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1.
Chem Pharm Bull (Tokyo) ; 70(2): 175-181, 2022.
Artigo em Inglês | MEDLINE | ID: mdl-35110439

RESUMO

Two novel triterpene glycosides (1 and 2), 17 known triterpene glycosides (3-19), two known flavonoid glycosides (20 and 21), and two known norsesquiterpene glucosides (22 and 23) were isolated from Hedera rhombea (Araliaceae) leaves. The structures of 1 and 2 were determined by spectroscopic analysis, including two-dimensional NMR spectroscopy, and chromatographic analysis of the hydrolyzed products. The cytotoxicity of the isolated triterpene glycosides (1-19) against HL-60 human promyelocytic leukemia cells was evaluated. Compounds 9, 10, and 11 were cytotoxic to HL-60 cells with IC50 values of 7.2, 21.9, and 32.8 µM, respectively. Other compounds isolated from the leaves were not cytotoxic at sample concentrations of 50 µM.


Assuntos
Antineoplásicos Fitogênicos/farmacologia , Araliaceae/química , Glicosídeos/farmacologia , Folhas de Planta/química , Triterpenos/farmacologia , Antineoplásicos Fitogênicos/química , Antineoplásicos Fitogênicos/isolamento & purificação , Proliferação de Células/efeitos dos fármacos , Sobrevivência Celular/efeitos dos fármacos , Relação Dose-Resposta a Droga , Ensaios de Seleção de Medicamentos Antitumorais , Glicosídeos/química , Glicosídeos/isolamento & purificação , Células HL-60 , Humanos , Estrutura Molecular , Relação Estrutura-Atividade , Triterpenos/química , Triterpenos/isolamento & purificação
2.
Nat Prod Res ; 36(8): 2085-2096, 2022 Apr.
Artigo em Inglês | MEDLINE | ID: mdl-33203260

RESUMO

Two new fatty acid esters of triterpenoids (1-2) together with eleven known compounds (3-13) were obtained after investigation of the CH2Cl2-MeOH (1:1) crude extract from the leaves of Schefflera barteri Harms. All these compounds (1-13) were isolated for the first time from this plant among which compounds 3, 4, 6 and 9-13 were also isolated from the genus Schefflera for the first time. The structures of the isolated compounds were elucidated by analyses of their spectroscopic data (1D and 2D NMR, and MS). The antibacterial and cytotoxic activities of crude extracts, fractions and compounds (1, 2, 5, 6, 8 and 9) were investigated against both Gram-negative and Gram-positive bacteria strains as well as on human cervix carcinoma and colon adenocarcinoma cancer cell lines, respectively. They showed weak to significant activity towards the strains and malignant cells used.


Assuntos
Araliaceae , Triterpenos , Araliaceae/química , Ésteres/análise , Ácidos Graxos/análise , Feminino , Humanos , Extratos Vegetais/química , Folhas de Planta/química , Triterpenos/química
3.
Molecules ; 26(12)2021 Jun 21.
Artigo em Inglês | MEDLINE | ID: mdl-34205529

RESUMO

Polyscias fruticosa (L.) leaves contain significant bioactive compounds with high antioxidant activity such as chlorophylls, total polyphenols, etc. but these have still been underutilized. In this study, the kinetics of chlorophyll and antioxidant activity extraction from P. fruticosa leaves by microwave-assisted extraction (MAE) were investigated. Microwave power was 300, 450, or 600 (W); the ratio of material/solvent varied from 1:40 to 1:80 (g/mL). In this study, the second-order kinetic model successfully predicted the change of chlorophyll and antioxidant activity during MAE. The increase of microwave power or/and the solvent amount increased saturated extraction efficiency and the extraction rate constant. However, the saturated concentration of chlorophyll and antioxidant activity increased with the increment of microwave power and the decrease in solvent amount.


