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1.
J Photochem Photobiol B ; 202: 111674, 2020 Jan.
Artigo em Inglês | MEDLINE | ID: mdl-31778953

RESUMO

The present work showed the preparation of gold (Au NPs) and silver nanoparticles (Ag NPs) using aqueous leaf extract of Clinacanthus nutans Lindau (C. Lindau). The prepared NPs were studied using various microscopic and spectroscopic techniques, which confirmed the formation of crystalline Ag NPs, Au NPs that are stabilized with C. Lindau extract polyphenols. The prepared Au NPs and Ag NPs are studied to assess their comparative analgesic and muscle relaxant activities conducted on BALB/c mice. The muscle relaxant studies displayed that Ag NPs were comparatively higher efficient than Au NPs and methanolic C. Lindau extract in traction examination. Additionally, the analgesic studies exhibited that Ag NPs, Au NPs showed maximum percentage reduction in acetic acid induced writhing at the concentrations of 50, 100 and 150 mg/kg body weight. Further, these results conclude that as prepared Au NPs and Ag NPs prepared from C. Lindau leaf extract demonstrated very good analgesic and muscle relaxant activities for the use of pain management in nursing care.


Assuntos
Acanthaceae/química , Analgésicos/síntese química , Ouro/química , Nanopartículas Metálicas/química , Prata/química , Acanthaceae/metabolismo , Ácido Acético/toxicidade , Analgésicos/farmacologia , Analgésicos/uso terapêutico , Animais , Química Verde , Nanopartículas Metálicas/uso terapêutico , Camundongos , Camundongos Endogâmicos BALB C , Relaxamento Muscular/efeitos dos fármacos , Cuidados de Enfermagem , Dor/induzido quimicamente , Dor/tratamento farmacológico , Manejo da Dor/métodos , Extratos Vegetais/química , Folhas de Planta/química , Folhas de Planta/metabolismo
2.
BMC Complement Altern Med ; 19(1): 257, 2019 Sep 14.
Artigo em Inglês | MEDLINE | ID: mdl-31521140

RESUMO

BACKGROUND: Clinacanthus nutans extracts have been consumed by the cancer patients with the hope that the extracts can kill cancers more effectively than conventional chemotherapies. Our previous study reported its anti-inflammatory effects were caused by inhibiting Toll-like Receptor-4 (TLR-4) activation. However, we are unsure of its anticancer effect, and its interaction with existing chemotherapy. METHODS: We investigated the anti-proliferative efficacy of polar leaf extracts (LP), non-polar leaf extracts (LN), polar stem extract (SP) and non-polar stem extracts (SN) in human breast, colorectal, lung, endometrial, nasopharyngeal, and pancreatic cancer cells using 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide, MTT assay. The most potent extracts was tested along with gemcitabine using our established drug combination analysis. The effect of the combinatory treatment in apoptosis were quantified using enzyme-linked immunosorbent assay (ELISA), Annexin V assay, antibody array and immunoblotting. Statistical significance was analysed using one-way analysis of variance (ANOVA) and post hoc Dunnett's test. A p-value of less than 0.05 (p < 0.05) was considered statistical significance. RESULTS: All extracts tested were not able to induce potent anti-proliferative effects. However, it was found that pancreatic ductal adenocarcinoma, PDAC (AsPC1, BxPC3 and SW1990) were the cell lines most sensitive cell lines to SN extracts. This is the first report of C. nutans SN extracts acting in synergy with gemcitabine, the first line chemotherapy for pancreatic cancer, as compared to conventional monotherapy. In the presence of SN extracts, we can reduce the dose of gemcitabine 2.38-5.28 folds but still maintain the effects of gemcitabine in PDAC. SN extracts potentiated the killing of gemcitabine in PDAC by apoptosis. Bax was upregulated while bcl-2, cIAP-2, and XIAP levels were downregulated in SW1990 and BxPC3 cells treated with gemcitabine and SN extracts. The synergism was independent of TLR-4 expression in pancreatic cancer cells. CONCLUSION: These results provide strong evidence of C. nutans extracts being inefficacious as monotherapy for cancer. Hence, it should not be used as a total substitution for any chemotherapy agents. However, SN extracts may synergise with gemcitabine in the anti-tumor mechanism.


Assuntos
Acanthaceae/química , Antineoplásicos/farmacologia , Apoptose/efeitos dos fármacos , Carcinoma de Células Escamosas/fisiopatologia , Desoxicitidina/análogos & derivados , Neoplasias Pancreáticas/fisiopatologia , Extratos Vegetais/farmacologia , Proteína 3 com Repetições IAP de Baculovírus/genética , Proteína 3 com Repetições IAP de Baculovírus/metabolismo , Carcinoma de Células Escamosas/tratamento farmacológico , Carcinoma de Células Escamosas/genética , Carcinoma de Células Escamosas/metabolismo , Linhagem Celular Tumoral , Proliferação de Células/efeitos dos fármacos , Desoxicitidina/farmacologia , Sinergismo Farmacológico , Humanos , Neoplasias Pancreáticas/tratamento farmacológico , Neoplasias Pancreáticas/genética , Neoplasias Pancreáticas/metabolismo , Proteínas Proto-Oncogênicas c-bcl-2/genética , Proteínas Proto-Oncogênicas c-bcl-2/metabolismo
3.
Molecules ; 24(18)2019 Sep 04.
Artigo em Inglês | MEDLINE | ID: mdl-31487946

RESUMO

Ophiopogonis Radix, also known as Mai-dong in Chinese, was a commonly used traditional Chinese medicine (TCM) and functional health food. Two products of Ophiopogonis Radix are largely produced in the Sichuan and Zhejiang province, which are called "Chuan maidong (CMD)" and "Zhe maidong (ZMD)" respectively. To distinguish and evaluate the quality of CMD and ZMD, an analytical method based on ultra-fast performance liquid chromatography coupled with triple quadrupole-linear ion trap mass spectrometry (UFLC-QTRAP-MS/MS) was established for simultaneous determination of 32 constituents including 4 steroidal saponins, 3 homisoflavonoids, 15 amino acids, and 10 nucleosides in 27 Mai-dong samples from Sichuan and Zhejiang. Furthermore, principal components analysis (PCA), partial least squares discriminant analysis (PLS-DA), t-test, and grey relational analysis (GRA) were applied to discriminate and evaluate the samples from Sichuan and Zhejiang based on the contents of 32 constituents. The results demonstrated that the bioactive constituents in CMD and ZMD were significantly different, and CMD performed better in the quality assessment than ZMD. This study not only provides a basic information for differentiating CMD and ZMD, but offers a new insight into comprehensive evaluation and quality control of Ophiopogonis Radix from two different producing areas.


