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1.
Gene ; 897: 148081, 2024 Mar 01.
Artículo en Inglés | MEDLINE | ID: mdl-38101713

RESUMEN

Azadiradione is a small bioactive limonoid found in the seed of Azadirachta Indica, an Indian medicinal plant commonly known as Neem. Recently, it has been shown to ameliorate the disease pathology in fly and mouse model of Huntington's disease by restoring impaired proteostasis. Here we report that the azadiradione could be involved in modulating the synaptic function through increased expression of Ube3a, a dual function protein having ubiquitin ligase and co-activator functions and associated with Angelman syndrome and autism. Treatment of azadiradione to HT22 hippocampal cell line and in adult mice induced the expression of Ube3a as well as two important synaptic function and plasticity regulating proteins, parvalbumin and brain-derived neurotropic factor (BDNF). Interestingly, another synaptic plasticity modulating protein Arc (activity-regulated cytoskeletal associated protein) was down-regulated by azadiradione. Partial knockdown of Ube3a in HT22 cell abrogated azadiradione induced expression of parvalbumin and BDNF. Ube3a-maternal deficient mice also exhibited significantly decreased expression of parvalbumin and BDNF in their brain and treatment of azadiradione in these animals did not rescue the altered expression of either parvalbumin or BDNF. These results indicate that azadiradione-induced expression of parvalbumin and BDNF in the brain is mediated through Ube3a and suggest that azadiradione could be implicated in restoring synaptic dysfunction in many neuropsychiatric/neurodegenerative disorders.


Asunto(s)
Síndrome de Angelman , Limoninas , Ratones , Animales , Limoninas/farmacología , Factor Neurotrófico Derivado del Encéfalo/genética , Factor Neurotrófico Derivado del Encéfalo/metabolismo , Parvalbúminas/metabolismo , Ubiquitina-Proteína Ligasas/genética , Ubiquitina-Proteína Ligasas/metabolismo , Encéfalo/metabolismo , Síndrome de Angelman/genética , Síndrome de Angelman/metabolismo , Síndrome de Angelman/patología , Modelos Animales de Enfermedad
3.
Adv Exp Med Biol ; 1391: 137-159, 2022.
Artículo en Inglés | MEDLINE | ID: mdl-36472821

RESUMEN

Infertility is a universal health problem affecting 15% of couples, out of which 20-30% cases are due to male infertility. The leading causes of male infertility include hormonal defects, physical reasons, sexual problems, hazardous environment, stressful lifestyle, genetic factors, epigenetic factors, and oxidative stress. Various physiological functions involve reactive oxygen species (ROS) and nitrogen species at appropriate levels for proper smooth functioning. ROS control critical reproductive processes such as capacitation, acrosomal reaction, hyperactivation, egg penetration, and sperm head decondensation. The excessive free radicals or imbalance between ROS and endogenous antioxidant enzymes damages sperm membrane by inducing lipid peroxidation causing mitochondrial dysfunction and DNA damage that eventually lead to male infertility. Numerous synthetic products are available in the market to treat infertility problems, largely ending in side effects and repressing symptoms. Ayurveda contains a particular group of Rasayana herbs, called vajikarana, that deals with nourishment and stimulation of sexual tissues, improves male reproductive vitality, and deals with oxidative stress via antioxidant mechanism. The present study aims to describe oxidative stress and the role of herbal drugs in treating male infertility.


Asunto(s)
Infertilidad Masculina , Semen , Masculino , Humanos , Medicina Ayurvédica , Epigenómica , Infertilidad Masculina/tratamiento farmacológico , Estrés Oxidativo
5.
J Ethnopharmacol ; 292: 115178, 2022 Jun 28.
Artículo en Inglés | MEDLINE | ID: mdl-35278608

RESUMEN

ETHNOPHARMACOLOGICAL RELEVANCE: Renal disease is a significant public health concern that affects people all over the world. The main limitations of conventional therapy are the adverse reaction on human health and the expensive cost of drugs. Indeed, it is necessary to develop new therapeutic strategies that are less expensive and have fewer side effects. As a consequence of their natural compounds, medicinal plants can be used as an alternative therapy to cure various ailments including kidney diseases. OBJECTIVE: of the study: This review paper has two principal goals: (1) to inventory and describe the plants and their ancestral use by Moroccan society to cure renal problems, (2) to link traditional use with scientific confirmations (preclinical and clinical). METHODS: To analyze pharmacological effects, phytochemical, and clinical trials of plants, selected for renal therapy, a bibliographical search was undertaken by examining ethnobotanical investigations conducted in Morocco between 1991 and 2019 and consulting peer-reviewed papers from all over the world. RESULTS: Approximately 290 plant species, spanning 81 families and 218 genera have been reported as being utilized by Moroccans to manage renal illness. The most frequently mentioned species in Morocco were Herniaria hirsuta subsp. cinerea (DC.), Petroselinum crispum (Mill.) Fuss and Rosmarinus officinalis L. The leaves were the most frequently used plant parts, followed by the whole plant. Decoction and infusion were the most popular methods of preparation. A record of 71 plant species was studied in vitro and/or in vivo for their therapeutic efficacy against kidney disorders, including 10 plants attempting to make it to the clinical stage. Twenty compounds obtained from 15 plants have been studied for the treatment of kidney diseases. CONCLUSION: Medicinal herbs could be a credible alternative therapy for renal illness. However, additional controlled trials are required to confirm their efficiency in patients with kidney failure. Overall, this work could be used as a database for future exploration.


