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1.
BMJ Glob Health ; 8(8)2023 08.
Artículo en Inglés | MEDLINE | ID: mdl-37558269

RESUMEN

Management of COVID-19 in Africa is challenging due to limited resources, including the high cost of vaccines, diagnostics, medical devices and routine pharmaceuticals. These challenges, in addition to wide acceptability, have resulted in increased use of herbal medicines based on African traditional medicines (ATMs) by patients in Africa. This is in spite of the often-significant gaps in evidence regarding these traditional medicines as to their efficacy and safety for COVID-19. African scientists, with some support from their governments, and guidance from WHO and other bodies, are addressing this evidence gap, developing and testing herbal medicines based on ATMs to manage mild-to-moderate cases of COVID-19. Such efforts need further support to meet public health needs.


Asunto(s)
COVID-19 , Humanos , Medicinas Tradicionales Africanas , Pandemias , África , Extractos Vegetales
2.
Mol Cell Biochem ; 477(1): 225-240, 2022 Jan.
Artículo en Inglés | MEDLINE | ID: mdl-34655418

RESUMEN

Severe acute respiratory syndrome-coronavirus-2 (COVID-19) virus uses Angiotensin-Converting Enzyme 2 (ACE2) as a gateway for their entry into the human body. The ACE2 with cleaved products have emerged as major contributing factors to multiple physiological functions and pathogenic complications leading to the clinical consequences of the COVID-19 infection Decreased ACE2 expression restricts the viral entry into the human cells and reduces the viral load. COVID-19 infection reduces the ACE2 expression and induces post-COVID-19 complications like pneumonia and lung injury. The modulation of the ACE2-Ang (1-7)-Mas (AAM) axis is also being explored as a modality to treat post-COVID-19 complications. Evidence indicates that specific food components may modulate the AAM axis. The variations in the susceptibility to COVID-19 infection and the post-COVID its complications are being correlated with varied dietary habits. Some of the food substances have emerged to have supportive roles in treating post-COVID-19 complications and are being considered as adjuvants to the COVID-19 therapy. It is possible that some of their active ingredients may emerge as the direct treatment for the COVID-19.


Asunto(s)
Angiotensina I/metabolismo , Enzima Convertidora de Angiotensina 2/metabolismo , COVID-19/complicaciones , COVID-19/dietoterapia , Fragmentos de Péptidos/metabolismo , Proto-Oncogenes Mas/metabolismo , Enfermedades Cardiovasculares/patología , Enfermedades Cardiovasculares/virología , Proteínas en la Dieta/farmacología , Flavonoides/farmacología , Humanos , Pulmón/patología , Pulmón/virología , Aceites de Plantas/farmacología , Polifenoles/farmacología , Terpenos/farmacología , Internalización del Virus , Vitaminas/farmacología
3.
Biomolecules ; 11(12)2021 12 03.
Artículo en Inglés | MEDLINE | ID: mdl-34944471

RESUMEN

Depression is one of the most frequently observed psychological disorders, affecting thoughts, feelings, behavior and a sense of well-being in person. As per the WHO, it is projected to be the primitive cause of various other diseases by 2030. Clinically, depression is treated by various types of synthetic medicines that have several limitations such as side-effects, slow-onset action, poor remission and response rates due to complicated pathophysiology involved with depression. Further, clinically, patients cannot be given the treatment unless it affects adversely the job or family. In addition, synthetic drugs are usually single targeted drugs. Unlike synthetic medicaments, there are many plants that have flavonoids and producing action on multiple molecular targets and exhibit anti-depressant action by affecting multiple neuronal transmissions or pathways such as noradrenergic, serotonergic, GABAnergic and dopaminergic; inhibition of monoamine oxidase and tropomyosin receptor kinase B; simultaneous increase in nerve growth and brain-derived neurotrophic factors. Such herbal drugs with flavonoids are likely to be useful in patients with sub-clinical depression. This review is an attempt to analyze pre-clinical studies, structural activity relationship and characteristics of reported isolated flavonoids, which may be considered for clinical trials for the development of therapeutically useful antidepressant.


Asunto(s)
Antidepresivos/uso terapéutico , Depresión/tratamiento farmacológico , Flavonoides/uso terapéutico , Antidepresivos/química , Antidepresivos/farmacología , Depresión/metabolismo , Flavonoides/química , Flavonoides/farmacología , Humanos , Transducción de Señal , Relación Estructura-Actividad , Transmisión Sináptica/efectos de los fármacos
4.
Mol Cell Biochem ; 476(6): 2345-2364, 2021 Jun.
Artículo en Inglés | MEDLINE | ID: mdl-33587232

