nutrição Animal , Animais , Betaína/farmacologia , Bovinos/genética , Bovinos/crescimento & desenvolvimento , Suplementos Nutricionais , Ingestão de Energia/fisiologia , Feminino , Regulação da Expressão Gênica no Desenvolvimento/efeitos dos fármacos , Crescimento e Desenvolvimento/efeitos dos fármacos , Crescimento e Desenvolvimento/genética , Transtornos de Estresse por Calor/sangue , Transtornos de Estresse por Calor/veterinária , Resposta ao Choque Térmico/fisiologia , Temperatura Alta , Umidade , Fator de Crescimento Insulin-Like I/metabolismo , Leucócitos Mononucleares/efeitos dos fármacos , Leucócitos Mononucleares/metabolismo , Estações do AnoRESUMO
We describe the case of a bladder exstrophy-epispadias complex (BEEC), in which a "split" appendix was used simultaneously as a posterior urethral replacement (for strictured Mitchell's repair) as well as a Mitrofanoff channel. Split appendix had been used before for simultaneous Mitrofanoff and Malone's antegrade contrast enema channels to manage neurogenic bladder and bowel. To the best of our knowledge, this is the first reported case for the use of split appendix for urethral reconstruction in a child with BEEC.
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A large number of patients undergoing bariatric surgery are deficient in copper, and Roux-en-Y gastric bypass can further aggravate it. Delays in diagnosis and treatment of copper deficiency can leave patients with residual neurological disability. This has led to recommendation from the British Obesity and Metabolic Surgery Society that copper levels should be monitored annually after gastric bypass. This review concludes that copper deficiency in adequately supplemented patients is rare and can be adequately treated if a related haematological or neurological disorder is diagnosed. The cost of routine monitoring may therefore not be justified for adequately supplemented, asymptomatic patients who have undergone Roux-en-Y gastric bypass. The screening may however be necessary for high-risk patient groups to prevent severe complications and permanent disability.
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Cobre/deficiência , Derivação Gástrica/efeitos adversos , Obesidade Mórbida/cirurgia , Feminino , Doenças Hematológicas/diagnóstico , Doenças Hematológicas/etiologia , Humanos , Assistência de Longa Duração/métodos , Masculino , Doenças do Sistema Nervoso/diagnóstico , Doenças do Sistema Nervoso/etiologiaRESUMO
Cancer is the second largest leading cause of death worldwide and breast cancer is the most prevailing cause of mortality among all cases of malignant neoplastic disease in adult females. The incidence rate of breast malignant neoplastic disease is predominantly higher in Western women, when compared to women in Asian nations. The definitive reason for this conflict is even unknown, but dietary factors have been conceived to account for approximately 30% of cancers in Western nations. It has been hypothesized that ethnicity, including use of a variety of spices in the food would be a major reason. Among all spices, turmeric (Curcuma longa) has been proven for its better anticancer potential. In this review different molecular mechanisms including cell cycle arrest; G0/G1 and/or G2/M phase cell cycle arrest by up-regulating Cdk inhibitor, p21/WAF/CIPI and p53, inhibition of transcriptional factors; NFκB, AP-1, TNFα, IL, STAT-3, and PPAR-γ, downstream gene regulation; c-myc, Bcl-2, COX-2, NOS, Cyclin D1, TNFα, interleukins and MMP-9, growth factors; bFGF, EGF, GCSF, IL-8, PDGF, TGFα, TNF, VEGF and cell adhesion molecules; fibronectin, vitronectin, and collagen which are involved in angiogenesis and metastasis, alsothe effectiveness of curcumin, when given in combination with chemotherapeutics like cyclophosphamide, doxorubicin, mitomycin etc. in treating breast cancer have been reviewed.