Asunto(s)
Plantas Medicinales , Insuficiencia Renal , Etnobotánica , Etnofarmacología , Femenino , Conocimientos, Actitudes y Práctica en Salud , Humanos , Masculino , Medicina Tradicional/métodos , Fitoquímicos/uso terapéutico , Fitoterapia/métodos , Plantas Medicinales/química
6.
J Ethnopharmacol ; 283: 114666, 2022 Jan 30.
Artículo en Inglés | MEDLINE | ID: mdl-34592338

RESUMEN

ETHNOPHARMACOLOGICAL RELEVANCE: Ervatamia coronaria, a popular garden plant in India and some other parts of the world is known traditionally for its anti-inflammatory and anti-cancer properties. The molecular bases of these functions remain poorly understood. AIM OF THE STUDY: Efficacies of the existing therapies for colorectal cancer (CRC) are limited by their life-threatening side effects and unaffordability. Therefore, identifying a safer, efficient, and affordable therapeutic is urgent. We studied the anti-CRC activity of an alkaloid-rich fraction of E. coronaria leaf extracts (AFE) and associated underlying mechanism. MATERIALS AND METHODS: Activity guided solvant fractionation was adopted to identify the activity in AFE. Different cell lines, and tumor grown in syngeneic mice were used to understand the anti-CRC effect. Methodologies such as LCMS, MTT, RT-qPCR, immunoblot, immunohistochemistry were employed to understand the molecular basis of its activity. RESULTS: We showed that AFE, which carries about six major compounds, is highly toxic to colorectal cancer (CRC) cells. AFE induced cell cycle arrest at G1 phase and p21 and p27 genes, while those of CDK2, CDK-4, cyclin-D, and cyclin-E genes were downregulated in HCT116 cells. It predominantly induced apoptosis in HCT116p53+/+ cells while the HCT116p53-/- cells under the same treatment condition died by autophagy. Notably, AFE induced upregulation of AMPK phosphorylation, and inhibition of both of the mTOR complexes as indicated by inhibition of phosphorylation of S6K1, 4EBP1, and AKT. Furthermore, AFE inhibited mTOR-driven conversion of cells from reversible cell cycle arrest to senescence (geroconversion) as well as ERK activity. AFE activity was independent of ROS produced, and did not primarily target the cellular DNA or cytoskeleton. AFE also efficiently regressed CT26-derived solid tumor in Balb/c mice acting alone or in synergy with 5FU through inducing autophagy as a major mechanism of action as indicated by upregulation of Beclin 1 and phospho-AMPK, and inhibition of phospho-S6K1 levels in the tumor tissue lysates. CONCLUSION: AFE induced CRC death through activation of both apoptotic and autophagy pathways without affecting the normal cells. This study provided a logical basis for consideration of AFE in future therapy regimen to overcome the limitations associated with existing anti-CRC chemotherapy.


Asunto(s)
Alcaloides/farmacología , Antineoplásicos Fitogénicos/farmacología , Neoplasias Colorrectales/tratamiento farmacológico , Tabernaemontana/química , Proteínas Quinasas Activadas por AMP/metabolismo , Alcaloides/aislamiento & purificación , Animales , Antineoplásicos Fitogénicos/aislamiento & purificación , Apoptosis/efectos de los fármacos , Autofagia/efectos de los fármacos , Puntos de Control del Ciclo Celular/efectos de los fármacos , Células HCT116 , Células HT29 , Humanos , Masculino , Ratones , Ratones Endogámicos BALB C , Transducción de Señal/efectos de los fármacos , Serina-Treonina Quinasas TOR/metabolismo , Ensayos Antitumor por Modelo de Xenoinjerto
7.
J Tradit Complement Med ; 9(2): 106-118, 2019 Apr.
Artículo en Inglés | MEDLINE | ID: mdl-30963045