Assuntos
Antioxidantes/farmacologia , Araliaceae/química , Clorofila/farmacologia , Extratos Vegetais/farmacologia , Folhas de Planta/química , Cromatografia Líquida de Alta Pressão/métodos , Etanol/química , Cinética , Micro-Ondas , Extratos Vegetais/química , Polifenóis/química , Polifenóis/farmacologia , Solventes/química
4.
Nutrients ; 13(5)2021 Apr 23.
Artigo em Inglês | MEDLINE | ID: mdl-33922621

RESUMO

Metabolic syndrome is a worldwide health problem, and obesity is closely related to type 2 diabetes, cardiovascular disease, hypertension, and cancer. According to WHO in 2018, the prevalence of obesity in 2016 tripled compared to 1975. D. morbifera reduces bad cholesterol and triglycerides levels in the blood and provides various antioxidant nutrients and germicidal sub-stances, as well as selenium, which helps to remove active oxygen. Moreover, D. morbifera is useful for treating cardiovascular diseases, hypertension, hyperlipidemia, and diabetes. Therefore, we study in vivo efficacy of D. morbifera to investigate the prevention effect of obesity and cholesterol. The weight and body fat were effectively reduced by D. morbifera water (DLW) extract administration to high-fat diet-fed C57BL/6 mice compared to those of control mice. The group treated with DLW 500 mg∙kg-1∙d-1 had significantly lower body weights compared to the control group. In addition, High-density lipoprotein (HDL) cholesterol increased in the group treated with DLW 500 mg∙kg-1∙d-1. The effect of DLW on the serum lipid profile could be helpful to prevent obesity. DLW suppresses lipid formation in adipocytes and decreases body fat. In conclusion, DLW can be applied to develop anti-obesity functional foods and other products to reduce body fat.


Assuntos
Fármacos Antiobesidade/farmacologia , Araliaceae/química , Hipolipemiantes/farmacologia , Extratos Vegetais/farmacologia , Folhas de Planta/química , Animais , Colesterol/sangue , Colesterol/urina , Regulação da Expressão Gênica/efeitos dos fármacos , Masculino , Malondialdeído/sangue , Malondialdeído/urina , Camundongos Endogâmicos C57BL , Óxido Nítrico/sangue , Óxido Nítrico/urina , Estresse Oxidativo/efeitos dos fármacos , Extratos Vegetais/toxicidade , Proteínas/genética , Proteínas/metabolismo , Água/química
5.
Carbohydr Res ; 502: 108279, 2021 Apr.
Artigo em Inglês | MEDLINE | ID: mdl-33691222

RESUMO

Fifteen triterpenoid saponins including five new compounds (Mannioside B: 3ß-[(ß-d-glucopyranosyl)oxy]urs-12-en-28-oic acid α-l-rhamnopyranosyl-(1 â†’ 4)-ß-d-glucopyranosyl-(1 â†’ 6)-ß-d-glucopyranosyl ester (1), mannioside C: 3ß-[(ß-d-glucopyranosyl)23-dioxy]urs-12-en-28-oic acid α-l-rhamnopyranosyl-(1 â†’ 4)-ß-d-glucopyranosyl-(1 â†’ 6)-ß-d-glucopyranosyl ester (2), mannioside D: 3ß,23-dihydroxyurs-12-en-28-oic acid ß-d-glucopyranosyl-(1 â†’ 6)- ß-d-glucopyranosyl ester (3), mannioside E: 3ß-hydroxy-23-oxolup-20(29)-en-28-oic acid α-l-rhamnopyranosyl-(1 â†’ 4)-ß-d-glucopyranosyl-(1 â†’ 6)-ß-d-glucopyranosyl ester (4) and mannioside F: (22S)-27ß-[(ß-d-glucopyranosyl)oxy]-22-hydroxyprotosta-12,24-dien-3ß-yl ß-d-glucopyranoside (5)) were isolated from the leaves of Schefflera mannii (Hook.f.) Harms. Their structures were established on the basis of 1D and 2D NMR data, mass spectrometry and chemical methods. The major isolated compounds were tested for their antiproliferative activity on human malignant epithelial (HeLa) cells but were not efficient at the concentration of 33 mM.