Assuntos
Acanthaceae/química , Medicina Tradicional Chinesa/normas , Cromatografia Líquida de Alta Pressão , Análise Discriminante , Geografia , Controle de Qualidade , Reprodutibilidade dos Testes , Espectrometria de Massas em Tandem
4.
Life Sci ; 234: 116753, 2019 Oct 01.
Artigo em Inglês | MEDLINE | ID: mdl-31419445

RESUMO

AIMS: Hypertension is a global disease that has been combating the world health for ages. Peristrophe roxburghiana (PR) is used in traditional medicine to treat hypertension and other ailments. The present study examined phytochemical constituents, antioxidant activities and GC-MS analysis of extracts of PR leaf and also evaluated their anti-hypertensive and anti-lipidemic effects in NG-nitro-L-arginine methyl ester (L-NAME) hypertensive rats. METHODS: Wistar rats were grouped into two groups: control and hypertensive. Hypertension was induced in the hypertensive group by oral gavage of 60 mg/kg b.w of L-NAME for 3 weeks. After induction, the hypertensive group was randomly sub-grouped into hypertensive, hypertensive treated and hypertensive untreated groups. These were orally gavaged respectively with 60 mg/kg b.w of L-NAME, 60 mg/kg b.w/day of L-NAME +200 mg/kg b.w of different extracts of PR (aqueous, ethanolic and methanolic extracts) and 60 mg/kg b.w of L-NAME +20 mg/kg b.w ramipril for 3 weeks. The blood pressure was measured by tail-cuff method at the third and sixth weeks. KEY FINDINGS: The results showed that the extracts of PR significantly decrease blood pressure, pro-atherogenic lipids and atherogenic ratios in L-NAME hypertensive rats. White blood cells count, neutrophil count and creatinine level were also effectively decreased by the extracts. Furthermore, the extracts increase serum nitric oxide (NO) level, anti-atherogenic lipid, glutathione level, lymphocyte and platelet count in the rats. SIGNIFICANCE: Extracts of PR leaf decrease blood pressure and increase NO level in L-NAME hypertensive rats and also corrected the hyperlipidemia and inflammatory response arising from the reduction in NO bioavailability.


Assuntos
Acanthaceae/química , Anti-Hipertensivos/uso terapêutico , Hipertensão/tratamento farmacológico , Hipolipemiantes/uso terapêutico , Extratos Vegetais/uso terapêutico , Animais , Anti-Hipertensivos/química , Pressão Sanguínea/efeitos dos fármacos , Hipertensão/sangue , Hipertensão/induzido quimicamente , Hipertensão/fisiopatologia , Hipolipemiantes/química , Lipídeos/sangue , Masculino , NG-Nitroarginina Metil Éster , Óxido Nítrico/sangue , Extratos Vegetais/química , Folhas de Planta/química , Ratos Wistar
5.
Molecules ; 24(17)2019 Aug 28.
Artigo em Inglês | MEDLINE | ID: mdl-31466218

RESUMO

Acanthus ilicifolius herb (AIH), the dry plant of Acanthus ilicifolius L., has long been used as a folk medicine for treating acute and chronic hepatitis. Phenylethanoid glycosides (PhGs) are one family of the main components in AIH with hepatoprotective, antioxidant, and anti-inflammatory activities. In this study, the pharmacokinetics of AIH was investigated preliminarily by ultra-performance liquid chromatography coupled with triple quadrupole mass spectrometry (UPLC-MS/MS). A simultaneously quantitative determination method for four PhGs (acteoside, isoacteoside, martynoside, and crenatoside) in rat plasma was first established by UPLC-MS/MS. These four PhGs were separated with an ACQUITY UPLC BEH C18 column (2.1 × 50 mm, 1.7 µm) by gradient elution (mobile phase: MeCN and 0.1% formic acid in water, 0.4 mL/min). The mass spectrometry detection was performed using negative electrospray ionization (ESI-) in multiple reaction monitoring (MRM) mode. By the established method, the preliminary pharmacokinetics of AIH was elucidated using the kinetic parameters of the four PhGs in rat plasma after intragastric administration of AIH ethanol extract. All four PhGs showed double peaks on concentration-time curves, approximately at 0.5 h and 6 h, respectively. Their elimination half-lives (t1/2) were different, ranging from 3.42 h to 8.99 h, although they shared similar molecular structures. This work may provide a basis for the elucidation of the pharmacokinetic characteristics of bioactive components from AIH.


