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1.
J Ethnopharmacol ; 250: 112461, 2020 Mar 25.
Artículo en Inglés | MEDLINE | ID: mdl-31830549

RESUMEN

ETHNOPHARMACOLOGICAL RELEVANCE: Phyllanthus niruri have a long history of use in the traditional treatment of various ailments including hypertension. Literature reports have indicated that it is a potent antihypertensive herbal medication used traditionally. AIM OF THE STUDY: This study was carried out to investigate the antihypertensive and vasodilatory activity of four solvents extracts of P. niruri namely; petroleum ether (PEPN), chloroform (CLPN), methanol (MEPN) and water (WEPN), with the aim of elucidating the mechanism of action and identifying the phytochemical constituents. MATERIALS AND METHODS: Male Spontaneous Hypertensive Rats (SHRs) were given oral gavage of P. niruri extract daily for two weeks and the blood pressure was recorded in vivo. We also determine the vasodilation effect of the extracts on rings of isolated thoracic aorta pre-contracted with phenylephrine (PE, 1 µM). Endothelium-intact or endothelium-denuded aorta rings were pre-incubated with various antagonists like 1H-[1,2,4] oxadiazolo-[4,3-a]quinoxalin-1-one (ODQ, 10 µM) and Methylene blue (MB 10 µM), sGC inhibitors; Nω-Nitro-L-arginine methyl ester hydrochloride (L-NAME, 10 µM) a nitric oxide synthase (NOS) inhibitor; atropine (10 µM), a cholinergic receptor blocker; indomethacin (10 µM), a cyclooxygenase inhibitor and various K+ channel blockers such as glibenclamide (10 µM) and tetraethyl ammonium (TEA 10 µM) for mechanism study. RESULTS: SHRs receiving P. niruri extracts showed a significant decrease in their blood pressure (BP) when compared to the baseline value, with PEPN being more potent. The extracts (0.125-4 mg/mL) also induced vasorelaxation on endothelium-intact aorta rings. PEPN elicited the most potent maximum relaxation effect (Rmax). Mechanism assessment of PEPN showed that its relaxation effect is significantly suppressed in endothelium-denuded aorta rings. Pre-incubation of aorta rings with atropine, L-NAME, ODQ, indomethacin, and propranolol also significantly attenuated its relaxation effect. Conversely, incubation with TEA and glibenclamide did not show a significant effect on PEPN-induced relaxation. CONCLUSION: This study indicates that the antihypertensive activity of P. niruri extract is mediated by vasoactive phytoconstituents that dilate the arterial wall via endothelium-dependent pathways and ß-adrenoceptor activity which, in turn, cause vasorelaxation and reduce blood pressure.


Asunto(s)
Antihipertensivos/farmacología , Phyllanthus , Extractos Vegetales/farmacología , Vasodilatadores/farmacología , Animales , Antihipertensivos/química , Aorta Torácica/efectos de los fármacos , Aorta Torácica/fisiología , Presión Sanguínea/efectos de los fármacos , GMP Cíclico/fisiología , Frecuencia Cardíaca/efectos de los fármacos , Hipertensión/tratamiento farmacológico , Hipertensión/fisiopatología , Técnicas In Vitro , Óxido Nítrico/fisiología , Fitoquímicos/análisis , Fitoquímicos/farmacología , Extractos Vegetales/química , Ratas Endogámicas SHR , Ratas Sprague-Dawley , Receptores Adrenérgicos beta/fisiología , Transducción de Señal/efectos de los fármacos , Vasodilatación/efectos de los fármacos , Vasodilatadores/química
2.
Artículo en Inglés | MEDLINE | ID: mdl-30108657

