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1.
J Diet Suppl ; 14(3): 323-333, 2017 May 04.
Artigo em Inglês | MEDLINE | ID: mdl-27588327

RESUMO

Flavonoid-rich extract prepared from Glycyrrhiza glabra has been found to be beneficial in patients with functional dyspepsia and was reported to possess some gut health-promoting properties such as antioxidant, anti-inflammatory and anti-Helicobacter pylori activities. In the present study, the flavonoid-rich extract of Glycyrrhiza glabra was evaluated for its compatibility with probiotic strains (Lactobacillus casei, Lactobacillus fermentum, Lactobacillus plantarum, and Streptococcus thermophilus), commercial probiotic drinks, and digestive enzymes (pancreatic α-amylase, α-glucosidase, phytase, xylanase, and pancreatic lipase). Results of this study indicated that the flavonoid-rich extract of Glycyrrhiza glabra is compatible with the tested probiotic strains, probiotic drinks and digestive enzymes.


Assuntos
Digestão/efeitos dos fármacos , Flavonoides/farmacologia , Microbioma Gastrointestinal/efeitos dos fármacos , Glycyrrhiza/química , Extratos Vegetais/farmacologia , Probióticos , 6-Fitase/efeitos dos fármacos , Endo-1,4-beta-Xilanases/efeitos dos fármacos , Humanos , Lactobacillus/efeitos dos fármacos , Lipase/efeitos dos fármacos , alfa-Amilases Pancreáticas/efeitos dos fármacos , Soluções , alfa-Glucosidases/efeitos dos fármacos
2.
Lipids Health Dis ; 12: 45, 2013 Mar 28.
Artigo em Inglês | MEDLINE | ID: mdl-23537396

RESUMO

BACKGROUND: Preparation of some novel heterocyclic compounds with long alkyl and alkenyl chain of cytotoxic activity. METHODS: Gamma linolenic acid, a poly unsaturated fatty acid and stearic acid, a saturated fatty acid were isolated from the microalga Spirulina platensis. Some novel gamma linolenic acid and stearic acid analogues having 1,3,4-oxadiazole and 1,2,4-triazole were synthesized and characterized by IR, 1H NMR, 13C NMR and mass spectral analysis. Cytotoxicity of these compounds was evaluated by the growth inhibition of A-549 cells in-vitro. RESULTS: Compound 1 and 3 showed comparable cytotoxicity against the human lung carcinoma A-549 cell lines.


Assuntos
Citotoxinas/síntese química , Citotoxinas/farmacologia , Spirulina/química , Ácidos Esteáricos/síntese química , Ácidos Esteáricos/farmacologia , Ácido gama-Linolênico/análogos & derivados , Ácido gama-Linolênico/farmacologia , Linhagem Celular Tumoral , Sobrevivência Celular/efeitos dos fármacos , Ensaios de Seleção de Medicamentos Antitumorais , Humanos , Espectroscopia de Ressonância Magnética , Oxidiazóis/química , Triazóis/química
3.
J Ethnopharmacol ; 145(2): 581-6, 2013 Jan 30.
Artigo em Inglês | MEDLINE | ID: mdl-23220194

RESUMO

ETHNOPHARMACOLOGICAL RELEVANCE: Glycyrrhiza glabra Linn. is regarded useful for peptic ulcer in traditional systems of medicine in India and Helicobacter pylori has been considered as one of the causative factors for peptic ulcer. Aim of the present study is to evaluate the anti-Helicobacter pylori action of GutGard(®), a flavonoid rich extract of Glycyrrhiza glabra and further to elucidate the possible mechanisms of its anti-Helicobacter pylori action. MATERIALS AND METHODS: Agar dilution and microbroth dilution methods were used to determine the minimum inhibitory concentration of GutGard(®) against Helicobacter pylori. Protein synthesis, DNA gyrase, dihydrofolate reductase assays and anti-adhesion assay in human gastric mucosal cell line were performed to understand the mechanisms of anti-Helicobacter pylori activity of GutGard(®). RESULTS: GutGard(®) exhibited anti-Helicobacter pylori activity in both agar dilution and microbroth dilution methods. Glabridin, the major flavonoid present in GutGard(®) exhibited superior activity against Helicobacter pylori while glycyrrhizin did not show activity even at 250 µg/ml concentration. In protein synthesis assay, GutGard(®) showed a significant time dependent inhibition as witnessed by the reduction in (35)S methionine incorporation into Helicobacter pylori ATCC 700392 strain. Additionally, GutGard(®) showed a potent inhibitory effect on DNA gyrase and dihydrofolate reductase with IC(50) value of 4.40 µg/ml and 3.33 µg/ml respectively. However, the extract did not show significant inhibition on the adhesion of Helicobacter pylori to human gastric mucosal cell line at the tested concentrations. CONCLUSION: The present study shows that, GutGard(®) acts against Helicobacter pylori possibly by inhibiting protein synthesis, DNA gyrase and dihydrofolate reductase.