RESUMEN

Diospyros melanoxylon Roxb. (D. melanoxylon) belongs to the family Ebenaceae and its leaves are very well known for making beedi throughout the World. The current study estimated the comparative extraction technique and its in-vitro antidiabetic prospective of the leaves of D. melanoxylon. Qualitative phytochemicals analysis of the samples from D. melanoxylon was carried out for the detection of secondary metabolites. Total phenolics, flavonoids, triterpenoids and tannins content of D. melanoxylon were estimated using colorimetric assay. Microwave-assisted extraction (MAE) technique with a low carbon output was observed for the speedy extraction of bioactive compounds obtained from Diospyros melanoxylon leaf extract. MAE produced a maximum yield of bioactive compounds which was found to be more efficient than ultrasound, soxhlet and maceration extraction. Qualitative HPLC analysis was performed for bioactive compounds. The in-vitro antidiabetic assay was performed using α-amylase and α-glucosidase inhibitory activity. In conclusion, the fractions exhibited the concentration-dependent inhibitory effect with significant (P < 0.0001) result. So the above performance might be accountable for the antidiabetic activity of D. Melanoxylon leaf extract due to presence of bioactive compounds.

8.
Steroids ; 139: 18-27, 2018 11.
Artículo en Inglés | MEDLINE | ID: mdl-30217788

RESUMEN

Ichnocarpus frutescens, a climber plant, is distributed all over India. As its different parts are used as anti-inflammatory agent, so we re-investigated the roots to isolate compounds and evaluate its biological efficacy. Also, in-silico molecular docking was carried out to elucidate the structure activity relationship (SAR) of isolated compounds toward identifies the drug target enzyme with validation, which was further supported by anti-inflammatory in-vitro and in-vivo experimental models. The compounds have been undertaken mainly to investigate the anti-inflammatory and analgesic efficacy along with molecular docking investigation followed by anti-proteinase, anti-denaturation and cyclooxygenase (COX) inhibition studies. Inflammatory cytokines like TNF-α and IL-6 were assayed from lipopolysaccharides (LPS) and Concavallin (CON A) stimulated human PBMC derived macrophages by Enyme linked immune sorbent assay (ELISA) method. The purity index of the lead compound was determined by HPLC. The compounds were illustrated as 2-hydroxy tricosanoic acid (1), stigmasterol glucoside (2), stigmasterol (3), ß-sitosterol (4) and ß-sitosterol glucoside (5). The test molecules showed significant anti-denaturation, anti-proteinase and analgesic effect validated with docking study. Compounds exhibited anti-inflammatory and pain killing action due to dexamethasone like phytosterol property. Promising anti-denaturation and anti-proteinase activity offered by the compound 5, may hold its promise to fight against arthritis by rejuvenating the osteoblast cells and destroying the bone-resorpting complex of hydrated protein, bone minerals by secreting the acid and an enzyme collagenase along with pain management. The lead bioactive compound i.e. ß-sitosterol glucoside (compound 5) demonstrated considerable anti-inflammatory activity showing more than 90% protection against the inflammatory cytokines at 50 µM dose. The anti-denaturation and COX-2 inhibition shown by the compound 5 was also noteworthy with the significant IC50 (ranging from 0.25 to 2.56 µM) that also supporting its future promise for developing as anti-inflammatory agent. Since the most bio-active compound (5) elicit promising acute anti-inflammatory action and peripheral anti-nociceptive pain killing action with a significant ED50 dose of 3.95 & 2.84 mg/kg i.p. respectively in the in-vivo animal model. It could suggest its potentiality as a good in-vivo bio available agent to be an emerging anti-inflammatory drug regimen scaffold in the future. It also establishes significant in-vitro and in-vivo result co-relation. Therefore, the compound 5 could be believed as a potent lead for designing anti-inflammatory, anti-arthritic drug or pain killer without showing any untoward effect.


Asunto(s)
Apocynaceae/química , Inflamación/tratamiento farmacológico , Dolor Nociceptivo/tratamiento farmacológico , Esteroides/administración & dosificación , Analgésicos/farmacología , Antiinflamatorios/farmacología , Citocinas/metabolismo , Ácidos Grasos Insaturados/química , Ácidos Grasos Insaturados/aislamiento & purificación , Glucósidos/química , Glucósidos/aislamiento & purificación , Humanos , Inflamación/patología , Interleucina-6/genética , Leucocitos Mononucleares/efectos de los fármacos , Lipopolisacáridos/química , Macrófagos/efectos de los fármacos , Simulación del Acoplamiento Molecular , Dolor Nociceptivo/patología , Percepción del Dolor/efectos de los fármacos , Extractos Vegetales/química , Extractos Vegetales/farmacología , Raíces de Plantas/química , Sitoesteroles/química , Sitoesteroles/aislamiento & purificación , Esteroides/química , Esteroides/aislamiento & purificación , Estigmasterol/análogos & derivados , Estigmasterol/química , Estigmasterol/aislamiento & purificación , Factor de Necrosis Tumoral alfa/genética
9.
Inflammopharmacology ; 26(1): 235-250, 2018 Feb.
Artículo en Inglés | MEDLINE | ID: mdl-29063488