RESUMEN

Pseudomonas aeruginosa is naturally resistant to many classes of antipseudomonal antibiotics due to the species ability to easily acquire resistance. Plant-based antibacterial agent in combination with the existing antibiotic proposes an alternative treatment regimen for the eradication of resistant bacterial infections. The antibacterial effects of the isolated epicatechin 3-gallate compound from Euphorbia hirta in combination with cefepime were investigated in vitro against resistant P. aeruginosa. The fractional inhibitory concentration index of the combination was determined using checkerboard broth microdilution method. Epicatechin 3-gallate combined with cefepime had produced synergistic effect against P. aeruginosa (with average FIC index of 0.24). The MIC of epicatechin 3-gallate was effectively reduced to MIC/4, MIC/8, MIC/16, and MIC/32 in the presence of cefepime. Time-kill study of epicatechin 3-gallate combined with cefepime exhibited remarkable bactericidal activity where the eradication of P. aeruginosa occurred within 4 h of treatment. Scanning electron micrographs revealed apparent cell membrane damage and leakage of cytoplasmic contents from P. aeruginosa cells which eventually led to the cell lysis after the combination treatment of epicatechin 3-gallate and cefepime. The potential of epicatechin 3-gallate to act synergistically with cefepime against clinically resistant P. aeruginosa strain possibly will maximize the successful outcomes when choosing empirical antibiotic treatment in hospitals or health care institutions.

3.
Pharmacogn Mag ; 13(Suppl 2): S311-S315, 2017 Jul.
Artículo en Inglés | MEDLINE | ID: mdl-28808398

RESUMEN

BACKGROUND: The escalating dominance of resistant Pseudomonas aeruginosa strains as infectious pathogen had urged the researchers to look for alternative and complementary drugs. OBJECTIVE: The objective of this study is to address the biological targets and probable mechanisms of action underlying the potent antibacterial effect of the isolated compounds from Euphorbia hirta (L.) against P. aeruginosa. MATERIALS AND METHODS: The action mechanisms of caffeic acid (CA) and epicatechin 3-gallate (ECG) on P. aeruginosa cells were investigated by several bacterial physiological manifestations involving outer membrane permeabilization, intracellular potassium ion efflux, and nucleotide leakage. RESULTS: The findings revealed that ECG and CA targeted both cell wall and cytoplasmic membrane of P. aeruginosa. The cellular membrane destruction and ensuing membrane permeability perturbation of P. aeruginosa had led to the ascending access of hydrophobic antibiotics, release of potassium ions, and leakages of nucleotides. CONCLUSION: The overall study concludes that ECG and CA isolated from E. hirta possess remarkable anti-infective potentials which can be exploited as drug template for the development of new antibacterial agent against resistant P. aeruginosa pathogen. SUMMARY: Epicatechin 3-gallate (ECG) and caffeic acid (CA) exhibited remarkable bactericidal abilities by increasing the outer membrane and plasma membrane permeability of Pseudomonas aeruginosa pathogenECG and CA had facilitated the entry of hydrophobic antibiotics into P. aeruginosa by disintegrating the lipopolysaccharides layer of the outer membraneECG-induced potassium efflux with efficiency close to that obtained with cefepime suggesting mode of action through membrane disruptionBoth ECG and CA had caused consistent leakage of intracellular nucleotide content with the increase in time. Abbreviations used: ECG: Epicatechin 3-gallate; CA: Caffeic acid; E. hirta: Euphoria hirta.

4.
J Ethnopharmacol ; 189: 253-76, 2016 Aug 02.
Artículo en Inglés | MEDLINE | ID: mdl-27220655

RESUMEN

ETHNOPHARMACOLOGICAL RELEVANCE: Kigelia africana is a quintessential African herbal medicinal plant with a pan-African distribution and immense indigenous medicinal and non-medicinal applications. The plant is use traditionally as a remedy for numerous disease such as use wounds healing, rheumatism, psoriasis, diarrhea and stomach ailments. It is also use as an aphrodisiac and for skin care. AIM OF THE REVIEW: The present review aims to compile an up-to-date review of the progress made in the continuous pharmacological and phytochemistry investigation of K. africana and the corresponding commercial and pharmaceutical application of these findings with the ultimate objective of providing a guide for future research on this plant. METHOD: The scholarly information needed for this paper were predominantly sourced from the electronic search engines such as Google, Google scholar; publishing sites such as Elsevier, scienceDirect, BMC, PubMed; other scientific database sites for chemicals such as ChemSpider, PubChem, and also from online books. RESULTS: Pharmacological investigations conducted confirm the anti-inflammatory, analgesic, antioxidant and anticancer activity of the extract of different parts of the plant. Bioactive constituents are found to be present in all parts of the plant. So far, approximately 150 compounds have been characterized from different part of the plant. Iridoids, naphthoquinones, flavonoids, terpenes and phenylethanoglycosides are the major class of compounds isolated. Novel compounds with potent antioxidant, antimicrobial and anticancer effect such as verbascoside, verminoside and pinnatal among others, have been identified. Commercial trade of K. africana has boosted in the las few decades. Its effect in the maintenance of skin has been recognized resulting in a handful of skin formulations in the market. CONCLUSIONS: The pharmaceutical potentials of K. africana has been recognized and have witness a surge in research interest. However, till date, many of its traditional medicinal uses has not been investigated scientifically. Further probing of the existential researches on its pharmacological activity is recommended with the end-goal of unravelling the pharmacodynamics, pharmacokinetics, clinical relevance and possible toxicity and side effects of both the extract and the active ingredients isolated.