Assuntos
Antibacterianos/farmacologia , Flavonoides/farmacologia , Glycyrrhiza , Helicobacter pylori/efeitos dos fármacos , Extratos Vegetais/farmacologia , DNA Girase/metabolismo , Inibidores Enzimáticos/farmacologia , Antagonistas do Ácido Fólico/farmacologia , Helicobacter pylori/metabolismo , Biossíntese de Proteínas/efeitos dos fármacos , Tetra-Hidrofolato Desidrogenase/metabolismo , Inibidores da Topoisomerase II
4.
J Pharm Pharmacol ; 64(10): 1501-9, 2012 Oct.
Artigo em Inglês | MEDLINE | ID: mdl-22943181

RESUMO

OBJECTIVES: This study involves the evaluation of Memecylon malabaricum Cogn. (Melastomataceae) leaves for antipsoriatic activity. METHODS: Aqueous extract, hydroalcoholic extract and their fractions of M. malabaricum leaves were evaluated for in-vivo antipsoriatic activity by mouse tail test and for in-vitro antipsoriatic activity using HaCaT cells, lipoxygenase inhibition and thymidine phosphorylase inhibition assays. Extracts and fractions were evaluated for total phenol and flavonoid contents. HPTLC was used for screening and fingerprint analysis of the extracts and active fraction. KEY FINDINGS: M. malabaricum hydroalcoholic extract (MMHA) and water fraction of MMHA (MMHAW) produced significant (P<0.05) percent orthokeratosis in the mouse tail test. All samples except MMHA showed a significant (P < 0.05) reduction in epidermal thickness in the mouse tail test when compared with control. Maximum activity against HaCaT cells was shown by chloroform fraction of MMHA (MMHAC). The M. malabaricum decoction (MMD) and water fraction of MMD (MMDW) showed equally good inhibition of lipoxygenase. In thymidine phosphorylase inhibition assay only MMD showed activity. CONCLUSIONS: The findings of this investigation reveal that the leaves of M. malabaricum have good antipsoriatic potential, which provides scope for further detailed research in to this plant for psoriasis.


Assuntos
Fármacos Dermatológicos/farmacologia , Melastomataceae/química , Extratos Vegetais/farmacologia , Psoríase/tratamento farmacológico , Animais , Linhagem Celular , Cromatografia em Camada Fina , Fármacos Dermatológicos/isolamento & purificação , Modelos Animais de Doenças , Flavonoides/isolamento & purificação , Flavonoides/farmacologia , Humanos , Queratinócitos/efeitos dos fármacos , Queratinócitos/metabolismo , Inibidores de Lipoxigenase/isolamento & purificação , Inibidores de Lipoxigenase/farmacologia , Camundongos , Fenóis/isolamento & purificação , Fenóis/farmacologia , Folhas de Planta , Psoríase/patologia
5.
Eur J Med Chem ; 54: 931-5, 2012 Aug.
Artigo em Inglês | MEDLINE | ID: mdl-22770606

RESUMO

Stearic acid, a saturated fatty acid was isolated from the microalga Spirulina platensis. Some novel stearic acid analogues having 1,3,4-oxadiazole, 1,2,4-triazole and 1,2,4-triazolo-[3,4-b]-1,3,4-thiadiazole are synthesized and characterized by IR, NMR and mass spectral analysis. All the synthesized compounds were screened for antimicrobial activity by using cup plate method. The synthesized compounds have been further screened for their antidepressant activity in swiss albino mice by forced swim test (FST), midbrain dopamine has been estimated and quantified. All the compounds showed good antimicrobial activity and compound 6 showed significant antidepressant activity.


Assuntos
Anti-Infecciosos/síntese química , Anti-Infecciosos/farmacologia , Antidepressivos/síntese química , Antidepressivos/farmacologia , Ácidos Esteáricos/síntese química , Ácidos Esteáricos/farmacologia , Animais , Anti-Infecciosos/química , Antidepressivos/química , Bactérias/efeitos dos fármacos , Comportamento Animal/efeitos dos fármacos , Técnicas de Química Sintética , Dopamina/metabolismo , Fungos/efeitos dos fármacos , Masculino , Camundongos , Ácidos Esteáricos/química , Natação
6.
Biol Pharm Bull ; 27(10): 1683-7, 2004 Oct.
Artigo em Inglês | MEDLINE | ID: mdl-15467220