Assuntos
Acanthaceae/química , Glicosídeos/sangue , Extratos Vegetais/administração & dosagem , Animais , Ácidos Cafeicos/sangue , Ácidos Cafeicos/farmacocinética , Cromatografia Líquida , Glucosídeos/sangue , Glucosídeos/farmacocinética , Glicosídeos/farmacocinética , Masculino , Fenóis/sangue , Fenóis/farmacocinética , Extratos Vegetais/farmacocinética , Ratos , Ratos Sprague-Dawley , Espectrometria de Massas em Tandem
6.
Biomed Res Int ; 2019: 6593125, 2019.
Artigo em Inglês | MEDLINE | ID: mdl-31467905

RESUMO

Methanolic extract of Clinacanthus nutans Lindau leaves (MECN) has been reported to exert antinociceptive activity. The present study aimed to elucidate the possible antinociceptive mechanisms of a lipid-soluble fraction of MECN, which was obtained after sequential extraction in petroleum ether. The petroleum ether fraction of C. nutans (PECN), administered orally to mice, was (i) subjected to capsaicin-, glutamate-, phorbol 12-myristate 13-acetate-, bradykinin-induced nociception model; (ii) prechallenged (intraperitoneal (i.p.)) with 0.15 mg/kg yohimbine, 1 mg/kg pindolol, 3 mg/kg caffeine, 0.2 mg/kg haloperidol, or 10 mg/kg atropine, which were the respective antagonist of α 2-adrenergic, ß-adrenergic, adenosinergic, dopaminergic, or muscarinic receptors; and (iii) prechallenged (i.p.) with 10 mg/kg glibenclamide, 0.04 mg/kg apamin, 0.02 mg/kg charybdotoxin, or 4 mg/kg tetraethylammonium chloride, which were the respective inhibitor of ATP sensitive-, small conductance Ca2+-activated-, large conductance Ca2+-activated-, or nonselective voltage-activated-K+ channel. Results obtained demonstrated that PECN (100, 250, and 500 mg/kg) significantly (P<0.05) inhibited all models of nociception described earlier. The antinociceptive activity of 500 mg/kg PECN was significantly (P<0.05) attenuated when prechallenged with all antagonists or K+ channel blockers. However, only pretreatment with apamin and charybdotoxin caused full inhibition of PECN-induced antinociception. The rest of the K+ channel blockers and all antagonists caused only partial inhibition of PECN antinociception, respectively. Analyses on PECN's phytoconstituents revealed the presence of antinociceptive-bearing bioactive compounds of volatile (i.e., derivatives of γ-tocopherol, α-tocopherol, and lupeol) and nonvolatile (i.e., cinnamic acid) nature. In conclusion, PECN exerts a non-opioid-mediated antinociceptive activity involving mainly activation of adenosinergic and cholinergic receptors or small- and large-conductance Ca2+-activated-K+ channels.


Assuntos
Acanthaceae/química , Analgésicos/farmacologia , Dor Nociceptiva/tratamento farmacológico , Extratos Vegetais/farmacologia , Alcanos/química , Analgésicos/química , Analgésicos não Entorpecentes/química , Analgésicos não Entorpecentes/farmacologia , Animais , Bradicinina/toxicidade , Capsaicina/toxicidade , Ácido Glutâmico/toxicidade , Humanos , Metanol/química , Camundongos , Dor Nociceptiva/induzido quimicamente , Dor Nociceptiva/patologia , Extratos Vegetais/química , Folhas de Planta/química , Canais de Potássio/genética , Acetato de Tetradecanoilforbol/análogos & derivados , Acetato de Tetradecanoilforbol/toxicidade
7.
Int J Mol Sci ; 20(14)2019 Jul 19.
Artigo em Inglês | MEDLINE | ID: mdl-31331112

RESUMO

The extracts of two mangrove species, Bruguiera cylindrica and Laguncularia racemosa, have been analyzed at sub-lethal concentrations for their potential to modulate biofilm cycles (i.e., adhesion, maturation, and detachment) on a bacterium, yeast, and filamentous fungus. Methanolic leaf extracts were also characterized, and MS/MS analysis has been used to identify the major compounds. In this study, we showed the following. (i) Adhesion was reduced up to 85.4% in all the models except for E. coli, where adhesion was promoted up to 5.10-fold. (ii) Both the sum and ratio of extracellular polysaccharides and proteins in mature biofilm were increased up to 2.5-fold and 2.6-fold in comparison to the negative control, respectively. Additionally, a shift toward a major production of exopolysaccharides was found coupled with a major production of both intracellular and extracellular reactive oxygen species. (iii) Lastly, detachment was generally promoted. In general, the L. racemosa extract had a higher bioactivity at lower concentrations than the B. cylindrica extract. Overall, our data showed a reduction in cells/conidia adhesion under B. cylindrica and L. racemosa exposure, followed by an increase of exopolysaccharides during biofilm maturation and a variable effect on biofilm dispersal. In conclusion, extracts either inhibited or enhanced biofilm development, and this effect depended on both the microbial taxon and biofilm formation step.


Assuntos
Acanthaceae/química , Biofilmes/efeitos dos fármacos , Extratos Vegetais/farmacologia , Bactérias/efeitos dos fármacos , Bactérias/crescimento & desenvolvimento , Biofilmes/crescimento & desenvolvimento , Cromatografia Líquida , Fungos/efeitos dos fármacos , Fungos/crescimento & desenvolvimento , Espectrometria de Massas , Metaboloma , Metabolômica/métodos , Extratos Vegetais/química , Folhas de Planta/química , Espécies Reativas de Oxigênio/metabolismo
8.
Pak J Pharm Sci ; 32(2): 697-702, 2019 Mar.
Artigo em Inglês | MEDLINE | ID: mdl-31081785