Asunto(s)
Bignoniaceae/química , Medicinas Tradicionales Africanas , Fitoquímicos/farmacología , Extractos Vegetales/farmacología , África , Animales , Etnobotánica , Etnofarmacología , Humanos , Fitoquímicos/química , Fitoquímicos/aislamiento & purificación , Fitoquímicos/toxicidad , Extractos Vegetales/química , Extractos Vegetales/aislamiento & purificación , Extractos Vegetales/toxicidad , Medición de Riesgo , Pruebas de Toxicidad
5.
Med Sci (Basel) ; 4(1)2016 Mar 08.
Artículo en Inglés | MEDLINE | ID: mdl-29083368

RESUMEN

Alstonia scholaris has been used by traditional medicine practitioners since the medieval ages for the treatment of diseases. The aim of this research was to evaluate the acute and sub-acute oral toxicity of its methanolic extract. The acute toxicity test was conducted using Sprague Dawley (SD) rats. The methanolic extract of Alstonia scholaris stem bark (ASME) was administrated in a single dose of 2000 mg/kg via oral gavage; and the animals were observed for any behavioral changes or mortality. In the sub-acute toxicity study, SD rats received three doses of ASME (250, 500 and 1000 mg/kg) for 28 days via oral gavage. During these 28 days of treatment, the rats were observed weekly for toxicity symptoms. Following the 28-day treatment, the rats were sacrificed for hematological, biochemical and histopathology studies. In the acute toxicity study, Alstonia scholaris was found to be non-toxic at a dose of 2000 mg/kg b.w. In the sub-acute toxicity study, significant variations in body weight, hematological and biochemical parameters were observed in the experimental groups at the dose of 500 and 1000 mg/kg with the death of two female rats being recorded at the highest dose (1000 mg/kg b.w.). Histopathological studies revealed slight degeneration (lesion) and centrilobular necrosis in the liver, which was most expressed in the highest-dose group. These results demonstrate that, while a single dose and short term oral intake of Alstonia scholaris bark extract caused no toxicity up to a dose of 2000 mg/kg b.w., toxic effects manifested in the long term treatment at the highest dose (500 and 1000 mg/kg). The long-term toxic effect was found to be associated with alterations in hematological compositions and end-organ damage to the liver. Thus, prolonged use of high doses of ASME orally should be discouraged and lower doses encouraged.