RESUMEN

The pandemic of Serious Acute Respiratory Syndrome Corona Virus-2 (SARS-CoV-2) that produces corona virus disease (COVID-19) has challenged the entire mankind by rapidly spreading globally in 210 countries affecting over 25 million people and about 1 million deaths worldwide. It continues to spread, afflicting the health system globally. So far there is no remedy for the ailment and the available antiviral regimens have been unsatisfactory for the clinical outcomes and the mode of treatment has been mainly supportive for the prevention of COVID-19-induced morbidity and mortality. From the time immortal the traditional plant-based ethno-medicines have provided the leads for the treatment of infectious diseases. Phytopharmaceuticals have provided potential and less toxic antiviral drugs as compared to conventional modern therapeutics which are associated with severe toxicities. The ethnopharmacological knowledge about plants has provided food supplements and nutraceuticals as a promise for prevention and treatment of the current pandemic. In this review article, we have attempted to comprehend the information about the edible medicinal plant materials with potential antiviral activity specifically against RNA virus which additionally possess property to improve immunity along with external and internal respiration and exhibit anti-inflammatory properties for the prevention and treatment of the disease. This will open an arena for the development of novel nutraceutical herbal formulations as an alternative therapy that can be used for the prevention and treatment of COVID-19.


Asunto(s)
Antivirales/farmacología , Tratamiento Farmacológico de COVID-19 , Plantas Comestibles/química , Plantas Medicinales/química , SARS-CoV-2/efectos de los fármacos , Antivirales/uso terapéutico , COVID-19/etiología , Etnofarmacología/métodos , Interacciones Huésped-Patógeno/efectos de los fármacos , Humanos , SARS-CoV-2/química , SARS-CoV-2/patogenicidad , SARS-CoV-2/fisiología , Síndrome Respiratorio Agudo Grave/tratamiento farmacológico , Internalización del Virus/efectos de los fármacos , Replicación Viral/efectos de los fármacos , Replicación Viral/fisiología
5.
Curr Drug Targets ; 22(4): 429-442, 2021.
Artículo en Inglés | MEDLINE | ID: mdl-32718288

RESUMEN

The Glioblastoma Multiforme (GBM; grade IV astrocytoma) exhorts tumors of star-shaped glial cells in the brain. It is a fast-growing tumor that spreads to nearby brain regions specifically to cerebral hemispheres in frontal and temporal lobes. The etiology of GBM is unknown, but major risk factors are genetic disorders like neurofibromatosis and schwannomatosis, which develop the tumor in the nervous system. The management of GBM with chemo-radiotherapy leads to resistance, and current drug regimen like Temozolomide (TMZ) is less efficacious. The reasons behind the failure of drugs are due to DNA alkylation in the cell cycle by enzyme DNA guanidase and mitochondrial dysfunction. Naturally occurring bioactive compounds from plants referred as phytochemicals, serve as vital sources for anti-cancer drugs. Some prototypical examples include taxol analogs, vinca alkaloids (vincristine, vinblastine), podophyllotoxin analogs, camptothecin, curcumin, aloe-emodin, quercetin, berberine etc. These phytochemicals often regulate diverse molecular pathways, which are implicated in the growth and progression of cancers. However, the challenges posed by the presence of BBB/BBTB to restrict the passage of these phytochemicals, culminates in their low bioavailability and relative toxicity. In this review, we integrated nanotech as a novel drug delivery system to deliver phytochemicals from traditional medicine to the specific site within the brain for the management of GBM.


Asunto(s)
Neoplasias Encefálicas , Glioblastoma , Nanopartículas , Fitoquímicos , Neoplasias Encefálicas/tratamiento farmacológico , Sistemas de Liberación de Medicamentos , Glioblastoma/tratamiento farmacológico , Humanos , Fitoquímicos/uso terapéutico
6.
J Ethnopharmacol ; 269: 113759, 2021 Apr 06.
Artículo en Inglés | MEDLINE | ID: mdl-33359916

RESUMEN

ETHNOPHARMACOLOGICAL RELEVANCE: Ashwagandha has been used as an ayurvedic medicine in the form of 'Rasayana' (as a tonic) even before 3000 BCE in India. As per Ayurveda, it has long been used traditionally for the treatment of inflammation, weakness, impotence, pulmonary tuberculosis. This plant is also beneficial in lumbago and leucorrhea in the female. In the recent past, Withania has shown its anti-cancerous activity in various experimental models. In addition, Withania also possesses many other properties such as anti-oxidant, anti-stress, adaptogenic, and regenerative which will eventually be beneficial and safe in treating cancer patients. AIM OF THE STUDY: This review aims to provide experimental evidence along with a deeper insight into molecular mechanisms of Ashwagandha (Withania somnifera (L.) Dunal) through which it acts as a chemotherapeutic agent against different types of breast cancer. MATERIALS AND METHODS: Literature searches with the help of electronic online databases (Elsevier, Google Scholar, Scopus, Springer Link, ScienceDirect, ResearchGate, PubMed) were carried out. The timeline for collection of data for the review article was from 2000 to 2019. The plant name was validated from The Plant List (2013). Version 1.1. Published on http://www.theplantlist.org/(accessed 21st March 2020). RESULTS: Various forms of Withania somnifera were used and several in vitro, in vivo, and clinical studies were reported by researchers. They found ashwagandha to exhibit anti-apoptotic, anti-metastatic, anti-invasive and anti-inflammatory properties and gave the evidence that ashwagandha has a capability for averting and treating breast cancer. CONCLUSION: Various in vitro and in vivo studies suggested Ashwagandha may possess a potential for treating breast cancer, especially ER/PR positive breast cancer and triple-negative breast cancer. A clinical trial has also been conducted in the past that suggested its potential in refining quality of life in breast cancer patients. Studies directed towards molecular pathways have helped in unravelling the key mechanisms of ashwagandha. Future research should be directed towards translational studies involving breast cancer patients. These will reinforce the ancient power of our Ayurvedic medicine.