RESUMO

The present investigation was undertaken to evaluate the antibacterial, antifungal and hemolytic activities of organic and aqueous fractions of Fumaria indica, Dicliptera bupleuroides and Curcuma zedoaria. The methanolic extracts of the plants were dissolved in the water (distilled) separately and then partitioned with the n-hexane, CHCl3, EtOAc and n-BuOH sequentially. Antibacterial activity was checked against Escherichia coli, Pasturella multocida, Bacillus subtilis and Staphylococcus aureus by the disc diffusion method using streptomycin sulphate, a standard antibiotic, as positive control. Antifungal activity was studied against four fungi i.e. Aspergillus niger, Aspergillus flavus, Ganoderma lucidum and Alternaria alternata by the disc diffusion method using fluconazole, a standard antifungal drug, as positive control. It was revealed that aqueous fraction of F. indica showed very good antibacterial activity against P. multocida with zone of inhibition 26mm and MIC of 98µg/mL. Its CHCl3 and n-BuOH fractions also displayed good results. Its CHCl3 fraction showed good antifungal activity against G. lucidum with zone of inhibition 24mm and MIC of 115µg/mL. Other polar fractions of F. indica showed good activity against somefungal strains. The CHCl3 and EtOAc fractions of D. bupleuroides displayed good antibacterial activity against some bacterial strains. Its EtOAc fraction showed good antifungal activity only against G. lucidum. The CHCl3 fraction of C. zedoaria showed good activity against all studied bacterial strains, while its EtOAc and n-BuOH fractions displayed good results against some bacterial strains. None of the fractions of C. zedoaria displayed antifungal activity against the under test strains. All the studied fractions of three plants showed very less toxicity except n-hexane fraction of D. bupleuroides which showed 79% toxicity.


Assuntos
Antibacterianos/farmacologia , Antifúngicos/farmacologia , Hemolíticos/farmacologia , Extratos Vegetais/farmacologia , Plantas Medicinais/química , Acanthaceae/química , Antibacterianos/química , Antifúngicos/química , Curcuma/química , Avaliação Pré-Clínica de Medicamentos , Fumaria/química , Bactérias Gram-Negativas/efeitos dos fármacos , Bactérias Gram-Positivas/efeitos dos fármacos , Hemólise/efeitos dos fármacos , Hemolíticos/química , Humanos , Testes de Sensibilidade Microbiana , Extratos Vegetais/química
9.
J Enzyme Inhib Med Chem ; 34(1): 999-1009, 2019 Dec.
Artigo em Inglês | MEDLINE | ID: mdl-31072143

RESUMO

This study explored the possible bioactive ingredients and target protein of Rostellularia procumbens (L.) Nees. The results of optical turbidimetry revealed that the ethyl acetate extraction obtained from R. procumbens (L.) Nees could inhibit platelet aggregation. Gene chip was used to investigate differentially expressed genes. According to the results of the gene chip, the targets of compounds isolated from the ethyl acetate extraction were predicted by network pharmacology. Computational studies revealed that chinensinaphthol methyl ether and neojusticin B may target the integrin αIIbß3 protein. The results of Prometheus NT.48 and microscale thermophoresis suggested that the molecular interactions between the two compounds with purified integrin αIIbß3 protein in the optimal test conditions were coherent with the docking results. To our best knowledge, this is the first report to state that chinensinaphthol methyl ether and neojusticin B target the integrin αIIbß3 protein.


Assuntos
Acanthaceae/química , Derivados de Benzeno/farmacologia , Dioxolanos/farmacologia , Éteres/farmacologia , Lignanas/farmacologia , Inibidores da Agregação de Plaquetas/farmacologia , Derivados de Benzeno/química , Derivados de Benzeno/isolamento & purificação , Dioxolanos/química , Dioxolanos/isolamento & purificação , Relação Dose-Resposta a Droga , Éteres/química , Éteres/isolamento & purificação , Humanos , Lignanas/química , Lignanas/isolamento & purificação , Agregação Plaquetária/efeitos dos fármacos , Inibidores da Agregação de Plaquetas/química , Inibidores da Agregação de Plaquetas/isolamento & purificação , Testes de Função Plaquetária , Relação Estrutura-Atividade
10.
Appl Biochem Biotechnol ; 189(3): 855-870, 2019 Nov.
Artigo em Inglês | MEDLINE | ID: mdl-31131419

RESUMO

Condensed tannins (CTS) have been isolated and purified from leaves of Acanthus ilicifolius Linn. And their structures were investigated by three methods: 13C nuclear magnetic resonance (13C NMR), reversed-phase high-performance liquid chromatography (RP-HPLC), and matrix-assisted laser desorption/ionization time-of-flight mass spectrometry (MALDI-TOF MS). The results showed that the CTS were a mixture of catechin/epicatechin, galatechin/epicatechin, and amphicin/epigalin, and that the polymer chain lengths were 3-mers to 14-mers. Antityrosinase activities and antioxidant activities of the CTS from A. ilicifolius leaves were further studied. The IC50 of the CTS on mushroom tyrosinase activity was determined to be 19.7 ± 0.13 µg/mL, and inhibition type analyses indicated that the CTS were mixed type inhibitors and their inhibition CTS was reversible. The CTS from A. ilicifolius leaves also exhibited potential antioxidant activity. The IC50 of DPPH and ABTS scavenging activities were 104 ± 0.894 µg/mL and 86 ± 0.616 µg/mL, respectively. And the FRAP value was 758.28 ± 2.42 mg AAE/g. In addition, we found that the CTS from A. ilicifolius leaves had an excellent effect on preserving the quality of fresh-cut apples by preventing apples from browning through reducing polyphenol oxidase activities in apples.


Assuntos
Acanthaceae/química , Antioxidantes/química , Antioxidantes/farmacologia , Malus/efeitos dos fármacos , Taninos/química , Taninos/farmacologia , Agaricales/enzimologia , Antioxidantes/isolamento & purificação , Conservação de Alimentos , Cinética , Malus/metabolismo , Monofenol Mono-Oxigenase/antagonistas & inibidores , Folhas de Planta/química , Polimerização , Taninos/isolamento & purificação
11.
Biomed Pharmacother ; 115: 108901, 2019 Jul.
Artigo em Inglês | MEDLINE | ID: mdl-31079002