6.
J Ethnopharmacol ; 175: 422-31, 2015 Dec 04.
Artículo en Inglés | MEDLINE | ID: mdl-26429073

RESUMEN

ETHNOPHARMACOLOGICAL RELEVANCE: Alstonia scholaris has a long history of use in the Ayurveda traditional treatment of various ailments including hypertension. We have reported the blood pressure lowering activity of the extract of A. scholaris. The following research aim to delineate the pharmacological mechanism involve in the antihypertensive action. MATERIALS AND METHOD: Vasorelaxant effect of the n-butanol fraction of A. scholaris (NBF-ASME) was evaluated on rat aorta pre-contracted with phenyelphrine (PE, 1 µM). Aortic rings preparation were pre-incubated with various antagonists like 1H-[1,2,4] oxadiazolo-[4,3-a]quinoxalin-1-one (ODQ 10 µM), methylene blue (MB 10 µM), Nω-nitro-L-arginine methyl ester hydrochloride (l-NAME 10 µM), atropine (10 µM), indomethacin (1 µM), ML-9 and various K(+) channel blockers such as glibenclamide (10 µM) and tetraethyl ammonium (TEA 10 µM) for mechanism study. RESULT: The results showed that pre-incubation of aortic rings with the extract (0.5, 1 and 2mg/mL) significantly inhibit the contractile response of the rings to phenylephrine-induced contraction (p<0.05-0.001). Removal of endothelium, incubation with L-NAME, indomethacin, atropine and propranolol did not significantly affect the relaxation effect of NBF-ASME. Furthermore, the K(+) channel blockers, TEA and glibenclamide showed no inhibitory effect. However, aortic rings pretreated with ODQ and ML-9 showed a significant suppression of the relaxation curve of NBF-ASME (p<0.01-0.001). In Ca(2+)-free solution, NBF-ASME inhibits the release of intracellular Ca(2+) from the sarcoplasmic reticulum. NBF-ASME also inhibits calcium chloride (CaCl2)-induced contraction in endothelium-denuded aortic rings. CONCLUSION: The results from this study suggests that A. scholaris exerts vasodilation via calcium channels blockade, direct activation of soluble guanylate cyclase and possibly by also inhibiting the formation of inositol 1, 4, 5-triphosphate.


Asunto(s)
Alstonia , Antihipertensivos/farmacología , Bloqueadores de los Canales de Calcio/farmacología , Extractos Vegetales/farmacología , Vasodilatadores/farmacología , 1-Butanol/química , Antagonistas de Receptores Adrenérgicos alfa 1/farmacología , Antagonistas Adrenérgicos beta/farmacología , Animales , Aorta Torácica/efectos de los fármacos , Aorta Torácica/fisiología , GMP Cíclico/metabolismo , Guanilato Ciclasa/metabolismo , Inositol 1,4,5-Trifosfato/metabolismo , Antagonistas Muscarínicos/farmacología , Óxido Nítrico/metabolismo , Corteza de la Planta , Bloqueadores de los Canales de Potasio/farmacología , Ratas Sprague-Dawley , Receptores Citoplasmáticos y Nucleares/metabolismo , Guanilil Ciclasa Soluble , Solventes/química , Vasoconstricción/efectos de los fármacos
7.
Asian Pac J Trop Med ; 8(8): 595-605, 2015 Aug.
Artículo en Inglés | MEDLINE | ID: mdl-26321511

RESUMEN

OBJECTIVES: To study the antidiabetic and antioxidant activities of nipa palm vinegar (NPV) used in traditional Malay medicine for treating diabetes. METHODS: NPV was extracted using liquid-liquid extraction method and the obtained samples were subjected to antidiabetic studies using normal and streptozotocin-induced diabetic rat models whereas antidoxidant activities were investigated via in vitro antioxidant tests namely 2,2-diphenyl-1-picrylhydrazyl and 2,2'-azinobis-3-ethylbenzothiozoline-6-sulfonic acid free radicals scavenging activities and the reducing power assay. RESULTS: Single administration of NPV and its extracts were not effective in both normal and diabetic rats. In intraperitoneal glucose tolerance test, NPV and its aqueous extract showed significant blood glucose lowering effect. In the sub-acute study, compared with the diabetic control, aqueous extract of NPV showed the most notable blood glucose lowering effect (56.6%) and a significant improvement in serum insulin levels (79.8%, P < 0.05). To assess NPV's antioxidant activity, three in vitro antioxidant tests were employed: 2,2-diphenyl-1-picrylhydrazyl and 2,2'-azinobis-3-ethylbenzothiozoline-6-sulfonic acid free radical-scavenging assays, and the reducing power assay. Ethyl acetate extract had the greatest antioxidant potential and content of phenolic and flavonoid compounds. A linear positive correlation between the antioxidant parameters was observed. Chemical profiling analysis of aqueous extract of NPV revealed the presence of acetic acid (35.25%), the main active constituent which significantly contributed to the observed antidiabetic activity. CONCLUSIONS: Aqueous extract of NPV possesses antihyperglycaemic activities comparable to the metformin, while the ethyl acetate extract precipitated significant antioxidant effects attributable to its high phenolic content. These findings suggest that antioxidant compounds of NPV do not contribute much towards the overall observed antidiabetic effect.