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Protocolos de Quimioterapia Combinada Antineoplásica/uso terapêutico , Neoplasias da Mama/tratamento farmacológico , Curcumina/uso terapêutico , Animais , Neoplasias da Mama/patologia , Ciclo Celular/efeitos dos fármacos , Proliferação de Células/efeitos dos fármacos , Quimioterapia Adjuvante , Feminino , HumanosRESUMO
This study investigated the inhibitory effect of aqueous extract of Trigonella foenum-graecum seeds (AqE-TFG) on fat accumulation and dyslipidemia in high fat diet- (HFD-) induced obese rats. Female Wistar rats were fed with HFD ad libitum, and the rats on HFD were treated orally with AqE-TFG or orlistat ((HFD for 28 days+AqE-TFG (0.5 and 1.0 g/kg) or orlistat (10 mg/kg) from day 8 to 28), respectively. Treatment with AqE-TFG produced significant reduction in body weight gain, body mass index (BMI), white adipose tissue (WAT) weights, blood glucose, serum insulin, lipids, leptin, lipase, and apolipoprotein-B levels and elevation in adiponectin levels. AqE-TFG improved serum aspartate amino transferase (AST), alanine amino transferase (ALT), and lactate dehydrogenase (LDH) levels. AqE-TFG treatment reduced the hepatic and cardiac thiobarbituric acid reactive substances (TBARS) and elevated the antioxidant enzyme (glutathione (GSH), superoxide dismutase (SOD), and catalase (CAT)) levels. In addition, liver and uterine WAT lipogenic enzyme (fatty acid synthetase (FAS) and glucose-6-phosphate dehydrogenase (G6PD)) activities were restored towards normal levels. These findings demonstrated the preventive effect of AqE-TFG on fat accumulation and dyslipidemia, due to inhibition of impaired lipid digestion and absorption, in addition to improvement in glucose and lipid metabolism, enhancement of insulin sensitivity, increased antioxidant defense, and downregulation of lipogenic enzymes.
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Antioxidantes/farmacologia , Dieta Hiperlipídica/efeitos adversos , Dislipidemias/tratamento farmacológico , Extratos Vegetais/farmacologia , Sementes/química , Trigonella/química , Tecido Adiposo Branco , Aminoácidos/química , Animais , Antropometria , Antioxidantes/química , Índice de Massa Corporal , Peso Corporal , Modelos Animais de Doenças , Feminino , Homeostase , Lactonas/uso terapêutico , Obesidade , Orlistate , Estresse Oxidativo , Extratos Vegetais/química , Ratos , Ratos Wistar , Aumento de PesoRESUMO
The emergence of multidrug-resistant and vancomycin-resistant enterococci during the last decade has made it difficult to treat nosocomial infections. Although various enterococcal species have been identified, only two (Enterococcus faecalis and Enterococcus faecium) are responsible for the majority of human infections. Vancomycin is an important therapeutic alternative against multidrug-resistant enterococci but is associated with a poor prognosis. Resistance to vancomycin dramatically reduces the therapeutic options for enterococcal infections. The bacterium develops resistance by modifying the C-terminal d-alanine of peptidoglycan to d-lactate, creating a d-Ala-d-Lac sequence that effectively reduces the affinity of vancomycin for the peptidoglycan by 1000-fold. Moreover, the resistance genes can be transferred from enterococci to Staphylococcus aureus, thereby posing a threat to patient safety and also a challenge for treating physicians. Judicious use of vancomycin and broad-spectrum antibiotics must be implemented, but strict infection control measures must also be followed to prevent nosocomial transmission of these organisms. Furthermore, improvements in clinical practice, rotation of antibiotics, herbal drugs, nanoantibiotics and the development of newer antibiotics based on a pharmacogenomic approach may prove helpful to overcome dreadful vancomycin-resistant enterococcal infections.
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OBJECTIVES: The present study was designed to evaluate the effect of aqueous extract of Trigonella foenum-graecum(AqE-TFG) seeds on monosodium glutamate (MSG)-induced dyslipidemia and oxidative stress in Wistar rats. MATERIALS AND METHODS: Neonatal Wistar rats were treated subcutaneously with MSG (4 g/kg b.w.) from day 2 to 14 after birth, on alternate days. After attaining six-weeks of age, MSG-treated rats were administered with AqE-TFG (0.5 and 1 g/kg b.w., orally) or orlistat (10 mg/kg b.w., orally) for 28 days, respectively. Serum chemistry and relevant enzymes in hepato-cardiac tissues were assessed on day 29. RESULTS: AqE-TFG produced significant reduction in serum total cholesterol (TC), triglycerides (TGs), lactate dehydrogenase (LDH), aspartate amino transferase (AST), alanine amino transferase (ALT), hepatic and cardiac lipid peroxides (MDA) levels and elevation in serum high density lipoprotein cholesterol (HDL-C), hepatic and cardiac antioxidant enzymes [glutathione (GSH), and superoxide dismutase (SOD) and catalase (CAT)] levels. CONCLUSION: Results were comparable with orlistat, a standard anti-obesity drug, and provide clear evidence that the AqE-TFG treatment offered significant protection against MSG-induced dyslipidemia and oxidative stress, and may play an important role in amelioration of the free radical generated consequences like dyslipidemia and atherosclerosis.