RESUMO

An ingredient was isolated from Acanthus ilicifolius and identified as 4-hydroxy-2(3H)-benzoxazolone (HBOA). Its protective effects and underlying mechanism on liver fibrosis were investigated. Briefly, rats were intragastrically administrated with 50% CCl4 twice a week for 12 weeks to induce liver fibrosis. Meanwhile, the animals were treated with various medicines from weeks 8 to 12. Then the histological change, serum biochemical index, inflammatory factors and hepatocyte apoptosis were detected. Moreover, the TGF-ß1/Smads, NF-κB and ERK signaling pathways were also detected to illustrate the underlying mechanism. The results showed that HBOA significantly ameliorated CCl4-induced liver injury and collagen accumulation in rats, as evidenced by the histopathologic improvement. Moreover, HBOA markedly decreased hepatocyte apoptosis by regulating the expression levels of caspase-3, -9 and -12, as well as the Bcl-2 family. The mechanism study showed that HBOA significantly decreased the expressions of α-smooth muscle actin (α-SMA) and collagen and inhibited the generation of excessive extracellular matrix (ECM) components by restoring the balance between matrix metalloproteinases (MMPs) and its inhibitor (TIMPs). HBOA markedly alleviated oxidative stress and inflammatory cytokines through inhibiting the NF-κB pathway. In addition, HBOA significantly down-regulated the levels of TGF-ß1, Smad2/3, Smad4 and up-regulated the level of Smad7, inhibiting the TGF-ß1/Smads signaling pathway. Moreover, HBOA significantly blocked the ERK signaling pathway, leading to the inactivation of hepatic stellate cells. This study suggests that HBOA exerts a protective effect against liver fibrosis via modulating the TGF-ß1/Smads, NF-κB and ERK signaling pathways, which will be developed as a potential agent for the treatment of liver fibrosis.


Assuntos
Anti-Inflamatórios/farmacologia , Benzoxazóis/farmacologia , Cirrose Hepática Experimental/prevenção & controle , Sistema de Sinalização das MAP Quinases/efeitos dos fármacos , NF-kappa B/metabolismo , Proteínas Smad/metabolismo , Fator de Crescimento Transformador beta/metabolismo , Acanthaceae/química , Animais , Anti-Inflamatórios/isolamento & purificação , Benzoxazóis/isolamento & purificação , Tetracloreto de Carbono , Cirrose Hepática Experimental/imunologia , Cirrose Hepática Experimental/metabolismo , Masculino , Medicina Tradicional Chinesa , Estresse Oxidativo/efeitos dos fármacos , Estresse Oxidativo/imunologia , Ratos Sprague-Dawley
12.
BMC Complement Altern Med ; 19(1): 79, 2019 Apr 02.
Artigo em Inglês | MEDLINE | ID: mdl-30940120

RESUMO

BACKGROUND: Methanol extract (MECN) of Clinacanthus nutans Lindau leaves (family Acanthaceae) demonstrated peripherally and centrally mediated antinociceptive activity via the modulation of opioid/NO-mediated, but cGMP-independent pathway. In the present study, MECN was sequentially partitioned to obtain petroleum ether extract of C. nutans (PECN), which was subjected to antinociceptive study with aims of establishing its antinociceptive potential and determining the role of opioid receptors and L-arginine/nitric oxide/cyclic-guanosine monophosphate (L-arg/NO/cGMP) pathway in the observed antinociceptive activity. METHODS: The antinociceptive potential of orally administered PECN (100, 250, 500 mg/kg) was studied using the abdominal constriction-, hot plate- and formalin-induced paw licking-test in mice (n = 6). The effect of PECN on locomotor activity was also evaluated using the rota rod assay. The role of opioid receptors was determined by pre-challenging 500 mg/kg PECN (p.o.) with antagonist of opioid receptor subtypes, namely ß-funaltrexamine (ß-FNA; 10 mg/kg; a µ-opioid antagonist), naltrindole (NALT; 1 mg/kg; a δ-opioid antagonist) or nor-binaltorphimine (nor-BNI; 1 mg/kg; a κ-opioid antagonist) followed by subjection to the abdominal constriction test. In addition, the role of L-arg/NO/cGMP pathway was determined by prechallenging 500 mg/kg PECN (p.o.) with L-arg (20 mg/kg; a NO precursor), 1H-[1, 2, 4] oxadiazolo [4,3-a]quinoxalin-1-one (ODQ; 2 mg/kg; a specific soluble guanylyl cyclase inhibitor), or the combinations thereof (L-arg + ODQ) for 5 mins before subjection to the abdominal constriction test. PECN was also subjected to phytoconstituents analyses. RESULTS: PECN significantly (p < 0.05) inhibited nociceptive effect in all models in a dose-dependent manner. The highest dose of PECN (500 mg/kg) also did not significantly (p > 0.05) affect the locomotor activity of treated mice. The antinociceptive activity of PECN was significantly (p < 0.05) inhibited by all antagonists of µ-, δ-, and κ-opioid receptors. In addition, the antinociceptive activity of PECN was significantly (p < 0.05) reversed by L-arg, but insignificantly (p > 0.05) affected by ODQ. HPLC analysis revealed the presence of at least cinnamic acid in PECN. CONCLUSION: PECN exerted antinocicpetive activity at peripheral and central levels possibly via the activation of non-selective opioid receptors and modulation of the NO-mediated/cGMP-independent pathway partly via the synergistic action of phenolic compounds.