8.
Nutrients ; 7(8): 7012-26, 2015 Aug 20.
Artículo en Inglés | MEDLINE | ID: mdl-26308046

RESUMEN

Nypa fruticans Wurmb. vinegar, commonly known as nipa palm vinegar (NPV) has been used as a folklore medicine among the Malay community to treat diabetes. Early work has shown that aqueous extract (AE) of NPV exerts a potent antihyperglycemic effect. Thus, this study is conducted to evaluate the effect of AE on postprandial hyperglycemia in an attempt to understand its mechanism of antidiabetic action. AE were tested via in vitro intestinal glucose absorption, in vivo carbohydrate tolerance tests and spectrophotometric enzyme inhibition assays. One mg/mL of AE showed a comparable outcome to the use of phloridzin (1 mM) in vitro as it delayed glucose absorption through isolated rat jejunum more effectively than acarbose (1 mg/mL). Further in vivo confirmatory tests showed AE (500 mg/kg) to cause a significant suppression in postprandial hyperglycemia 30 min following respective glucose (2 g/kg), sucrose (4 g/kg) and starch (3 g/kg) loadings in normal rats, compared to the control group. Conversely, in spectrophotometric enzymatic assays, AE showed rather a weak inhibitory activity against both α-glucosidase and α-amylase when compared with acarbose. The findings suggested that NPV exerts its anti-diabetic effect by delaying carbohydrate absorption from the small intestine through selective inhibition of intestinal glucose transporters, therefore suppressing postprandial hyperglycemia.


Asunto(s)
Arecaceae/química , Hiperglucemia/tratamiento farmacológico , Extractos Vegetales/farmacología , Animales , Glucemia/metabolismo , Prueba de Tolerancia a la Glucosa , Concentración de Iones de Hidrógeno , Hipoglucemiantes/farmacología , Absorción Intestinal/efectos de los fármacos , Modelos Lineales , Masculino , Ratas , Ratas Sprague-Dawley , alfa-Amilasas/metabolismo , alfa-Glucosidasas/metabolismo
9.
Artículo en Chino | WPRIM | ID: wpr-672434

RESUMEN

Objective:To study the antidiabetic and antioxidant activities of nipa palm vinegar (NPV) used in traditional Malay medicine for treating diabetes.Methods:NPV was extracted using liquid-liquid extraction method and the obtained samples were subjected to antidiabetic studies using normal and streptozotocin-induced diabetic rat models whereas antidoxidant activities were investigated viain vitroantioxidant tests namely 2,2-diphenyl-1-picrylhydrazyl and 2,2’-azinobis-3-ethylbenzothiozoline-6-sulfonic acid free radicals scavenging activities and the reducing power assay.Results:Single administration of NPV and its extracts were not effective in both normal and diabetic rats. In intraperitoneal glucose tolerance test, NPV and its aqueous extract showed significant blood glucose lowering effect. In the sub-acute study, compared with the diabetic control, aqueous extract of NPV showed the most notable blood glucose lowering effect (56.6%) and a significant improvement in serum insulin levels (79.8%, P<0.05). To assess NPV’s antioxidant activity, threein vitro antioxidant tests were employed:2,2-diphenyl-1-picryhydrazyl and 2,2’-azinobis-3-ethylbenzothiozoline-6-sulfonic acid free radical-scavenging assays, and the reducing power assay. Ethyl acetate extract had the greatest antioxidant potential and content of phenolic and flavonoid compounds. A linear positive correlation between the antioxidant parameters was observed. Chemical profiling analysis of aqueous extract of NPV revealed the presence of acetic acid (35.25%), the main active constituent which significantly contributed to the observed antidiabetic activity.Conclusions:Aqueous extract of NPV possesses antihyperglycaemic activities comparable to the metformin, while the ethyl acetate extract precipitated significant antioxidant effects attributable to its high phenolic content. These findings suggest that antioxidant compounds of NPV do not contribute much towards the overall observed antidiabetic effect.