Assuntos
Araliaceae/química , Folhas de Planta/química , Saponinas/isolamento & purificação , Triterpenos/isolamento & purificação , Espectroscopia de Ressonância Magnética , Conformação Molecular , Saponinas/química , Triterpenos/química
6.
Nat Prod Res ; 35(19): 3285-3292, 2021 Oct.
Artigo em Inglês | MEDLINE | ID: mdl-31790291

RESUMO

Three new triterpene saponins including two lupane-types and an ursane-type were isolated from the leaves of Trevesia palmata. Their structures were determined as 2α,3ß,23-trihydroxylup-20(29)-en-28-oic acid 3-O-α-L-arabinopyranoside (1), 2α,3ß,23-trihydroxylup-20(29)-en-28-oic acid 3-O-[α-L-arabinopyranoside]-28-O-[ß-D-glucopyranosyl] ester (2), and 2α,3ß,23-trihydroxyurs-12-en-28-oic acid 3-O-[α-L-arabinopyranoside]-28-O-[ß-D-glucopyranosyl(1→2)-ß-D-glucopyranosyl] ester (3) by analysis of their HR-ESI-MS, 1D and 2D NMR spectra. The 2α,3ß,23-trioxygenated pentacyclic triterpenes were uncommonly found in the nature. At concentration of 100 µM, compounds 1-3 inhibited NO production in LPS activated BV2 cells with inhibitory rates of 17.4 ± 1.8%, 33.1 ± 1.2%, and 11.7 ± 2.2%, respectively. But, they did not significantly inhibit yeast α-glucosidase activity.


Assuntos
Araliaceae/química , Triterpenos Pentacíclicos/farmacologia , Saponinas , Triterpenos , Animais , Linhagem Celular , Camundongos , Triterpenos Pentacíclicos/isolamento & purificação , Folhas de Planta/química , Saponinas/isolamento & purificação , Saponinas/farmacologia , Triterpenos/isolamento & purificação , Triterpenos/farmacologia
7.
Nutrients ; 14(1)2021 Dec 27.
Artigo em Inglês | MEDLINE | ID: mdl-35010975

RESUMO

Hepatic fibrosis results from chronic liver damage and is characterized by excessive accumulation of extracellular matrix (ECM). In this study, we showed that dendropanoxide (DPX), isolated from Dendropanax morbifera, had anti-fibrotic effects on hepatic fibrosis by inhibiting hepatic stellate cell (HSC) activation. DPX suppressed mRNA and protein expression of α-SMA, fibronectin, and collagen in activated HSCs. Moreover, DPX (40 mg/kg) treatment significantly lowered levels of liver injury markers (aspartate aminotransferase and alanine transaminase), expression of fibrotic markers, and deposition of ECM in a carbon tetrachloride-induced mouse model. Anti-fibrotic effects of DPX were comparable to those of silymarin in a hepatic fibrosis mouse model. As a possible mechanism of anti-fibrotic effects, we showed that DPX inhibited autophagosome formation (LC3B-II) and degradation of p62, which have important roles in HSC activation. These findings suggest that DPX inhibits HSC activation by inhibiting autophagy and can be utilized in hepatic fibrosis therapy.


Assuntos
Células Estreladas do Fígado/efeitos dos fármacos , Cirrose Hepática/prevenção & controle , Triterpenos/farmacologia , Animais , Araliaceae/química , Intoxicação por Tetracloreto de Carbono , Linhagem Celular , Relação Dose-Resposta a Droga , Humanos , Cirrose Hepática/induzido quimicamente , Masculino , Camundongos , Camundongos Endogâmicos C57BL , Estrutura Molecular , Componentes Aéreos da Planta/química , Substâncias Protetoras/química , Substâncias Protetoras/farmacologia , Distribuição Aleatória , Silimarina/farmacologia , Triterpenos/administração & dosagem , Triterpenos/química
8.
Molecules ; 27(1)2021 Dec 29.
Artigo em Inglês | MEDLINE | ID: mdl-35011416