RESUMEN

The plant Euphorbia tirucalli Linn has been successfully used as a tribal folk medicine in India and Africa for the management of acute inflammatory, arthritic, nociceptive pain and asthmatic symptoms. The present study was conducted to assess the anti-inflammatory, analgesic, anti-asthmatic and anti-arthritic role of the total steroid and terpenoid rich fractions of the hydro-alcoholic extract of E. tirucalli root (STF-HAETR). STF-HAETR fraction demonstrated 71.25 ± 2.5 and 74.25 ± 5.1% protection against acetic acid-induced pain and central neuropathic pain at 75 and 100 mg/kg doses, respectively. It showed 96.97% protection against acute inflammation at 100 mg/kg with 1.6-fold better activity than the standard drug. The fraction exhibited such efficacy via inhibition of proinflammatory cytokines TNF-α, IFN-γ, by 61.12 and 65.18%, respectively, at 100 µg/mL. Inhibition of cyclooxygenase and Nitric oxide synthase in a dose-dependent manner affirms its analgesic and anti-inflammatory activity. The spectrophotometric analysis reveals that STF-HAETR induces ameliorative effect against heat-induced denaturation of Bovine serum albumin (BSA) and exhibits significant anti-proteinase activity. The plant fraction also demonstrated anti-asthmatic activity by displaying 62.45% protection against histamine induced bronchoconstriction or dyspnoea. Our findings suggest that STF-HAETR could be an effective safe therapeutic agent to treat nociceptive pain, acute inflammation, asthma, and arthritis which may authenticate its traditional use.


Asunto(s)
Antiinflamatorios/farmacología , Euphorbia/química , Inflamación/tratamiento farmacológico , Dolor Nociceptivo/tratamiento farmacológico , Raíces de Plantas/química , Esteroides/farmacología , Terpenos/farmacología , Ácido Acético/farmacología , Analgésicos/farmacología , Animales , Artritis/tratamiento farmacológico , Artritis/metabolismo , Línea Celular Tumoral , Citocinas/metabolismo , Edema/tratamiento farmacológico , Edema/metabolismo , Femenino , Inflamación/metabolismo , Masculino , Medicina Tradicional/métodos , Ratones , Óxido Nítrico/metabolismo , Óxido Nítrico Sintasa/metabolismo , Dolor Nociceptivo/metabolismo , Fitoterapia/métodos , Extractos Vegetales/farmacología , Prostaglandina-Endoperóxido Sintasas/metabolismo , Células RAW 264.7 , Ratas
10.
Oncotarget ; 7(48): 78281-78296, 2016 Nov 29.
Artículo en Inglés | MEDLINE | ID: mdl-27835876

RESUMEN

Aggregation of proteins with the expansion of polyglutamine tracts in the brain underlies progressive genetic neurodegenerative diseases (NDs) like Huntington's disease and spinocerebellar ataxias (SCA). An insensitive cellular proteotoxic stress response to non-native protein oligomers is common in such conditions. Indeed, upregulation of heat shock factor 1 (HSF1) function and its target protein chaperone expression has shown promising results in animal models of NDs. Using an HSF1 sensitive cell based reporter screening, we have isolated azadiradione (AZD) from the methanolic extract of seeds of Azadirachta indica, a plant known for its multifarious medicinal properties. We show that AZD ameliorates toxicity due to protein aggregation in cell and fly models of polyglutamine expansion diseases to a great extent. All these effects are correlated with activation of HSF1 function and expression of its target protein chaperone genes. Notably, HSF1 activation by AZD is independent of cellular HSP90 or proteasome function. Furthermore, we show that AZD directly interacts with purified human HSF1 with high specificity, and facilitates binding of HSF1 to its recognition sequence with higher affinity. These unique findings qualify AZD as an ideal lead molecule for consideration for drug development against NDs that affect millions worldwide.


Asunto(s)
ADN/metabolismo , Proteínas de Drosophila/metabolismo , Drosophila melanogaster/metabolismo , Factores de Transcripción del Choque Térmico/metabolismo , Limoninas/farmacología , Enfermedades Neurodegenerativas/prevención & control , Fármacos Neuroprotectores/farmacología , Péptidos/metabolismo , Extractos Vegetales/farmacología , Agregación Patológica de Proteínas , Animales , Azadirachta/química , ADN/genética , Modelos Animales de Enfermedad , Relación Dosis-Respuesta a Droga , Proteínas de Drosophila/genética , Drosophila melanogaster/genética , Células HCT116 , Células HEK293 , Factores de Transcripción del Choque Térmico/genética , Humanos , Limoninas/aislamiento & purificación , Limoninas/metabolismo , Enfermedades Neurodegenerativas/genética , Enfermedades Neurodegenerativas/metabolismo , Enfermedades Neurodegenerativas/patología , Fármacos Neuroprotectores/aislamiento & purificación , Fármacos Neuroprotectores/metabolismo , Extractos Vegetales/aislamiento & purificación , Extractos Vegetales/metabolismo , Unión Proteica , Semillas , Factores de Tiempo , Transfección
11.
Int Immunopharmacol ; 41: 106-115, 2016 Dec.
Artículo en Inglés | MEDLINE | ID: mdl-27838586