10.
BMC Complement Altern Med ; 13: 346, 2013 Dec 09.
Artículo en Inglés | MEDLINE | ID: mdl-24321370

RESUMEN

BACKGROUND: The frequent occurrences of antibiotic-resistant biofilm forming pathogens have become global issue since various measures that had been taken to curb the situation led to failure. Euphorbia hirta, is a well-known ethnomedicinal plant of Malaysia with diverse biological activities. This plant has been used widely in traditional medicine for the treatment of gastrointestinal, bronchial and respiratory ailments caused by infectious agents. METHODS: In the present study, chemical compositions of methanol extract of E. hirta L. aerial part was analyzed by gas chromatography and gas chromatography coupled to mass spectrometry. A relevant in vitro model was developed to assess the potency of the E. hirta extract to inhibit the bacterial biofilm formation as well as to eradicate the established biofilms. Besides biofilm, E. hirta extract was also evaluated for the inhibition efficacy on planktonic cells using tetrazolium microplate assay. For these purposes, a panel of clinically resistant pathogens and American type culture collection (ATCC) strains were used. RESULTS: The methanolic extract of aerial part of E. hirta was predominantly composed of terpenoid (60.5%) which is often regarded as an active entity accountable for the membrane destruction and biofilm cell detachment. The highest antibacterial effect of crude E. hirta extract was observed in the clinical isolates of Pseudomonas aeruginosa with minimum inhibitory concentration (MIC) value of 0.062 mg/ml. The extract also displayed potent biofilm inhibition and eradication activity against P. aeruginosa with minimum biofilm inhibition concentration (MBIC) and minimum biofilm eradication concentration (MBEC) values of 0.25 mg/ml and 0.5 mg/ml, respectively. CONCLUSIONS: The crude methanol extract of E. hirta has proven to have interesting and potential anti-biofilm properties. The findings from this study will also help to establish a very promising anti-infective phytotherapeutical to be exploited in the pharmaceutical industries.


Asunto(s)
Antibacterianos/farmacología , Biopelículas/efectos de los fármacos , Euphorbia/química , Extractos Vegetales/farmacología , Antibacterianos/química , Bacterias/efectos de los fármacos , Infecciones Bacterianas/microbiología , Cromatografía de Gases y Espectrometría de Masas , Humanos , Metanol , Pruebas de Sensibilidad Microbiana , Componentes Aéreos de las Plantas/química , Extractos Vegetales/química
11.
BMC Complement Altern Med ; 13: 39, 2013 Feb 20.
Artículo en Inglés | MEDLINE | ID: mdl-23425283

RESUMEN

BACKGROUND: One vital therapeutic approach for the treatment of type 2 diabetes mellitus is the use of agents that can decrease postprandial hyperglycaemia by inhibiting carbohydrate digesting enzymes. The present study investigated the effects of bioassay-guided extract and fractions of the dried fruit pericarp of Phaleria macrocarpa, a traditional anti-diabetic plant, on α-glucosidase and α-amylase, in a bid to understand their anti-diabetic mechanism, as well as their possible attenuation action on postprandial glucose increase. METHODS: Methanol extract (ME), obtained by successive solvent extraction, its most effective liquid-liquid n-butanol fraction (NBF) and the flash column chromatographic sub-fraction (SFI), were evaluated for in vitro α-glucosidase (yeast) and α-amylase (porcine) activity inhibition. Furthermore, confirmatory in vivo tests were carried out in streptozotocin-induced diabetic rats (SDRs) using oral glucose, sucrose and starch tolerance tests. RESULTS: At the highest concentration employed (100 µg/ml), NBF showed highest inhibition against α-glucosidase (75%) and α-amylase (87%) in vitro (IC50 = 2.40 ± 0.23 µg/ml and 58.50 ± 0.13 µg/ml, respectively) in a dose-dependent fashion; an effect found to be about 20% higher than acarbose (55%), a standard α-glucosidase inhibitor (IC50 = 3.45 ± 0.19 µg/ml). The ME and SFI also inhibited α-glucosidase (IC50 = 7.50 ± 0.15 µg/ml and 11.45 ± 0.28 µg/ml) and α-amylase (IC50 = 43.90 ± 0.19 µg/ml and 69.80 ± 0.25 µg/ml), but to a lesser extent. In in vivo studies with diabetic rats, NBF and SFI effectively reduced peak blood glucose (PBG) by 15.08% and 6.46%, and the area under the tolerance curve (AUC) by 14.23% and 12.46%, respectively, after an oral sucrose challenge (P < 0.05); thereby validating the observed in vitro action. These reduction effects on PBG and AUC were also demonstrated in glucose and starch tolerance tests, but to a lesser degree. CONCLUSIONS: These findings reveal that P. macrocarpa can attenuate hyperglycaemia in both in vitro and in vivo conditions by potently inhibiting carbohydrate hydrolysing enzymes, making it a viable plant for sourcing natural compounds for the management of type 2 diabetes mellitus.