Assuntos
Acanthaceae/química , Analgésicos/farmacologia , GMP Cíclico/metabolismo , Óxido Nítrico/metabolismo , Extratos Vegetais/farmacologia , Receptores Opioides/efeitos dos fármacos , Alcanos , Analgésicos/química , Animais , Masculino , Camundongos , Camundongos Endogâmicos ICR , Extratos Vegetais/química , Folhas de Planta/química , Receptores Opioides/metabolismo , Transdução de Sinais/efeitos dos fármacos
13.
Molecules ; 24(7)2019 04 09.
Artigo em Inglês | MEDLINE | ID: mdl-30970652

RESUMO

The preservation of active constituents in fresh herbs is affected by drying methods. An effective drying method for Strobilanthes crispus which is increasingly marketed as an important herbal tea remains to be reported. This study evaluated the effects of conventional and new drying technologies, namely vacuum microwave drying methods, on the antioxidant activity and yield of essential oil volatiles and phytosterols. These drying methods included convective drying (CD) at 40 °C, 50 °C, and 60 °C; vacuum microwave drying (VMD) at 6, 9, and 12 W/g; convective pre-drying and vacuum microwave finish drying (CPD-VMFD) at 50 °C and 9 W/g; and freeze-drying (FD). GC­MS revealed 33 volatiles, and 2-hexen-1-ol, 2-hexenal, 1-octen-3-ol, linalool, and benzaldehyde were major constituents. The compounds ß-sitosterol and α-linolenic acid were the most abundant phytosterol and fatty acid, respectively, in fresh S. crispus. The highest phenolic content was achieved with CD at 60 °C. The highest antioxidant activity was obtained with CD at 40 °C and VMD at 9 W/g. On the contrary, the highest total volatiles and phytosterols were detected with CD at 50 °C and VMD at 9 W/g, respectively. This study showed that CD and VMD were effective in producing highly bioactive S. crispus. A suitable drying parameter level, irrespective of the drying method used, was an important influencing factor.


Assuntos
Acanthaceae/química , Antioxidantes/análise , Micro-Ondas , Fitosteróis/análise , Liofilização , Vácuo
14.
J Food Sci ; 84(5): 1201-1207, 2019 May.
Artigo em Inglês | MEDLINE | ID: mdl-30942900

RESUMO

The present study investigated the recovery of antioxidative compounds obtained from Pseuderanthemum palatiferum (Nees) Radlk. and their biological activities using subcritical water in comparison with hot water, Soxhlet, and methanol extraction. In this study, high-performance liquid chromatography (HPLC) and three commonly used assays, that is, 2,2-diphenyl-1-picrylhydrazyl assays, 2,2'-azino-bis(3-ethylbenzothiazoline-6-sulfonic acid), and ferric reducing antioxidant power, were employed to measure the number of valuable compounds and their antioxidant capacities, respectively. Additionally, the antimicrobial ability of the various extracts against seven pathogenic bacteria strains was assessed. The results demonstrated that the extracts obtained from subcritical water extraction (SWE) contain the highest amount of saponin (33.82 ± 2.08 mg diosgenin/g), phenolic (34.87 ± 0.29 mg CE/g), and protein (104.66 ± 7.63 mg BSA/g), which are obtained at 170 °C, 190 °C, and 230 °C, respectively. The highest amounts of total sugar and flavonoids (211.73 ± 1.58 mg glucose/g and 20.71 ± 0.42 mg RE/g, respectively) were obtained at lower temperature (130 °C and 130 °C, respectively), and these values were higher than those obtained from hot water, Soxhlet, and methanol extraction. HPLC analysis indicated that the highest amount of apigenin (3.46 ± 0.03 mg/g) and kaempferol (2.43 ± 0.03 mg/g) were obtained by SWE at 170 °C and 190 °C, respectively. Furthermore, the extracts from SWE exhibited higher antimicrobial activity against five of the seven pathogenic bacterial strains tested compared with those obtained from conventional extraction methods. Therefore, subcritical water could be utilized as a cost-effective and green solvent to extract valuable compounds from P. palatiferum (Nees) Radlk. leaf. PRACTICAL APPLICATION: Subcritical water was able to recover more bioactive compounds from the sample, such as phenolics, flavonoids, saponin, protein, and polysaccharides, than conventional solvents. The mixture of polyphenolic-polysaccharide-protein conjugates could be used in further steps, isolation, and purification, and applied to functional food.


Assuntos
Acanthaceae/química , Fracionamento Químico/métodos , Extratos Vegetais/química , Antibacterianos/análise , Antibacterianos/química , Antibacterianos/isolamento & purificação , Antibacterianos/farmacologia , Antioxidantes/análise , Antioxidantes/química , Antioxidantes/isolamento & purificação , Bactérias/efeitos dos fármacos , Cromatografia Líquida de Alta Pressão , Flavonoides/análise , Flavonoides/química , Flavonoides/isolamento & purificação , Fenóis/análise , Fenóis/química , Fenóis/isolamento & purificação , Solventes/química , Temperatura Ambiente , Água/química
15.
Biomed Pharmacother ; 113: 108724, 2019 May.
Artigo em Inglês | MEDLINE | ID: mdl-30877884

RESUMO

AIMS: Clinacanthus nutans (C. nutans) has demonstrated anti-inflammatory activity, however, the active compound generating this activity remains unknown. The aim of this study was to identify the bioactive compound in C. nutans responsible for its anti-inflammatory, in-vitro wound healing, and anti-biofilm activities. MAIN METHODS: A pure compound was isolated from the chloroform extract (CE) of C. nutans leaves by chromatographic techniques and bioassay-guided fractionation. This compound's structure was determined by spectroscopic analyses (FTIR/NMR/HRES-MS). Biological activities were evaluated using cytotoxicity, nitric oxide (NO), wound scratch, anti-microbial activity, and anti-biofilm assays; and the compound's bactericidal depth into the biofilm was visualized by confocal laser scanning microscopy. KEY FINDINGS: CE and its pure isolated compound, purpurin-18 phytyl ester (P18PE), significantly inhibited lipopolysaccharide (LPS)-induced NO production in RAW 264.7 cells at concentrations of 100 µg/ml and 10-100 µg/ml, respectively. These concentrations significantly induced wound closure by human gingival fibroblasts. CE (100-1000µg/ml) and P18PE (1-500 µg/ml) did not inhibit Streptococcus (S.) mutans growth. However, these concentrations significantly reduced S. mutans biofilm formation below 50% at 250 µg/ml for CE, and 25 µg/ml for P18PE (p<0.05). SIGNIFICANCE: C. nutans contains a bioactive compound, P18PE, which exhibits anti-inflammatory, in-vitro wound healing, and anti-biofilm activities.