Asunto(s)
Antineoplásicos Fitogénicos/farmacología , Neoplasias de la Mama/tratamiento farmacológico , Fitoquímicos/farmacología , Extractos Vegetales/farmacología , Withania/química , Animales , Antineoplásicos Fitogénicos/uso terapéutico , Neoplasias de la Mama/metabolismo , Neoplasias de la Mama/fisiopatología , Femenino , Humanos , Medicina Ayurvédica/métodos , Fitoquímicos/química , Fitoquímicos/uso terapéutico , Extractos Vegetales/química , Extractos Vegetales/uso terapéutico
7.
Drug Res (Stuttg) ; 70(2-03): 65-70, 2020 Feb.
Artículo en Inglés | MEDLINE | ID: mdl-31931549

RESUMEN

Tuberculosis (TB) is one of the oldest fatal diseases of history. Multidrugresistant tuberculosis (MDRTB) is a major public health issue in the world. In India, the incidence is getting up despite the Indian revised National Tuberculosis Control Programme. India has six recognize medicine systems in this category, namely Ayurveda, Siddha, Unani and Yoga, Naturopathy and Homoeopathy. This review study was undertaken to evaluate the efficacy of different drug treatments based on Indian Systems of Traditional Medicines to the standard MDR-TB regimen. This review mainly focuses on the combinational approaches towards treatment protocols, prevention strategies, and management of tuberculosis in different established systems of medicine in India. Along with allopathic drugs, these AYUSH based drugs work in synergistic manner. Recent research suggests that Homeopathic treatment along with the antibiotics synergise the effect of antibiotics while reaching to its site of action. Additionally in Siddha system, formulation of medicinal herbs showing significant activity against TB bacteria. Furthermore, adopting the management or principles of Unani system would be beneficial in health and disease. Similarly, Unani and Naturopathy through natural healing are equally effective. On the other hand, medicinal plants from the Ayurveda that have been successfully employed to treat TB because of less toxicity and side effect in comparison with existing antibiotics. The findings in this review have provided scientific support for anti-TB activity of different medicinal system of India via numerous underlying mechanisms.


Asunto(s)
Antituberculosos/administración & dosificación , Medicina Tradicional/métodos , Tuberculosis Resistente a Múltiples Medicamentos/tratamiento farmacológico , Antituberculosos/efectos adversos , Antituberculosos/farmacología , Sinergismo Farmacológico , Quimioterapia Combinada , Humanos , India/epidemiología , Mycobacterium tuberculosis/efectos de los fármacos , Mycobacterium tuberculosis/aislamiento & purificación , Plantas Medicinales/química , Tuberculosis Resistente a Múltiples Medicamentos/epidemiología , Tuberculosis Resistente a Múltiples Medicamentos/microbiología
8.
Front Biosci (Schol Ed) ; 10(1): 175-184, 2018 01 01.
Artículo en Inglés | MEDLINE | ID: mdl-28930525

RESUMEN

According to a relatively recent UNICEF report, 15 percent of the infant population of the world is of low birth weight with India accounting for one third of all the world's low-weight newborns. Twenty percent of all low birth weight infants die within a month. This mortality figure is higher in developing countries due to inadequate nutritional intake by pregnant women. Development of a new package of nutrient-rich food based on egg or milk or soy bean proteins, containing multiple micronutrient supplements, available at affordable cost, may protect against morbidity and mortality among pregnant women as well as low birth weight in newborns. These benefits may continue to decrease morbidity and mortality during infancy and childhood and might reduce the risk of chronic diseases in later adult life.