RESUMEN

The plant Euphorbia neriifolia Linn has been successfully used for the management of acute inflammatory, arthritic, nociceptive pain and relieves the asthmatic symptom as a tribal folk medicine in India. The present study was conducted to evaluate the anti-inflammatory, analgesic, anti-arthritic activity from total steroid and terpenoid rich fractions derived from hydro-alcoholic extract of Euphorbia neriifolia stem (STF-HAENS). STF-HAENS fraction demonstrated 68.58±2.5% and 75.25±5.1% protection against acetic acid-induced pain and central neuropathic pain at 80mg/kg. It also showed 98.47% protection against acute inflammation at 100mg/kg with 1.7 fold higher protective activity than the standard drug. The fraction exhibited this efficacy via inhibition of proinflammatory cytokines TNF-α, IFN-γ, IL-12 and IL-6 by 74%, 81.26%, 92.10% and 93.4% respectively at 100µg/ml. It also showed dual inhibition of cyclooxygenase (COX) and lipooxygenase (LOX) activity in a dose-dependent manner that elicited the desired pharmacological action. The fraction downregulated nitric-oxide production from lipopolysaccharide (LPS) stimulated PBMC derived macrophages. The spectrophotometric analysis reveals the STF-HAENS induced ameliorative effect against heat-induced denaturation of BSA protein and exhibited significant antiproteinase activity. Our findings suggest that STF-HAENS could be used as an effective safe therapeutic agent for treatment of nociceptive pain, acute inflammation and arthritis.


Asunto(s)
Analgésicos/uso terapéutico , Antiinflamatorios/uso terapéutico , Artritis/tratamiento farmacológico , Euphorbia , Dolor Nociceptivo/tratamiento farmacológico , Extractos Vegetales/uso terapéutico , Ácido Acético , Analgésicos/análisis , Analgésicos/farmacología , Analgésicos/toxicidad , Animales , Antiinflamatorios/análisis , Antiinflamatorios/farmacología , Antiinflamatorios/toxicidad , Araquidonato 12-Lipooxigenasa/metabolismo , Artritis/inducido químicamente , Artritis/patología , Carragenina , Células Cultivadas , Citocinas/antagonistas & inhibidores , Citocinas/metabolismo , Femenino , Calor , Humanos , Lipopolisacáridos/farmacología , Pulmón/efectos de los fármacos , Pulmón/metabolismo , Macrófagos/efectos de los fármacos , Macrófagos/metabolismo , Masculino , Óxido Nítrico/metabolismo , Óxido Nítrico Sintasa de Tipo II/metabolismo , Dolor Nociceptivo/inducido químicamente , Fitoquímicos/análisis , Fitoquímicos/farmacología , Fitoquímicos/uso terapéutico , Fitoquímicos/toxicidad , Fitoterapia , Extractos Vegetales/análisis , Extractos Vegetales/farmacología , Extractos Vegetales/toxicidad , Tallos de la Planta , Ratas Wistar , Esteroides/análisis , Esteroides/farmacología , Esteroides/uso terapéutico , Esteroides/toxicidad , Terpenos/análisis , Terpenos/farmacología , Terpenos/uso terapéutico , Terpenos/toxicidad
12.
J Acupunct Meridian Stud ; 9(3): 109-17, 2016 Jun.
Artículo en Inglés | MEDLINE | ID: mdl-27342884

RESUMEN

A predominant number of diseases affecting women are related to female hormones. In most of the cases, these diseases are reported to be associated with menstrual problems. These diseases affect female reproductive organs such as the breast, uterus, and ovaries. Estrogen is the main hormone responsible for the menstrual cycle, so irregular menstruation is primarily due to a disturbance in estrogen levels. Estrogen imbalance leads to various pathological conditions in premenopausal women, such as endometriosis, breast cancer, colorectal cancer, prostate cancer, poly cysts, intrahepatic cholestasis of pregnancy, osteoporosis, cardiovascular diseases, obesity, etc. In this review, we discuss common drug targets and therapeutic strategies, including acupuncture and compounds of natural origin, for the treatment of diseases caused by estrogen deficiency.