Assuntos
Biofilmes/efeitos dos fármacos , Óxido Nítrico/antagonistas & inibidores , Porfirinas/farmacologia , Cicatrização/efeitos dos fármacos , Acanthaceae/química , Animais , Anti-Inflamatórios/administração & dosagem , Anti-Inflamatórios/farmacologia , Células Cultivadas , Relação Dose-Resposta a Droga , Ésteres , Fibroblastos/efeitos dos fármacos , Fibroblastos/metabolismo , Gengiva/citologia , Humanos , Lipopolissacarídeos/administração & dosagem , Camundongos , Extratos Vegetais/farmacologia , Folhas de Planta , Porfirinas/química , Porfirinas/isolamento & purificação , Células RAW 264.7 , Streptococcus mutans/efeitos dos fármacos
16.
Biomed Pharmacother ; 113: 108702, 2019 May.
Artigo em Inglês | MEDLINE | ID: mdl-30844658

RESUMO

Rhinacanthus nasutus has traditionally been used in the treatment of various disorders including diabetes mellitus. Rhinacanthins-rich extract (RRE) is a semipurified R. nasutus leaf extract that contains 60% w/w of rhinacanthin-C (RC) obtained by a green extraction process. The purpose of this study was to investigate the anti-hyperglycemic and anti-hyperlipidemic activity of RRE (15 mg/kg equivalent to RC content) in comparison to its marker compound RC (15 mg/kg) and the standard drug glibenclamide (Glb) (600 µg/kg) in nicotinamide-streptozotocin induced diabetic rats for 28 days. In addition, the in silico pharmacokinetic and toxicity analysis of RC was also performed. RRE, RC and Glb significantly reduced the FBG, HbA1c and food/water intake while increasing the insulin level and body weight in diabetic rats without affecting the normal rats. The serum lipid, liver and kidney biomarkers were markedly normalized by RRE, RC and Glb in diabetic rats without affecting the normal rats. Moreover, the histopathology of the pancreas revealed that RRE, RC and Glb evidently restored the islets of Langerhans in diabetic rats. The overall results indicated that RRE has equivalent antidiabetic potential to that of RC. Moreover, the in silico pharmacokinetic and toxicity analysis predicts that RC is orally non-toxic, non-carcinogenic and non-mutagenic with a decent bioavailability. The undertaken study suggests that RRE could be used as an effective natural remedy in the treatment of diabetes.


Assuntos
Acanthaceae/química , Diabetes Mellitus Experimental/tratamento farmacológico , Hipoglicemiantes/uso terapêutico , Hipolipemiantes/uso terapêutico , Naftoquinonas/uso terapêutico , Extratos Vegetais/uso terapêutico , Animais , Peso Corporal/efeitos dos fármacos , Simulação por Computador , Diabetes Mellitus Experimental/metabolismo , Ingestão de Alimentos/efeitos dos fármacos , Hemoglobina A Glicada/análise , Química Verde , Hipoglicemiantes/farmacocinética , Hipoglicemiantes/toxicidade , Hipolipemiantes/farmacocinética , Hipolipemiantes/toxicidade , Resistência à Insulina , Metabolismo dos Lipídeos/efeitos dos fármacos , Masculino , Naftoquinonas/farmacocinética , Naftoquinonas/toxicidade , Niacinamida , Pâncreas/efeitos dos fármacos , Pâncreas/patologia , Extratos Vegetais/farmacocinética , Folhas de Planta/química , Ratos Wistar , Estreptozocina
17.
Phytochemistry ; 162: 39-46, 2019 Jun.
Artigo em Inglês | MEDLINE | ID: mdl-30852259

RESUMO

Qing Dai (Naturalis Indigo) is a traditional Chinese medicine (TCM) used as a topical agent in moderate psoriasis, targeting interleukin-17 (IL-17). In this study, it was prepared from the aerial parts of Strobilanthes cusia. Three undescribed indole alkaloid derivatives, indigodoles A-C, along with seven known compounds were isolated from this preparation of Qing Dai and their structures were elucidated from spectroscopic data, including NMR, MS, UV, IR, optical rotation, and CD. As well, most compounds were tested against IL-17. Indigodole C and tryptanthrin could significantly inhibit IL-17 production of Th17 cells. In addition, indigodole A and indirubin showed notably anti-IL-17 gene expression in dose-dependent effects without cytotoxicities toward Th17 and Jurkat cells, respectively. Overall, our studies indicate that the aforementioned indole alkaloids could contribute to anti-IL 17 properties of Qing Dai.


Assuntos
Acanthaceae/química , Medicamentos de Ervas Chinesas/química , Alcaloides Indólicos/química , Alcaloides Indólicos/farmacologia , Interleucina-17/antagonistas & inibidores , Medicina Tradicional Chinesa , Componentes Aéreos da Planta/química , Animais , Interleucina-17/biossíntese , Camundongos , Modelos Moleculares , Conformação Molecular , Células Th17/efeitos dos fármacos , Células Th17/metabolismo
18.
J Ethnobiol Ethnomed ; 15(1): 13, 2019 Feb 19.
Artigo em Inglês | MEDLINE | ID: mdl-30782180