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Fármacos Antiobesidade/farmacologia , Dislipidemias/induzido quimicamente , Estresse Oxidativo/efeitos dos fármacos , Extratos Vegetais/farmacologia , Sementes/metabolismo , Glutamato de Sódio/efeitos adversos , Trigonella/química , Animais , Fármacos Antiobesidade/metabolismo , Biomarcadores/metabolismo , Colesterol/sangue , Aromatizantes , Lactonas/farmacologia , Orlistate , Extratos Vegetais/metabolismo , Ratos , Ratos Wistar , Sementes/química , Triglicerídeos/sangueRESUMO
BACKGROUND AND OBJECTIVES: Because of the developing resistance of Mycobacterium species against currently available anti-mycobacterial drugs, there is an urgent need for new drug development. In this study, we have evaluated the in vitro anti-mycobacterial activity of Plumeria bicolor extract and its phytoconstituents - plumericin and isoplumericin against multi-drug resistance Mycobacterium tuberculosis. METHODS: The in vitro anti-mycobacterial activity of chloroform extract of P. bicolor, plumericin and isoplumericin were tested against M. tuberculosis (H37Rv) and four multi-drug resistant (MDR) clinical isolates by measuring the minimum inhibitory concentration (MIC) using MTT (Tetrazolium bromide [3-(4, 5-dimethylthiazol-2-yl)-2,5-diphenyl-tetrazolium bromide]) assay. The extract and both compounds were further evaluated by standard assay procedures to determine their minimum bactericidal concentration (MBC). Cytotoxicity of these compounds was performed against J774G8 murine macrophage cell lines. The activity was represented in the mean (±SD) of duplicate samples from three independent assays. RESULTS: Plumericin showed better activity against pan sensitive as well as four MDR strains of M. tuberculosis with MIC values of 2.1 ± 0.12, 1.3 ± 0.15, 2.0 ± 0.07, 1.5 ± 0.13 & 2.0 ± 0.14 µg/mL and MBC values of 3.6 ± 0.22, 2.5 ± 0.18, 3.8 ± 0.27, 2.9 ± 0.20 & 3.7 ± 0.32 µg/mL than isoplumericin, respectively. Interestingly, both isolated active compounds showed an advantage over rifampicin (80 times) and isoniazid (8 times) by being highly active against the MDR strains. The extract and both compounds were found to be non-toxic against J774G8 macrophages up to the used concentrations. CONCLUSION: Plumericin showed more potent activity than isoplumericin. The excellent activity of these compounds against MDR strains opens a possibility of obtaining new anti-mycobacterial drug candidate in near future.
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Antituberculosos/farmacologia , Indenos/farmacologia , Iridoides/farmacologia , Mycobacterium tuberculosis , Tuberculose Resistente a Múltiplos Medicamentos/tratamento farmacológico , Animais , Antituberculosos/química , Antituberculosos/toxicidade , Apocynaceae , Linhagem Celular , Relação Dose-Resposta a Droga , Humanos , Indenos/química , Indenos/toxicidade , Iridoides/química , Iridoides/toxicidade , Testes de Sensibilidade Microbiana , Extratos VegetaisRESUMO
BACKGROUND: Grewia asiatica Linn. (Family: Tiliaceae), called Phalsa in Hindi is an Indian medicinal plant used for a variety of therapeutic and nutritional uses. The root bark of the plant is traditionally used in rheumatism (painful chronic inflammatory condition). AIMS: The present study demonstrates the analgesic and anti-inflammatory activity of root bark of G. asiatica in rodents. SETTINGS AND DESIGN: The methanolic extract of Grewia asiatica (MEGA) and aqueous extract of Grewia asiatica (AEGA) of the bark were prepared and subjected to phytochemical tests and pharmacological screening for analgesic and anti-inflammatory effect in rodents. MATERIALS AND METHODS: Analgesic effect was studied using acetic acid-induced writhing in mice and hot plate analgesia in rats while anti-inflammatory activity was investigated using carrageenan-induced paw oedema in rats. The MEGA or AEGA was administered orally in doses of 200 and 400 mg/kg/day of body weight. STATISTICAL ANALYSIS: Data were analysed by one-way analysis of variance followed by Dunnett's test. RESULTS: The extracts showed a significant inhibition of writhing response and increase in hot plate reaction time and also caused a decrease in paw oedema. The effects were comparable with the standard drugs used. CONCLUSIONS: The present study indicates that root bark of G. asiatica exhibits peripheral and central analgesic effect and anti-inflammatory activity, which may be attributed to the various phytochemicals present in root bark of G. asiatica.