Asunto(s)
Diabetes Mellitus Experimental/tratamiento farmacológico , Carbohidratos de la Dieta/metabolismo , Inhibidores de Glicósido Hidrolasas , Hiperglucemia/prevención & control , Extractos Vegetales/uso terapéutico , Thymelaeaceae , alfa-Amilasas/antagonistas & inhibidores , Animales , Área Bajo la Curva , Glucemia/metabolismo , Diabetes Mellitus Experimental/enzimología , Diabetes Mellitus Experimental/metabolismo , Diabetes Mellitus Tipo 2/tratamiento farmacológico , Digestión/efectos de los fármacos , Relación Dosis-Respuesta a Droga , Frutas , Hiperglucemia/metabolismo , Hipoglucemiantes/farmacología , Hipoglucemiantes/uso terapéutico , Masculino , Extractos Vegetales/farmacología , Ratas , Ratas Sprague-Dawley , Sacarosa/metabolismo
12.
J Acupunct Meridian Stud ; 5(4): 176-82, 2012 Aug.
Artículo en Inglés | MEDLINE | ID: mdl-22898066

RESUMEN

Orthosiphon stamineus extracts contain three flavonoids (3'-hydroxy-5,6,7,4'-tetramethoxyflavone, sinensetin, and eupatorin) as bioactive substances. Previous reported high performance liquid chromatography- ultraviolet (HPLC-UV) methods for the determination of these flavonoids have several disadvantages, including unsatisfactory separation times and not being well validated according to International Conference on Harmonisation of Technical Requirements for Registration of Pharmaceuticals for Human Use (ICH) standard guidelines. A rapid, specific reversed-phase HPLC method with isocratic elution of acetonitrile: isopropyl alcohol: 20mM phosphate buffer (NaH(2)PO(4)) (30:15:55, v/v) (pH 3.5) at a flow-rate of 1ml/minute, a column temperature of 25°C, and ultraviolet (UV) detection at 340 nm was developed. The method was validated and applied for quantification of different types of O stamineus extracts and fractions. The method allowed simultaneous determination of 3'-hydroxy-5,6,7,4'-tetramethoxyflavone, sinensetin, and eupatorin in the concentration range of 0.03052-250 µg/ml. The limits of detection and quantification, respectively, were 0.0076 and 0.061 µg/ml for 3'-hydroxy-5,6,7,4'-tetramethoxyflavone, 0.0153 and 0.122 µg/ml for sinensetin and 0.0305 and 0.122 µg/ml for eupatorin. The percent relative standard deviation (% RSD) values for intraday were 0.048-0.368, 0.025-0.135, and 0.05-0.476 for 3'-hydroxy-5,6,7,4'-tetramethoxyflavone, sinensetin, and eupatorin, respectively, and those for intraday precision were 0.333-1.688, 0.722-1.055, and 0.548-1.819, respectively. The accuracy for intraday were 91.25%-103.38%, 94.32%-109.56%, and 92.85%-109.70% for 3'-hydroxy-5,6,7,4'-tetramethoxyflavone, sinensetin, and eupatorin, respectively, and those for interday accuracy were 97.49%-103.92%, 103.58%-104.57%, and 103.9%-105.33%, respectively. The method was found to be simple, accurate and precise and is recommended for routine quality control analysis of O stamineus extract containing the three flavonoids as the principle components in the extract.