RESUMO

Hairy root cultures are considered as a valuable source of bioactive phytoconstituents with expanding applicability for their production. In the present study, hairy root cultures of Polyscias filicifolia (Araliaceae), a traditional Southeast Asian medicinal plant, were established. The transformation with Agrobacterium rhizogenes ATCC 15834 allowed to obtain 15 root lines. The K-1 line, demonstrating the highest growth capabilities, was subjected to further investigations. To enhance the biosynthetic potential of hairy roots, methyl jasmonate elicitation approach was applied (MeJA; at different doses and exposure time), with subsequent transfer of elicited roots to control medium. This strategy resulted in chlorogenic acid production up to 1.59 mg/g dry weight. HPLC-PDA-ESI-MS analysis demonstrated variation in extracts composition and allowed to identify different caffeic and ferulic acid derivatives. Next, cytotoxic, antigenotoxic, and anti-photogenotoxic properties of hairy roots extracts were determined. None of the tested extracts were cytotoxic. In addition, they demonstrated significant antigenotoxic activity with the highest protective potential; up to 52% and 49% of inhibition of induction ratio (IR) induced by the 2-aminoanthracene was revealed for extracts derived from hairy roots elicited for 3 days with 50 µM MeJA and roots elicited for 7 days with 100 µM MeJA and then transferred for 30 days to control medium, respectively. These same extracts exhibited the highest anti-photogenotoxic potential, up to 36% of inhibition of chloropromazine-induced genotoxicity.


Assuntos
Araliaceae/química , Extratos Vegetais/farmacologia , Raízes de Plantas/química , Substâncias Protetoras/farmacologia , Cromatografia Líquida de Alta Pressão , Dano ao DNA/efeitos dos fármacos , Dano ao DNA/efeitos da radiação , Relação Dose-Resposta a Droga , Espectrometria de Massas , Compostos Fitoquímicos/química , Compostos Fitoquímicos/farmacologia , Extratos Vegetais/química , Extratos Vegetais/isolamento & purificação , Raízes de Plantas/crescimento & desenvolvimento , Substâncias Protetoras/química , Substâncias Protetoras/isolamento & purificação , Protetores contra Radiação/química , Protetores contra Radiação/farmacologia , Espectrometria de Massas por Ionização por Electrospray
9.
J Ethnopharmacol ; 279: 113675, 2021 Oct 28.
Artigo em Inglês | MEDLINE | ID: mdl-33301919

RESUMO

ETHNOPHARMACOLOGICAL RELEVANCE: Schefflera is the largest genus in the family Araliaceae, which contains 602 known species indigenous to Asia, Africa, and the southwest Pacific region, several of which are used in traditional medicine. AIM OF THE REVIEW: The review discusses current knowledge of the traditional uses, phytochemistry, and biological activities of Schefflera species, to assess the medicinal potential of this genus. MATERIALS AND METHODS: The literature were explored using the keyword "Schefflera" in SciFinder®, Google Scholar®, and PubMed® databases. The taxonomy of all reported plants was authenticated using "The Plant List". Additional data on traditional uses was obtained from secondary references including books and online resources. RESULTS: Fourteen species were documented as traditional medicines in China, India, Vietnam, Thailand, and Indonesia, specifically to manage rheumatism, pain, and trauma. Other species are used in the treatment of liver disorders, skin conditions, respiratory infections, cancer, diarrhea, malaria, paralysis, and many other conditions. The main phytochemical constituents identified were triterpenoids and saponins, with sesquiterpenes, phenylpropanoids, and lignans. Pharmacological properties of extracts and pure isolated compounds included analgesic, anti-inflammatory, anticancer, hypoglycemic, antimicrobial, hepatoprotective, neuroprotective, antimalarial, and antiallergic effects. CONCLUSION: The reported biological activities of Schefflera species support their traditional uses, although the available data, even for medicinal species, was limited. Reports of chemical constituents or biological activities could be found for only about 20 species, but suggest that further investigation of efficacy and safety of the largely unexplored genus Schefflera is necessary.