Asunto(s)
Micronutrientes/administración & dosificación , Complicaciones del Embarazo/prevención & control , Suplementos Dietéticos , Femenino , Humanos , Embarazo
9.
Biomed Pharmacother ; 83: 221-228, 2016 Oct.
Artículo en Inglés | MEDLINE | ID: mdl-27372406

RESUMEN

PURPOSE: Tephrosia purpurea (T. purpurea) has been reported to prevent cataract formation in senile cataract model as well as proven effective in STZ induced type 1 diabetes. Aldose reductase (AR) is a key enzyme in the intracellular polyol pathway responsible for the development of diabetic cataract. OBJECTIVE: To investigate the effects of T. purpurea in the light of inhibition of aldose reductase enzyme in polyol pathway. METHODS: We studied the effects of alcoholic extract and flavonoid fraction of T. purpurea in streptozotocin (STZ, 45mg/kg, i.v.)-induced type I diabetic cataract in rats. The animals were divided into five groups as control, control treated with alcoholic and flavonoid fraction, diabetic control and diabetic treated with alcoholic and flavonoid fraction. In-vitro aldose reductase inhibitory activity was also evaluated. Further, molecular docking study was performed with crystal structure of aldose reductase and its known chemical constituents of the plant. RESULTS: The IC50 value of alcoholic extract for aldose reductase inhibition was found to be 209.13µg/ml, and that of flavonoid fraction was found to be 46.73µg/ml. Administration of STZ produced significantly abnormal levels of serum glucose, serum insulin, soluble protein and antioxidants in the lens homogenate. Treatment with alcoholic extract and flavonoid fraction of T. purpurea were able to normalize these levels. Some of the active constituents of T. purpurea showed significant interactions with aldose reductase enzyme in molecular docking studies. CONCLUSIONS: Our data suggested that both the extracts might be helpful in delaying the development of diabetic cataract due to the presence of rutin and quercetin. This beneficial effect may be due to its significant inhibition of aldose reductase enzyme and anti-oxidant activity.


Asunto(s)
Aldehído Reductasa/antagonistas & inhibidores , Catarata/tratamiento farmacológico , Catarata/enzimología , Complicaciones de la Diabetes/tratamiento farmacológico , Inhibidores Enzimáticos/uso terapéutico , Extractos Vegetales/uso terapéutico , Sustancias Protectoras/uso terapéutico , Tephrosia/química , Aldehído Reductasa/metabolismo , Animales , Antioxidantes/metabolismo , Sitios de Unión , Compuestos de Bifenilo/química , Glucemia/metabolismo , Catarata/sangre , Complicaciones de la Diabetes/sangre , Complicaciones de la Diabetes/enzimología , Inhibidores Enzimáticos/farmacología , Femenino , Depuradores de Radicales Libres/farmacología , Insulina/sangre , Cristalino/efectos de los fármacos , Cristalino/metabolismo , Cristalino/patología , Masculino , Simulación del Acoplamiento Molecular , Fitoquímicos/análisis , Picratos/química , Extractos Vegetales/farmacología , Sustancias Protectoras/farmacología , Ratas Sprague-Dawley , Solubilidad
10.
Indian J Exp Biol ; 54(7): 457-466, 2016 Jul.
Artículo en Inglés | MEDLINE | ID: mdl-29466624

RESUMEN

Globally, diabetes is a serious health issue affecting one in 11 adults and consumes 12% of global health expenditure. Prevalence of dyslipidemia in diabetes is not uncommon since decades. Further, patients with type II diabetes have 2-4 folds more risk for cardiovascular disease (CVD). Plants with antioxidant potential are known to have beneficial effects in diabetes and its complications: Natural compounds, flavonoids particularly, ameliorate hyperglycemia as well as CVD. Here, we evaluated common wasteland weed Tephrosia purpurea, used traditionally as folk medicine to treat many disorders including diabetes. We studied the effect of 8-wk treatment of flavonoid-rich fraction of T. purpurea (FFTp) (40 mg/kg/day/p.o.) on various biochemical, cardiovascular and lenticular parameters on streptozotocin (STZ) (45 mg/kg, i.v.) induced type I diabetic rats. STZ administration produced significant hyperglycemia, dyslipidemia, and altered cardiac biomarkers like lactate dehydrogenase, creatinine kinase and reduced antioxidants in lenticular tissues of rats. Treatment with FFTp significantly prevented STZ-induced hyperglycemia, dyslipidemia as well as cardiovascular markers. We observed decreased rate of pressure development (+dp/dt) and decay (-dp/dt) in STZ diabetic hearts which was prevented by FFTp. Further, the soluble protein levels and the antioxidants were also elevated in the diabetic rats by the treatment. In conclusion, our data suggest that FFTp produces beneficial effects on diabetes induced cardiovascular complications and cataract. Such beneficial actions may be attributed to the antioxidant property of flavonoids, quercetin or rutin, present in T. purpurea.