Asunto(s)
Terapia por Acupuntura , Estrógenos/deficiencia , Femenino , Humanos , Salud de la Mujer
13.
Curr Pharm Des ; 22(2): 247-64, 2016.
Artículo en Inglés | MEDLINE | ID: mdl-26561064

RESUMEN

Diseases associated with chronic inflammatory pathology claim a major share of worldwide deaths each year. A principal reason behind the huge number of casualties is associated with mild or unnoticed symptoms for long period of time since the outset, and that specific treatment options for these diseases have not yet emerged. Current anti-inflammatory drugs essentially have become ineffective for long term protection from these diseases as they also interfere with essential cellular pathways and associated toxicities. Notably, recent studies with a number of phytochemicals have shown promising results. These compounds isolated from various medicinal plants express their anti-inflammatory activities by down regulating expression of several crucial pro-inflammatory mediators. These are mostly antioxidants; inhibit induction of key transcription factors like nuclear factor kappa B (NF-κB) that are responsible for expression of proinflammatory mediators, and other growth regulators. Definitely, some of these compounds have the potential to be developed into new therapeutic agents to better control inflammation associated diseases in near future. This review summarizes recent findings on the molecular mechanisms through which various inflammatory activities are linked to disease progression and a group of natural products that have shown promise in controlling these processes.


Asunto(s)
Antiinflamatorios/administración & dosificación , Inflamación/prevención & control , Fitoterapia , Enfermedad Crónica/prevención & control , Suplementos Dietéticos , Humanos
14.
Pharm Biol ; 53(9): 1379-85, 2015.
Artículo en Inglés | MEDLINE | ID: mdl-25858438

RESUMEN

CONTEXT: Thespesia populnea Sol. ex Correa (Malvaceae), an indigenous tree species in India, is of interest to researchers because traditionally its heartwood is used in the treatment of ulcer and colic pain. OBJECTIVE: To validate its folk use in the treatment of ulcerative colitis (UC). MATERIALS AND METHODS: Mice were administered intrarectal DNBS and then treated with different plant extracts (100 and 200 mg/kg), 30 min before and 24 and 48 h after DNBS infusion. Colonic mucosal injury was assessed by macroscopic and histological examination. Furthermore, malondialdehyde (MDA), myeloperoxidase (MPO), protease, and hemoglobin (Hb) contents were measured in tissue and blood samples. RESULTS: Administration of various extracts ameliorated macroscopic and microscopic scores which were altered due to DNBS treatment in mice. Hb concentration in blood was restored significantly by the aqueous extract to 17.20 ± 0.5, which was reduced to 13.80 ± 0.5 after treatment with DNBS. MDA level was increased to 10.82 nm/mg and 10.25 nm/ml in tissue and blood, respectively, due to DNBS treatment which was reduced to 2.69 nm/mg and 3.59 nm/ml in tissue and blood, respectively, by aqueous extract treatment. Similarly, MPO level was increased to 412 U/mg and 404 U/ml in tissue and blood, respectively, which was significantly reduced to 205 U/mg and 219 U/ml in tissue and blood, respectively, by aqueous extract treatment. Aqueous extract significantly reduced protease activity which was markedly increased in DNBS-treated animals. DISCUSSION AND CONCLUSION: Aqueous extract of heartwood of T. populnea is effective in the treatment of UC.


Asunto(s)
Antiinflamatorios/farmacología , Colitis Ulcerosa/prevención & control , Colon/efectos de los fármacos , Fármacos Gastrointestinales/farmacología , Mucosa Intestinal/efectos de los fármacos , Malvaceae , Extractos Vegetales/farmacología , Animales , Antiinflamatorios/aislamiento & purificación , Biomarcadores/metabolismo , Colitis Ulcerosa/inducido químicamente , Colitis Ulcerosa/metabolismo , Colitis Ulcerosa/patología , Colon/metabolismo , Colon/patología , Sulfato de Dextran , Modelos Animales de Enfermedad , Fármacos Gastrointestinales/aislamiento & purificación , Hemoglobinas/metabolismo , Mucosa Intestinal/metabolismo , Mucosa Intestinal/patología , Masculino , Malondialdehído/metabolismo , Malvaceae/química , Ratones , Péptido Hidrolasas/metabolismo , Peroxidasa/metabolismo , Fitoterapia , Extractos Vegetales/aislamiento & purificación , Plantas Medicinales
15.
J Ethnopharmacol ; 159: 274-84, 2015 Jan 15.
Artículo en Inglés | MEDLINE | ID: mdl-25459447