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A randomized, double-blind, placebo-controlled study was conducted to evaluate the efficacy of OciBest, an extract of Ocimum tenuiflorum Linn. in symptomatic control of general stress. The participants received either placebo (n = 79) or OciBest (n = 71; 1200 mg of actives per day) for six weeks. The severity of stress-related symptoms was self-evaluated by patients at weeks 0, 2, 4 and 6 of the trial period using a symptom rating scale. After six weeks of intervention, scores of symptoms such as forgetfulness, sexual problems of recent origin, frequent feeling of exhaustion, and frequent sleep problems of recent origin decreased significantly (P ≤ 0.05) in OciBest group as compared with placebo group. Also, the total symptom scores of OciBest group revealed significant reduction (P ≤ 0.05) as compared to placebo group. The overall improvement in OciBest group was found to be 1.6 times or 39% more in the control of general stress symptoms with respect to placebo. No adverse events were reported during the study. The findings revealed that OciBest was found to be effective and well tolerated by all the patients over the six weeks of study period.
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BACKGROUND & OBJECTIVES: The severe toxicity, exorbitant cost and emerging resistance of Leishmania species against most of the currently used drugs underscores the urgent need for the alternative drugs. The present study evaluates in vitro anti-leishmanial activity of Plumeria bicolor and its isolated compounds. METHODS: The in vitro anti-parasitic activity of chloroform extract of Plumeria bicolor, plumericin and isoplumericin were tested alongwith appropriate controls against promastigote and amastigote forms of Leishmania donovani using 96 well microtiter plate. The concentration used for assessing the anti-leishmanial activity of extract of Plumeria bicolor and both isolated compounds were 100 µg/ml and 15 µM, respectively. The viability of the cells was assessed by MTT assay. The cytotoxicity of these compounds was performed against J774G8 murine macrophage cells lines at the concentration of 30 µM. RESULTS: The Plumeria bicolor extract showed activity with the IC 50 of 21±2.2 and 14±1.6 µg/ml against promastigote and amastigote forms of L. donovani, respectively. Plumericin consistently showed high activity with the IC 50 of 3.17±0.12 and 1.41±0.03 µM whereas isoplumericin showed the IC50 of 7.2±0.08 µM and 4.1±0.02 µM against promastigote and amastigote forms, respectively. Cytotoxic effect of the chloroform extract of P. bicolor, plumericin and isoplumericin was evaluated in murine macrophage (J774G8) model with CC50 value of 75±5.3 µg/ml, 20.6±0.5 and 24±0.7 µM, respectively. INTERPRETATION & CONCLUSIONS: Our results indicated that plumericin showed more potent activity than isoplumericin and might be a promising anti-leishmanial agent against L. donovani.
Assuntos
Antiparasitários/farmacologia , Indenos/farmacologia , Iridoides/farmacologia , Leishmania donovani/efeitos dos fármacos , Extratos Vegetais/farmacologia , Animais , Apocynaceae/química , Linhagem Celular , Humanos , Concentração Inibidora 50 , Leishmania/efeitos dos fármacos , Leishmania/parasitologia , Leishmania donovani/patogenicidade , Macrófagos/citologia , CamundongosRESUMO
This study evaluated the in vitro antifungal activity of the chloroform extract of Plumeria bicolor and its phytoconstituents plumericin and isoplumericin against Candida species and Cryptococcus neoformans by measuring the Minimum Inhibitory Concentration (MIC) and Minimum Fungicidal Concentration (MFC). Plumericin's consistently high activity against Candida albicans, C. krusei, C. glabrata, C. tropicalis and Cryptococcus neoformans was more potent than isoplumericin and the standard antifungal drug nystatin suggesting its potential as a drug candidate for candidiasis and cryptococcosis.