Asunto(s)
Diabetes Mellitus Experimental/tratamiento farmacológico , Flavonoides/uso terapéutico , Fitoterapia , Tephrosia , Animales , Antioxidantes/farmacología , Catarata/prevención & control , Diabetes Mellitus Experimental/complicaciones , Dislipidemias/tratamiento farmacológico , Femenino , Hemodinámica/efectos de los fármacos , Masculino , Ratas , Ratas Sprague-Dawley , Estreptozocina , Tephrosia/química
11.
Curr Eye Res ; 41(2): 222-31, 2016.
Artículo en Inglés | MEDLINE | ID: mdl-25848963

RESUMEN

PURPOSE: Recent investigations have shown that phytochemical antioxidants can scavenge free radicals and prevent various diseases like cataract. The objective of the present study was to assess the efficacy of the Tephrosia purpurea in preventing these changes in the lens of selenite-induced cataract models. MATERIALS AND METHODS: Cataract was induced by a single injection of sodium selenite (4 mg/kg, s.c.) to 9-day-old Sprague-Dawley rat pups. The treatment with different extracts of T. purpurea was started on 10th day and continued for 30 days in pups pretreated with sodium selenite. The animals were treated orally with either quercetin (1 mg/kg), flavonoid rich fraction (40 mg/kg) or alcohol extract (300 mg/kg) of T. purpurea. Cataract was visualized after 30 days. Encapsulated lenses were analyzed for reduced glutathione and malondialdehyde. Lenses were also analyzed for total protein, insoluble protein, total nitrite, calcium levels, protein sulfhydryl content as well as for the activities of superoxide dismutase and Ca(2+)-ATPase. RESULTS: Morphological examination of the rat lenses revealed normal transparent lens with minimal or partial nuclear opacity in control whereas dense opacity developed in rat lens treated with selenite. Both the extracts of T. purpurea produced reduction in nuclear opacity as well as improvement in the insoluble proteins, protein sulfhydryl, total nitrite, calcium levels and Ca(2+)-ATPase activity in lenses. The extracts decreased malondialdehyde levels but also prevented the loss of reduced glutathione levels. CONCLUSION: Our data suggests therapeutic potential of T. purpurea for the treatment of cataract.


Asunto(s)
Antioxidantes/uso terapéutico , Catarata/prevención & control , Modelos Animales de Enfermedad , Cristalino/efectos de los fármacos , Extractos Vegetales/uso terapéutico , Tephrosia/química , Animales , Animales Recién Nacidos , Calcio/metabolismo , ATPasas Transportadoras de Calcio/metabolismo , Catarata/inducido químicamente , Catarata/metabolismo , Catarata/patología , Femenino , Glutatión/metabolismo , Cristalino/metabolismo , Cristalino/patología , Masculino , Malondialdehído/metabolismo , Medicina Ayurvédica , Estrés Oxidativo , Ratas , Ratas Sprague-Dawley , Selenito de Sodio/toxicidad
12.
J Pharm Pharm Sci ; 16(4): 530-40, 2013.
Artículo en Inglés | MEDLINE | ID: mdl-24210061

RESUMEN

PURPOSE: Diabetes mellitus is characterized by hyperglycemia resulting from defects in insulin secretion, action or both. The use of medicinal plants for the treatment of diabetes mellitus dates back from the Ebers papyrus of about 1550 B.C. One of the major problems with herbal drugs is that the active ingredients are not well defined. It is important to know the active components and their molecular interactions which will help to analyze their therapeutic efficacy and also to standardize the product. There are a number of medicinal plants known for their anti-diabetic effect that possess similarities in their active chemical components, e.g. iridoid and secoiridoid glycosides. METHODS: In this study, we have compared the structure of various iridoid and secoiridoid glycosides to design a novel pharmacophore. We further developed a structure-activity relationship for the inhibition of glycogen phosphorylase-a. CONCLUSION: By using docking studies, we are proposing, for the first time, that inhibition of glycogen phosphorylase-a activity is a common target for iridoids and secoiridoids to elicit anti-diabetic effects. This article is open to POST-PUBLICATION REVIEW. Registered readers (see "For Readers") may comment by clicking on ABSTRACT on the issue's contents page.


Asunto(s)
Glucógeno Fosforilasa/antagonistas & inhibidores , Hipoglucemiantes/farmacología , Glicósidos Iridoides/farmacología , Glucógeno Fosforilasa/metabolismo , Hipoglucemiantes/química , Glicósidos Iridoides/química , Simulación del Acoplamiento Molecular , Relación Estructura-Actividad
13.
Ayu ; 34(4): 440-4, 2013 Oct.
Artículo en Inglés | MEDLINE | ID: mdl-24696584