RESUMO

BACKGROUND: Indigo-dyed textiles have been central to the cultural identity of Landian Yao (literally "blue clothes Yao") people in Southwest China for centuries, driving a significant local market for naturally dyed indigo cloth. In the past two decades, local indigo production for traditional textiles has declined for several reasons: Firstly, the younger generation of Landian Yao has shifted to using western style jeans and T-shirts. Secondly, due to its labor-intensive nature. In contrast, at a global scale, including in China, there has been a revival of interest in natural indigo use. This is due to a growing awareness in the fashion industry about human and environmental health issues related to synthetic dye production. Ironically, this new awareness comes at a time when traditional knowledge of indigo dyeing is being lost in many places in China, with weaving and use of natural dyes now limited to some remote areas. In this study, we recorded indigo dyeing processes used by Landian Yao people and documented the plant species used for indigo dyeing. METHODS: Field surveys were conducted to the study area from September 2015 to November 2016, supplemented by follow-up visits in July 2018 and November 2018. We interviewed 46 key informants between 36 and 82 years old who still continued traditional indigo dyeing practices. Most were elderly people. Semi-structured interviews were used. During the field study, we kept a detailed account of the methods used by Landian Yao dyers. The data were then analyzed by using utilization frequency to determine the best traditional recipe of indigo dye extraction. All the specimens of documented species were collected and deposited at the herbarium of Kunming Institute of Botany. RESULTS: Our results showed that indigo dyeing was divided into two main steps: (1) indigo pigment extraction and (2) dyeing cloth. The general procedures of indigo dye extraction included building or buying a dye vat, fermentation, removal of the leaves of indigo producing plant species, addition of lime, oxygenation, followed by collection, and the storage of the indigo paste. The procedures of dyeing cloth included preparing the dye solutions, dyeing cloth, washing, and air drying. It is notable that Landian Yao dyers formerly only performed the dyeing process on the goat days in the lunar calendar from June to October. After comparing the range of local indigo extraction methods, our results showed that the following was best of these traditional recipes: a indigo-yielding plant material to tap water ratio of 30 kg: 200 l, lime 3 kg, a fermentation time of 2-3 d, aeration by agitation for up to 60 min, and a precipitation time of 2-3 h. Our results show that 17 plant species in 11 families were recorded in the indigo dyeing process. With the exception of the indigo sources, only Dioscorea cirrhosa Lour. and Artemisia argyi H.Lév. & Vaniot were previously recorded in dyeing processes. Other species given in this paper are recorded for the first time in terms of their use in the indigo dyeing process. In the study area, Landian Yao men were in charge of indigo dye extraction, and the women were responsible for dyeing cloth. CONCLUSIONS: The Landian Yao has completely mastered the traditional indigo dyeing craft and are one of the well-deserved identity blues. Indigo production from plants using traditional methods is a slow process compared to synthetic dyes and is not suitable for modern and rapid industrial production. Therefore, our study records the detailed information of traditional indigo dyeing to protect and inherit it. Strobilanthes cusia (Nees) Kuntze is the main indigo source in Landian Yao that is widely used in the world and can be commercially exploited as an indigo plant. For commercial and environment benefits, we suggest that producing natural indigo for the commercial market is a good choice.


Assuntos
Corantes , Etnobotânica , Têxteis , Acanthaceae/química , Adulto , Idoso , Idoso de 80 Anos ou mais , China , Feminino , Humanos , Indigofera/química , Conhecimento , Masculino , Pessoa de Meia-Idade , Plantas
19.
Asian Pac J Cancer Prev ; 20(2): 601-609, 2019 Feb 26.
Artigo em Inglês | MEDLINE | ID: mdl-30806066

RESUMO

Objective: This study was conducted to investigate the antiproliferative activity of extracts of Clinacanthus nutans leaves against human cervical cancer (HeLa) cells. Methods: C. nutans leaves were subjected to extraction using 80% methanol or water. The methanol extract was further extracted to obtain hexane, dichloromethane (DCM), and aqueous fractions. The antiproliferative activity of the extracts against HeLa cells was determined. The most cytotoxic extract was furthered analyzed by apoptosis and cell cycle assays, and the phytochemical constituents were screened by gas chromatography-mass spectrometry (GC-MS). Results: All of the extracts were antiproliferative against HeLa cells, and the DCM fraction had the lowest IC50 value of 70 µg/mL at 48 h. Microscopic studies showed that HeLa cells exposed to the DCM fraction exhibited marked morphological features of apoptosis. The flow cytometry study also confirmed that the DCM fraction induced apoptosis in HeLa cells, with cell cycle arrest at the S phase. GC-MS analysis revealed the presence of at least 28 compounds in the DCM fraction, most of which were fatty acids. Conclusion: The DCM fraction obtained using the extraction method described herein had a lower IC50 value than those reported in previous studies that characterized the anticancer activity of C. nutans against HeLa cells.


Assuntos
Acanthaceae/química , Antineoplásicos/farmacologia , Apoptose/efeitos dos fármacos , Proliferação de Células/efeitos dos fármacos , Extratos Vegetais/farmacologia , Folhas de Planta/química , Ciclo Celular/efeitos dos fármacos , Células HeLa , Humanos
20.
Asian Pac J Cancer Prev ; 20(2): 563-567, 2019 Feb 26.
Artigo em Inglês | MEDLINE | ID: mdl-30803221

RESUMO

Problem statement: Clinicanthus nutans has been used by Malaysian since long time ago. It is used to treat many diseases including cancer. Many studies carried out on its crude extract but no clear report on the specific secondary metabolites responsible for its nature in treating selected diseases. Objective: This study aims to confirm the practice carried out by many people on the usage of Clinicanthus nutans in treating cancer. Methods: C. nutans leaves were extracted by methanol. Thin layer chromatography was used to identify the suitable solvent for fractions separation. The fractions were then separated at larger volume using gravity column chromatography. Each fraction was tested on its anti-proliferative activity on Hep-G2 liver cancer cells by MTT assay. The phytochemical screening was carried out to identify the bioactive compound based on qualitative analysis. Results: The fraction 2 (F2) of C. nutans showed the lowest IC50 value of 1.73 µg/ml against Hep-G2 cancer cells, and it is identified as triterpenes. Conclusion: The fraction F2 identified as triterpenes isolated from C. nutans has potential as an anti-proliferative agent against liver cancer.


Assuntos
Acanthaceae/química , Proliferação de Células/efeitos dos fármacos , Neoplasias Hepáticas/tratamento farmacológico , Neoplasias Hepáticas/patologia , Fitoterapia , Extratos Vegetais/farmacologia , Triterpenos/farmacologia , Células Hep G2 , Humanos
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