Assuntos
Araliaceae/química , Medicina Tradicional/métodos , Extratos Vegetais/farmacologia , Animais , Etnofarmacologia , Humanos , Compostos Fitoquímicos/química , Compostos Fitoquímicos/isolamento & purificação , Compostos Fitoquímicos/farmacologia , Fitoterapia/métodos , Extratos Vegetais/química
10.
J Ethnopharmacol ; 267: 113631, 2021 Mar 01.
Artigo em Inglês | MEDLINE | ID: mdl-33246122

RESUMO

ETHNOPHARMACOLOGICAL RELEVANCE: The root of Dendropanax dentiger (Harms) Merr. is a pivotal folk Chinese medicine against rheumatoid arthritis (RA) with no scientific validation. AIM OF THE STUDY: This study was conducted to explore the anti-RA effect of the D. dentiger extract on complete Freund's adjuvant-induced arthritis (AIA) in rats and identified its major bio-constituents. MATERIALS AND METHODS: Dendropanax dentiger roots extracts (127.5, 255.0 and 510.0 mg/kg, once daily) were orally at day 7 post-administration adjuvant and lasting for 22 days. The therapeutic effects of D. dentiger roots extract on AIA rats were investigated by body weight growth, arthritis score, thymus and spleen indices, and histopathological analysis. Moreover, the levels of rheumatoid factor (RF), C-reactive protein (CRP), tumor necrosis factor alpha (TNF-α), interleukin-1ß (IL-1ß), IL-4, IL-6, IL-10, IL-17, cyclooxygenase-2 (COX-2), 5-lipoxygenase (5-LOX) and matrix metalloproteinase-2 (MMP-2) were also evaluated. Finally, the major constituents were isolated and identified from D. dentiger roots extract with COX-2 inhibitory and antioxidant activities. RESULTS: Dendropanax dentiger roots extract remarkably alleviated the histological lesions of knee joint, increased body weight growth, decreased arthritis score, and reduced thymus and spleen indices in model rats. In parallel, the levels of RF, CRP, TNF-α, IL-1ß, IL-6, IL-17, COX-2, 5-LOX and MMP-2 were observably downregulated, while the levels of IL-4 and IL-10 were prominently upregulated in D. dentiger roots extract-treated rats. Meanwhile, 14 compounds were isolated and identified from D. dentiger roots extract, and four phenol derivatives (1, 4, 6 and 7) exhibited remarkable COX-2 inhibitory and antioxidant activities. CONCLUSIONS: Dendropanax dentiger roots extract possessed persuasive anti-RA effect may be partly responsible for phenol derivatives via modulation of inflammatory biomarkers, and supports the traditional folk use of D. dentiger in China.


Assuntos
Antioxidantes/farmacologia , Antirreumáticos/farmacologia , Araliaceae , Artrite Experimental/prevenção & controle , Inibidores de Ciclo-Oxigenase 2/farmacologia , Articulações/efeitos dos fármacos , Estresse Oxidativo/efeitos dos fármacos , Raízes de Plantas , Animais , Antioxidantes/isolamento & purificação , Antirreumáticos/isolamento & purificação , Araliaceae/química , Artrite Experimental/induzido quimicamente , Artrite Experimental/metabolismo , Artrite Experimental/patologia , Inibidores de Ciclo-Oxigenase 2/isolamento & purificação , Citocinas/metabolismo , Adjuvante de Freund , Mediadores da Inflamação/metabolismo , Articulações/metabolismo , Articulações/patologia , Raízes de Plantas/química , Ratos Sprague-Dawley
11.
Biomed Res Int ; 2020: 5084057, 2020.
Artigo em Inglês | MEDLINE | ID: mdl-33294445