RESUMEN

Polyphenols from natural source are potential therapeutics that act alone or supplement anti-diabetic drugs in the prevention and treatment of diabetes. The present investigation was undertaken to study the effect of hydroalcoholic extract (HE) of fruits of Emblica officinalis on type 1 diabetic rats. Diabetes was induced by streptozotocin (STZ) (45 mg/kg i.v.). HE (100 mg/kg, p.o.) was administered for 4 weeks and at the end of treatment, blood samples were collected and analyzed for various biochemical parameters. STZ produced a diabetic state exhibiting all the cardinal symptoms such as loss of body weight, polydipsia, polyuria, glucosuria, polyphagia, hypoinsulinemia, and hyperglycemia associated with hypercholesterolemia and hypertriglyceridemia. Treatment with HE prevented cardinal symptoms and caused significant decrease in fasting serum glucose, AUCglucose, cholesterol, triglyceride, low-density lipoprotein (LDL) and very LDL in diabetic rats. However, insulin, AUCinsulin, and serum high-density lipoprotein level were not significantly altered by treatment. Treatment also reduced lipid peroxidation and increased anti-oxidant parameters in the liver homogenates of diabetic rats. Polyphenol enriched fraction of HE significantly improved disarranged carbohydrate and lipid metabolism of chemically induced diabetes in rats. The mechanism of its anti-diabetic activity appears to be either improvement in peripheral glucose utilization, increased insulin sensitivity, or anti-oxidant property.

14.
Phytother Res ; 27(4): 624-7, 2013 Apr.
Artículo en Inglés | MEDLINE | ID: mdl-22718571

RESUMEN

We have previously shown the anti-diabetic effects of swertiamarin; however, pharmacokinetic analysis showed that swertiamarin had a plasma half-life of 1.3 h. Gentianine is an active metabolite of swertiamarin that possesses a pharmacophoric moiety. The aim of this study was to explore the possibility whether the anti-diabetic effect of swertiamarin is due to gentianine. Swertiamarin treatment had no significant effect on adipogenesis, or the mRNA expression of PPAR-γ and GLUT-4; however, there was a significant increase in the mRNA expression of adiponectin. On the other hand, treatment with gentianine significantly increased adipogenesis, which was associated with a significant increase in the mRNA expression of PPAR-γ, GLUT-4 and adiponectin. These findings suggest, for the first time, that the anti-diabetic effect of swertiamarin is due to gentianine, an active metabolite of swertiamarin.


Asunto(s)
Alcaloides/farmacología , Hipoglucemiantes/farmacología , Glucósidos Iridoides/farmacología , PPAR gamma/metabolismo , Pironas/farmacología , Células 3T3-L1 , Adipogénesis/efectos de los fármacos , Adiponectina/genética , Adiponectina/metabolismo , Animales , Diferenciación Celular/efectos de los fármacos , Transportador de Glucosa de Tipo 4/genética , Transportador de Glucosa de Tipo 4/metabolismo , Ratones , PPAR gamma/genética , Regulación hacia Arriba
15.
Phytother Res ; 26(8): 1259-61, 2012 Aug.
Artículo en Inglés | MEDLINE | ID: mdl-22228612

RESUMEN

Dyslipidaemia is one of the major risk factors for cardiovascular disease in diabetes mellitus. Lipid changes associated with diabetes mellitus are attributed to increases in free fatty acid flux, secondary to insulin resistance. In the present study, we have investigated the beneficial effects of swertiamarin on dyslipidaemic conditions associated with type 2 diabetes in streptozotocin-induced type 2 diabetic rats. Swertiamarin (50 mg/kg, i.p.) administered once a day for 6 weeks resulted in significant (p < 0.001) reductions in serum triglycerides, cholesterol and low-density lipoprotein levels in diabetic animals as compared with diabetic control animals. Serum fasting glucose was significantly (p < 0.05) decreased, moreover, the insulin sensitivity index was significantly (p < 0.05) increased in swertiamarin treated animals. Overall the data suggest that swertiamarin has beneficial effects on diabetic associated complications such as dyslipidaemia.


Asunto(s)
Diabetes Mellitus Experimental/tratamiento farmacológico , Dislipidemias/tratamiento farmacológico , Glucósidos Iridoides/uso terapéutico , Fitoterapia , Pironas/uso terapéutico , Animales , Glucemia/análisis , Diabetes Mellitus Tipo 2/tratamiento farmacológico , Gentianaceae/química , Hipoglucemiantes/farmacología , Resistencia a la Insulina , Glucósidos Iridoides/administración & dosificación , Lipasa/sangre , Lipoproteínas LDL/sangre , Masculino , Pironas/administración & dosificación , Ratas , Estreptozocina/efectos adversos
16.
J Cardiovasc Pharmacol Ther ; 16(3-4): 380-7, 2011.
Artículo en Inglés | MEDLINE | ID: mdl-21183729