RESUMEN

ETHNOPHARMACOLOGICAL RELEVANCE: Gelsemium sempervirens (L.) J.St.-Hil is a herb used for the treatment of various neuroses in both homeopathic and Ayurvedic systems. The present study examines whether Gelsemium reconstituted tincture can protect against scopolamine induced cognitive discrepancies in amnesic mouse model. In order to investigate the protective mechanism of Gelsemium against dementia, in vitro acetyl cholinesterase and ß-secretase enzyme inhibition and estimation of glutathione level in mouse brain were carried out. MATERIALS AND METHODS: The inhibition study on acetyl cholinesterase and ß-secretase enzyme was conducted on brain homogenate supernatant spectrophotometrically using specific substrate. Cognitive enhancement activity was assessed by elevated plus maze and passive avoidance study in scopolamine induced dementia mouse model. Glutathione, an anti-oxidant, was measured spectrophotometrically from scopolamine induced amnesic mice brain supernatant using 5,5'-dithiobis 2-nitrobenzoic acid in the presence and absence of Gelsemium tincture. RESULTS: Significant inhibition was found with Gelsemium on AChE and ß-secretase enzyme with an IC50 of 9.25 and 16.25 µg/ml, respectively, followed by increasing glutathione levels in comparison to the untreated dementia group. The effect of Gelsemium of scopolamine-induced cognitive deficits was determined by measuring the behavioral parameters and the antioxidant status of the brain after scopolamine (1mg/kg i.p.) injected amnesic mice. Gelsemium significantly demonstrated in vivo anti-dementia activity (60% protection) and increased exploratory behavior. CONCLUSION: Our investigations indicated that alkaloid, iridoids and coumarin enriched reconstituted Gelsemium tincture extract displays promising cognitive enhancement in adult mice after short-term oral treatment. Hence, Gelsemium can be a promising anti-dementia agent, mediating the protection against amnesia, attention disorders and learning dysfunctions through dual inhibition of both acetyl cholinesterases (no false positive effect was shown), ß-secretase and antioxidant activity.


Asunto(s)
Trastornos del Conocimiento/tratamiento farmacológico , Demencia/tratamiento farmacológico , Gelsemium , Memoria/efectos de los fármacos , Fitoterapia , Preparaciones de Plantas/uso terapéutico , Acetilcolinesterasa/genética , Acetilcolinesterasa/metabolismo , Secretasas de la Proteína Precursora del Amiloide/antagonistas & inhibidores , Secretasas de la Proteína Precursora del Amiloide/metabolismo , Animales , Ácido Aspártico Endopeptidasas/antagonistas & inhibidores , Ácido Aspártico Endopeptidasas/metabolismo , Reacción de Prevención/efectos de los fármacos , Conducta Animal/efectos de los fármacos , Encéfalo/efectos de los fármacos , Encéfalo/metabolismo , Trastornos del Conocimiento/inducido químicamente , Demencia/inducido químicamente , Glutatión/metabolismo , Masculino , Ratones , Preparaciones de Plantas/farmacología , Preparaciones de Plantas/toxicidad , ARN Mensajero/metabolismo , Escopolamina , Pruebas de Toxicidad Aguda
16.
Nat Prod Commun ; 9(7): 1045-55, 2014 Jul.
Artículo en Inglés | MEDLINE | ID: mdl-25230523

RESUMEN

Ischemic brain injury is one of the leading causes of death worldwide and has attracted a lot of attention in the field of drug discovery. Cerebral ischemia is a complex pathological process involving a series of mechanisms, including generation of free radicals, oxidative stress, disruption of the membrane function, release of neurotransmitters and apoptosis. Thrombolytic therapy is the most effective therapeutic strategy, but the benefits are far from being absolute. Increased attention in the field of drug discovery has been focused on using natural compounds from traditional medicinal herbs for neuroprotection, which appears to be a promising therapeutic option for cerebral ischemia with minimal systemic adverse effects that could limit their long term use. The scenario calls for extensive investigations which can result in the development of lead molecules for neuroprotection in the future. In this context, the present review focuses on possible mechanisms underlying the beneficial effects of herbal drugs in patients with cerebral ischemic injury. Natural compounds have been demonstrated to have neurofunctional regulatory actions with antioxidative, anti-inflammatory, calcium antagonizing and anti-apoptotic activities. Among the several leads obtained from plant sources as potential neuroprotective agents, resveratrol, EGb761, curcumin and epigallocatechin-3-gallate have shown significant therapeutic benefits in cerebral ischemic conditions. However, ligustilide, tanshinone, scutellarin and shikonin are the few lead molecules which are under investigation for treatment of cerebral ischemia.


Asunto(s)
Isquemia Encefálica/tratamiento farmacológico , Medicina de Hierbas/métodos , Accidente Cerebrovascular/tratamiento farmacológico , Humanos , Fitoterapia
17.
Nat Prod Commun ; 9(2): 287-90, 2014 Feb.
Artículo en Inglés | MEDLINE | ID: mdl-24689312

RESUMEN

Ayurveda has been the main guiding force in drug discovery from traditional medicine. In concept, this system is rooted in folk or ethnomedicine and in practice it shows further refinement and development in accordance with local traditions. Isolation of active principles from crude drugs, their pharmacological evaluation, therapeutic proving and clinical application resulted in the genesis of modem or so called allopathic medicine. To keep the opportunity alive for further development in traditional as well as modem medicines, it is necessary to have an uninterrupted connection with ethnomedicine. Since the practice of ethnomedicine is based on the age-long indigenous knowledge which has been orally transmitted through generations and sustained in traditions there is an urgent need to document such knowledge. The ongoing strategies adopted in India to document the precious traditional knowledge and conserve medicinal plants are discussed in this communication. India with her rich plant wealth and traditional knowledge about the medicinal use of plants has tremendous scope to provide leadership in ensuring human health and longevity.