RESUMO

A series of 8-substituted quinolines were synthesized and tested against seizures induced by maximal electro shock (MES), pentylenetetrazole (scMet) and antihypertensive activities. Neurologic deficit was evaluated by the rotarod test. Among the newly synthesized derivatives, several compounds with a 2-hydroxypropyloxyquinoline moiety displayed excellent anticonvulsant and antihypertensive activities. Compound 20 (8-(3'-(4''-phenylpiperazino)-2'-hydroxypropyloxy)quinoline) was potent in both series as an anticonvulsive agent. 13 (8-(3'-piperazino)-2'-hydroxypropyloxyquinoline) and 14 (8-(3'-imidazolo)-2'-hydroxypropyloxyquinoline) showed very good anticonvulsant activities in the propanol series of compound, whereas in the ethane series, 1 (8-(2'-piperazino-ethanoxy)quinoline) and 2 (8-(2'-imidazolo-ethanoxy)quinoline) were the most active as anticonvulsive agents. Compounds 20 (8-(3'-(4''-phenylpiperazino)-2'-hydroxypropyloxy)quinoline), 13 (8-(3'-piperazino)-2'-hydroxypropyloxyquinoline) and 19 (8-(3'-(4''-ethylpiperazino)-2'-hydroxypropyloxy)quinoline) have shown excellent antihypertensive activity. They have significantly antagonized the pressor response elicited by adrenaline. These pharmacological results suggest that their anticonvulsant and antihypertensive effects may be correlated to the presence of beta-blocking properties, and that those properties depend on the presence of aryloxypropanolamine.


Assuntos
Anticonvulsivantes/síntese química , Anticonvulsivantes/farmacologia , Anti-Hipertensivos/síntese química , Anti-Hipertensivos/farmacologia , Quinolinas/síntese química , Quinolinas/farmacologia , Animais , Anticonvulsivantes/toxicidade , Anti-Hipertensivos/toxicidade , Espectroscopia de Ressonância Magnética , Camundongos , Quinolinas/toxicidade , Ratos , Ratos Wistar , Espectrofotometria Infravermelho , Relação Estrutura-Atividade
7.
Chem Pharm Bull (Tokyo) ; 51(2): 162-70, 2003 Feb.
Artigo em Inglês | MEDLINE | ID: mdl-12576649

RESUMO

In the present study, a series of 2-substituted-pyridines were synthesized and characterized by IR, (1)H-NMR and Elemental Analysis. The compounds were assayed against seizures induced by maximal electro shock (MES) and pentylenetetrazole (scMet). Neurologic deficit was evaluated by the rotarod test. The decrease in the elevated motor activity by introceptive chemical stimuli (amphetamine antagonistic activity) was studied at the dose level of 25 and 50 mg/kg, antihistaminic and cardiac activity were also studied. All the compounds exhibited significant anticonvulsant activity. Compounds 2-(2-hydroxy-3-piperazinopropylamino)-6-aminopyridine, 2-[2-hydroxy-3-(1-imidazolyl)propylamino]-6-aminopyridine, 2-[2-(1-imidazolyl)ethylamino]-6-methylpyridine and 2-[2-(methylamino)ethylamino]-6-methylpyridine were most active of the series against MES-induced seizures. Compounds 2-[2-(phenylamino)ethylamino]-6-aminopyridine, 2-[2-[bis(2-hydroxyethyl)amino]ethylamino]-6-aminopyridine, 2-[2-(diethylamino)ethylamino]-6-methylpyridine and 2-[2-hydroxy-3-(1-imidazolyl)propylamino]-6-methylpyridine exhibited significant decrease in the elevated motor activity at the dose of 50 mg/kg. Remarkable sympathetic blocking activity was observed with 2-(2-hydroxy-3-piperazinopropylamino)-6-aminopyridine, 2-(2-hydroxy-3-morpholinopropylamino)-6-methylpyridine and 2-(2-hydroxy-3-piperazinopropylamino)-6-methylpyridine only. Compounds 2-[2-(diethylamino)ethylamino]-6-aminopyridine, 2-[2-[bis(2-hydroxyethyl)amino]ethylamino]-6-aminopyridine, and 2-[2-(diethylamino)ethylamino]-6-methylpyridine exhibited significant blocking of histamine induced contraction on guinea pig ileum.


Assuntos
Aminopiridinas/química , Aminopiridinas/farmacologia , Coração/efeitos dos fármacos , Íleo/efeitos dos fármacos , Animais , Anuros , Avaliação Pré-Clínica de Medicamentos/métodos , Feminino , Cobaias , Coração/fisiologia , Íleo/fisiologia , Técnicas In Vitro , Masculino , Camundongos , Relação Estrutura-Atividade
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