RESUMEN

Although sarpogrelate, a 5-HT(2A) receptor antagonist, has been reported to exert beneficial effects in diabetes, the mechanisms of its action are not understood. In this study, diabetes was induced in rats by an injection of streptozotocin (65 mg/kg) and the animals were assessed 7 weeks later. Decreased serum insulin as well as increased serum glucose, cholesterol, and triglyceride levels in diabetic animals were associated with increased blood pressure and heart/body weight ratio. Impaired cardiac performance in diabetic animals was evident by decreased heart rate, left ventricular developed pressure, rate of pressure development, and rate of pressure decay. Treatment of diabetic animals with sarpogrelate (5 mg/kg) or insulin (10 units/kg) daily for 6 weeks attenuated the observed changes in serum insulin, glucose, and lipid levels as well as blood pressure and cardiac function by varying degrees. Protein content for membrane glucose transporters (GLUT-1 and GLUT-4) was depressed in diabetic heart; the observed alteration in GLUT-4 was partially prevented by both sarpogrelate and insulin, whereas that in GLUT-1 was attenuated by sarpogrelate only. Incubation of myoblast cells with sarpogrelate and insulin stimulated glucose uptake; these effects were additive. 5-hydroxytryptamine was found to inhibit glucose-induced insulin release from the pancreas; this effect was prevented by sarpogrelate. These results suggest that sarpogrelate may improve cardiac function in chronic diabetes by promoting the expression of membrane glucose transporters as well as by releasing insulin from the pancreas.


Asunto(s)
Cardiotónicos/farmacología , Enfermedades Cardiovasculares/fisiopatología , Diabetes Mellitus Experimental/fisiopatología , Corazón/fisiopatología , Insulina/fisiología , Islotes Pancreáticos/fisiología , Succinatos/farmacología , Animales , Cardiotónicos/efectos adversos , Enfermedades Cardiovasculares/tratamiento farmacológico , Enfermedades Cardiovasculares/prevención & control , Fenómenos Fisiológicos Cardiovasculares , Células Cultivadas , Diabetes Mellitus/fisiopatología , Diabetes Mellitus Experimental/tratamiento farmacológico , Evaluación Preclínica de Medicamentos , Transportador de Glucosa de Tipo 4/fisiología , Masculino , Ratones , Mioblastos/fisiología , Ratas , Ratas Sprague-Dawley , Succinatos/efectos adversos
17.
Indian J Exp Biol ; 48(1): 26-30, 2010 Jan.
Artículo en Inglés | MEDLINE | ID: mdl-20358863

RESUMEN

The present investigation was undertaken to standardize and study the dose-dependent effect of three weeks treatment with hot and cold aqueous extract of E. littorale (0.5, 1 and 2 g/kg, po) on streptozotocin (STZ) induced type I diabetic (confirmed by histopathology) rats (45 mg/kg, iv single dose). Treatment of rats with STZ produced cardinal signs of diabetes-mellitus like a significant loss of body weight, polyuria and polydipsia. There was also a significant increase in fasting blood glucose levels and AUC(glucose) associated with decrease in insulin levels and AUC(insulin) in STZ-diabetic rats. Treatment with E. littorale hot extract (1 and 2 g/kg) significantly reduced the elevated food intake and water intake, glucose and AUC(glucose) levels of diabetic rats. There was also a significant increase in serum cholesterol, serum triglyceride in the STZ diabetic rats. Treatment with E. littorale hot extract (1 and 2 g/kg) significantly decreased all these elevated levels in diabetic rats. Hot aqueous extract of E. littorale at 0.5 g/kg produced a significant decrease in serum glucose and triglycerides. At this doses serum cholesterol and AUC(glucose) were not found to be altered significantly.TLC finger-print profiles were established for the aqueous extract using HPTLC. Swertiamarin, which was used as a chemical marker, was found to be one of the major components in the hot extract while it was absent in cold extract. The results suggest that E. littorale possesses potential antidiabetic activity and improves lipid profile at a small dose of 0.5 g/kg.


Asunto(s)
Diabetes Mellitus Experimental/tratamiento farmacológico , Gentianaceae , Fitoterapia , Animales , Diabetes Mellitus Tipo 1/tratamiento farmacológico , Hipoglucemiantes/farmacología , Masculino , Medicina Tradicional , Extractos Vegetales/farmacología , Ratas , Ratas Sprague-Dawley
18.
Mol Cell Biochem ; 340(1-2): 1-6, 2010 Jul.
Artículo en Inglés | MEDLINE | ID: mdl-20229291

RESUMEN

Diabetic nephropathy (DN) is one of the foremost causes of renal failure and a primary cause of diabetes mellitus related death. Previously, we have reported that aqueous extract of Enicostemma littorale has potential antidiabetic activity. In the present study, we have investigated the effect of aqueous extract of E. littorale 1 g/kg, p.o. and swertiamarin 50 mg/kg, p.o. daily for 3 weeks in type 1 DN complications in SD rats. DN was assessed by serum urea, creatinine, lipid profile and water intake levels. Treatment with aqueous extract of E. littorale and swertiamarin significantly decreased serum urea and creatinine and other parameters associated with the development of DN in type 1 diabetic rats. We have also found considerable improvement in histology of glomerular function of aqueous extract of E. littorale and swertiamarin-treated animals.