Asunto(s)
Medicina Ayurvédica , Medicina de Hierbas , India , Plantas Medicinales
18.
Phytochem Anal ; 25(1): 1-12, 2014.
Artículo en Inglés | MEDLINE | ID: mdl-24105963

RESUMEN

INTRODUCTION: Extraction forms the very basic step in research on natural products for drug discovery. A poorly optimised and planned extraction methodology can jeopardise the entire mission. OBJECTIVE: To provide a vivid picture of different chemometric tools and planning for process optimisation and method development in extraction of botanical material, with emphasis on microwave-assisted extraction (MAE) of botanical material. METHODS: A review of studies involving the application of chemometric tools in combination with MAE of botanical materials was undertaken in order to discover what the significant extraction factors were. Optimising a response by fine-tuning those factors, experimental design or statistical design of experiment (DoE), which is a core area of study in chemometrics, was then used for statistical analysis and interpretations. RESULTS: In this review a brief explanation of the different aspects and methodologies related to MAE of botanical materials that were subjected to experimental design, along with some general chemometric tools and the steps involved in the practice of MAE, are presented. A detailed study on various factors and responses involved in the optimisation is also presented. CONCLUSION: This article will assist in obtaining a better insight into the chemometric strategies of process optimisation and method development, which will in turn improve the decision-making process in selecting influential extraction parameters.


Asunto(s)
Fraccionamiento Químico/métodos , Microondas , Extractos Vegetales/análisis , Extractos Vegetales/química , Modelos Químicos
19.
Nat Prod Commun ; 8(10): 1487-92, 2013 Oct.
Artículo en Inglés | MEDLINE | ID: mdl-24354209

RESUMEN

Arthropod borne flaviviral diseases are a major public health concern in the tropics. However, the majority of cases are associated with Dengue virus (DENV), Yellow Fever virus (YFV), West Nile virus (WNV) and Chikungunya virus (CHIKV) infections. Despite their profound clinical and economic impact among large sections of the population there is a lack of effective treatment against these diseases. A large number of plants are available in nature, which may act as a source for lead molecules against various diseases including arthropod borne flaviviral infections. In this review we discuss various crude extracts as well as purified compounds from natural sources with promising anti-DENV, YFV, WNV and CHIKV activity.


Asunto(s)
Factores Biológicos/uso terapéutico , Infecciones por Flaviviridae/tratamiento farmacológico , Extractos Vegetales/uso terapéutico , Animales , Flavivirus/fisiología , Humanos , Aceites Volátiles/uso terapéutico
20.
Exp Parasitol ; 135(2): 183-7, 2013 Oct.
Artículo en Inglés | MEDLINE | ID: mdl-23850996

RESUMEN

In eastern and southern part of India Dregea volubilis (Family Asclepediaceae) is widely used as anthelmintic in traditional system of medicine. The present study was conducted to evaluate the fasciocidal activity of the methanol extract of D. volubilis leaves (MEDV) and to observe the drug's effect on organisms through scanning electron microscopic (SEM) study. Live parasites (Trematode: Fasciola gigantica) were collected in 0.9% phosphate-buffered saline from the bile ducts of buffalo. Those were incubated in the said media at 37 ± 1 °C either as control, or with MEDV at 5, 10, 25, 50 and 100 mg/ml as test groups or with albendazole at 10mg/ml as standard group. The efficacy of the extract was determined on the basis of paralysis (temporary loss of spontaneous movement of the organisms) and/or death of the liver flukes. Death was confirmed when the organisms lost their motility permanently and their motility could not be revived even when vigorously shaken or dipped in warm water. MEDV at all concentration effectively paralyzed first and then killed the liver flukes (p < 0.001). Maximum fasciocidal activity was found with concentration of 100 mg/ml at 38.83 ± 3.41 min. Through SEM study, severe damages were observed in both the suckers as well as on the tegumental surfaces of the treated liver flukes. The study confirmed the fasciocidal activity of the MEDV.


Asunto(s)
Antiplatelmínticos/farmacología , Apocynaceae/química , Fasciola/efectos de los fármacos , Extractos Vegetales/farmacología , Albendazol/farmacología , Animales , Búfalos , Fasciola/ultraestructura , Microscopía Electrónica de Rastreo , Hojas de la Planta/química
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