Asunto(s)
Cromatografía Líquida de Alta Presión/métodos , Flavonas/análisis , Flavonoides/análisis , Orthosiphon/química , Extractos Vegetales/análisis
13.
Molecules ; 17(5): 4986-5002, 2012 Apr 30.
Artículo en Inglés | MEDLINE | ID: mdl-22547320

RESUMEN

An earlier anti-hyperglycemic study with serial crude extracts of Phaleria macrocarpa (PM) fruit indicated methanol extract (ME) as the most effective. In the present investigation, the methanol extract was further fractionated to obtain chloroform (CF), ethyl acetate (EAF), n-butanol (NBF) and aqueous (AF) fractions, which were tested for antidiabetic activity. The NBF reduced blood glucose (p < 0.05) 15 min after administration, in an intraperitoneal glucose tolerance test (IPGTT) similar to metformin. Moreover, it lowered blood glucose in diabetic rats by 66.67% (p < 0.05), similar to metformin (51.11%), glibenclamide (66.67%) and insulin (71.43%) after a 12-day treatment, hence considered to be the most active fraction. Further fractionation of NBF yielded sub-fractions I (SFI) and II (SFII), and only SFI lowered blood glucose (p < 0.05), in IPGTT similar to glibenclamide. The ME, NBF, and SFI correspondingly lowered plasma insulin (p < 0.05) and dose-dependently inhibited glucose transport across isolated rat jejunum implying an extra-pancreatic mechanism. Phytochemical screening showed the presence of flavonoids, terpenes and tannins, in ME, NBF and SFI, and LC-MS analyses revealed 9.52%, 33.30% and 22.50% mangiferin respectively. PM fruit possesses anti-hyperglycemic effect, exerted probably through extra-pancreatic action. Magniferin, contained therein may be responsible for this reported activity.


Asunto(s)
Diabetes Mellitus Experimental/tratamiento farmacológico , Frutas/química , Fitoterapia , Extractos Vegetales/administración & dosificación , Thymelaeaceae/química , Animales , Bioensayo , Transporte Biológico , Glucemia/análisis , Fraccionamiento Químico , Diabetes Mellitus Experimental/metabolismo , Femenino , Prueba de Tolerancia a la Glucosa , Gliburida/administración & dosificación , Gliburida/química , Gliburida/uso terapéutico , Hipoglucemiantes/administración & dosificación , Hipoglucemiantes/química , Hipoglucemiantes/uso terapéutico , Insulina/sangre , Yeyuno/metabolismo , Masculino , Metformina/administración & dosificación , Metformina/química , Metformina/uso terapéutico , Metanol/química , Extractos Vegetales/química , Extractos Vegetales/uso terapéutico , Ratas , Ratas Sprague-Dawley , Solventes/química
14.
J Sci Food Agric ; 92(3): 593-7, 2012 Feb.
Artículo en Inglés | MEDLINE | ID: mdl-25520982

RESUMEN

BACKGROUND: In this study the chemical composition, antioxidant activities and cytotoxic effect of the essential oils of Myristica fragrans (nutmeg) and Morinda citrifolia (mengkudu) were determined. RESULTS: Thirty-eight compounds in nutmeg oil and six compounds in mengkudu oil were identified by gas chromatography­mass spectrometry. The free radical scavenging activity of nutmeg oil was superior of that mengkudu oil. The MTT assay of nutmeg oil on human colorectal carcinoma (HCT-116) and human breast carcinoma (MCF-7) cell lines showed IC50 values of 78.61 and 66.45 µg mL⁻¹, respectively. The mengkudu oil exhibited IC50 values of 91.46 and 78.15 µg mL⁻¹ for HCT-116 and MCF-7, respectively. CONCLUSION: The results showed that nutmeg oil can be developed as potent anti-cancer and antioxidant drugs.


Asunto(s)
Antineoplásicos Fitogénicos/farmacología , Antioxidantes/farmacología , Neoplasias de la Mama/tratamiento farmacológico , Neoplasias Colorrectales/tratamiento farmacológico , Morinda/química , Myristica/química , Aceites Volátiles/farmacología , Antineoplásicos Fitogénicos/análisis , Antineoplásicos Fitogénicos/química , Antineoplásicos Fitogénicos/aislamiento & purificación , Antioxidantes/análisis , Antioxidantes/química , Antioxidantes/aislamiento & purificación , Carcinoma/tratamiento farmacológico , Proliferación Celular/efectos de los fármacos , Descubrimiento de Drogas , Etnofarmacología , Femenino , Frutas/química , Cromatografía de Gases y Espectrometría de Masas , Células HCT116 , Humanos , Células MCF-7 , Malasia , Masculino , Aceites Volátiles/química , Aceites Volátiles/aislamiento & purificación , Concentración Osmolar
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