Asunto(s)
Diabetes Mellitus Experimental/tratamiento farmacológico , Diabetes Mellitus Tipo 1/tratamiento farmacológico , Nefropatías Diabéticas/prevención & control , Gentianaceae , Glucósidos/farmacología , Hipoglucemiantes/farmacología , Iridoides/farmacología , Extractos Vegetales/farmacología , Pironas/farmacología , Administración Oral , Animales , Biomarcadores/sangre , Glucemia/metabolismo , Creatinina/sangre , Diabetes Mellitus Experimental/sangre , Diabetes Mellitus Experimental/complicaciones , Diabetes Mellitus Experimental/patología , Diabetes Mellitus Tipo 1/sangre , Diabetes Mellitus Tipo 1/complicaciones , Diabetes Mellitus Tipo 1/patología , Nefropatías Diabéticas/sangre , Nefropatías Diabéticas/etiología , Nefropatías Diabéticas/patología , Ingestión de Líquidos/efectos de los fármacos , Glucósidos/administración & dosificación , Hipertrofia , Hipoglucemiantes/administración & dosificación , Glucósidos Iridoides , Iridoides/administración & dosificación , Glomérulos Renales/efectos de los fármacos , Glomérulos Renales/patología , Lípidos/sangre , Masculino , Extractos Vegetales/administración & dosificación , Pironas/administración & dosificación , Ratas , Ratas Sprague-Dawley , Urea/sangre
19.
Indian J Exp Biol ; 47(7): 564-70, 2009 Jul.
Artículo en Inglés | MEDLINE | ID: mdl-19761040

RESUMEN

Present investigation was undertaken to evaluate antihyperglycemic, antihyperlipidemic and antioxidant activities of Dihar, a polyherbal formulation containing drugs from eight different herbs viz., Syzygium cumini, Momordica charantia, Emblica officinalis, Gymnema sylvestre, Enicostemma littorale, Azadirachta indica, Tinospora cordifolia and Curcuma longa in streptozotocin (STZ, 45 mg/kg iv single dose) induced type 1 diabetic rats. STZ produced a significant increase in serum glucose, cholesterol, triglyceride, very low density lipoprotein, low density lipoprotein, creatinine, and urea levels in diabetic rat. Treatment with Dihar (100 mg/kg) for 6 weeks produced decrease in STZ induced serum glucose and lipids levels and increased insulin levels as compared to control. Dihar produced significant decrease in serum creatinine and urea levels in diabetic rats. There was a significant decrease in reduced glutathione, superoxide dismutase, catalase levels and increase in thiobarbituiric acid reactive species levels in the liver of STZ-induced diabetic rats. Administration of Dihar to diabetic rats significantly reduced the levels of lipid paroxidation and increased the activities of antioxidant enzymes. The results suggest Dihar to be beneficial for the treatment of type 1 diabetes.


Asunto(s)
Antioxidantes/farmacología , Diabetes Mellitus Experimental/tratamiento farmacológico , Hipoglucemiantes/farmacología , Hipolipemiantes/farmacología , Preparaciones de Plantas/farmacología , Animales , Glucemia/metabolismo , Diabetes Mellitus Experimental/metabolismo , Lípidos/sangre , Hígado/efectos de los fármacos , Hígado/metabolismo , Masculino , Medicina Ayurvédica , Fitoterapia , Plantas Medicinales , Ratas , Ratas Wistar
20.
J Nat Med ; 63(4): 437-42, 2009 Oct.
Artículo en Inglés | MEDLINE | ID: mdl-19633811

RESUMEN

We have investigated antihyperlipidaemic effect of swertiamarin (50 mg/kg, oral once) isolated from the perennial herb Enicostemma littorale Blume in poloxamer 407 (P-407)-induced hyperlipidaemic rats. Rats were made hyperlipidaemic by intraperitoneal administration of P-407 (400 mg/kg). Serum lipid levels such as total cholesterol, triglycerides and low-density lipoprotein cholesterol increased significantly (P < 0.001) compared with normal control rats. All these changes were significantly prevented in the rats treated with swertiamarin. Serum high-density lipoprotein (HDL) cholesterol was found to be reduced in the P-407 control rats. However, administration of swertiamarin significantly (P < 0.01) increased HDL levels and it showed a significant lipid-lowering effect, as well as a high antiatherogenic potential. Overall swertiamarin is an effective lipid-lowering lead compound and can be useful for preventing atherosclerosis.


Asunto(s)
Glucósidos/farmacología , Hipolipemiantes/farmacología , Iridoides/farmacología , Poloxámero/farmacología , Pironas/farmacología , Animales , Hiperlipidemias/inducido químicamente , Hiperlipidemias/tratamiento farmacológico , Glucósidos Iridoides , Masculino , Ratas , Ratas Wistar
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