RESUMO

Dendropanax dentiger root is a traditional medicinal plant in China and used to treat inflammatory diseases for centuries, but its phytochemical profiling and biological functions are still unknown. Thus, a rapid, efficient, and precise method based on ultra high-performance liquid chromatography coupled with quadrupole time-of-flight tandem mass spectrometry (UHPLC-Q-TOF-MS/MS) was applied to rapidly analyse the phytochemical profiling of D. dentiger with anti-inflammatory and antioxidant activities in vitro. As a result, a total of 78 chemical compositions, including 15 phenylpropanoids, 15 alkaloids, 14 flavonoids, 14 fatty acids, 7 phenols, 4 steroids, 4 cyclic peptides, 3 terpenoids, and 2 others, were identified or tentatively characterized in the roots of D. dentiger. Moreover, alkaloid and cyclic peptide were reported from D. dentiger for the first time. In addition, the ethanol crude extract of D. dentiger roots exhibited remarkable anti-inflammatory activity against cyclooxygenase- (COX-) 2 inhibitory and antioxidant activities in vitro. This study is the first to explore the phytochemical analysis and COX-2 inhibitory activity of D. dentiger. This study can provide important phytochemical profiles and biological functions for the application of D. dentiger roots as a new source of natural COX-2 inhibitors and antioxidants in pharmaceutical industry.


Assuntos
Anti-Inflamatórios/farmacologia , Antioxidantes/farmacologia , Araliaceae/química , Compostos Fitoquímicos/análise , Compostos Fitoquímicos/farmacologia , Raízes de Plantas/química , Alcaloides/química , Benzotiazóis/química , Compostos de Bifenilo/química , Inibidores de Ciclo-Oxigenase/farmacologia , Concentração Inibidora 50 , Compostos Fitoquímicos/química , Picratos/química , Extratos Vegetais/química , Padrões de Referência , Ácidos Sulfônicos/química
12.
PLoS One ; 15(10): e0240868, 2020.
Artigo em Inglês | MEDLINE | ID: mdl-33112916

RESUMO

Honey can be categorized as monofloral and polyfloral honey. There is a strong interest in science and commerce, to further differentiate honey. In the present study, Schefflera abyssinica and polyfloral honey from Sheka Forest, Ethiopia was investigated. Botanical origin was determined based on Melissopalynology. Refractive index, moisture, sugars, ash, pH, free acidity, hydroxymethylfurfural, optical density, diastase activity, protein, and color were determined based on the standard method of the international honey commission (IHC) and AOAC. Antioxidant activity and Antioxidant content were determined using UV- visible spectroscopy. The level of pollen dominancy for monofloral honey (Schefflera abyssinica) ranged from 76.2 to 85.8%. The polyfloral honey stuffed with a variety of pollen grain ranged from 2.2% (Coffea arabica) to 23.2% (Schefflera abyssinica). Schefflera abyssinica honey contained more total phenolic compounds (75.08 ± 2.40 mg GAE/100g), and total flavonoids (42.03 ± 1.49 mg QE/100 g), as well as had stronger DPPH (44.43 ± 0.97%) and hydrogen peroxide (78.00 ± 4.82%) scavenging activity. The principal component analysis revealed that Schefflera abyssinica honey associated with the antioxidant properties of total phenolic, total flavonoids, DPPH, and H2O2., which revealed that floral honey sources can essentially differentiated by antioxidant patterns. The higher electrical conductivity (0.42 ± 0.02 mS/cm), ash (0.41 ± 0.05 g/100g), pH (4.01 ± 0.08), optical density (0.26 ± 0.03) and diastase activity (5.21 ± 0.17 Schade units) were recorded in polyfloral honey. Schefflera abyssinica and polyfloral honey satisfy the requirement of national and international standards. The pollen analysis in combination with antioxidant properties distinguishes Schefflera abyssinica from polyfloral honeys.


Assuntos
Mel/análise , Antioxidantes/análise , Araliaceae/química , Coffea/química , Etiópia , Flavonoides , Flores/química , Peróxido de Hidrogênio/análise , Fenóis/análise , Pólen/química
13.
Bioorg Chem ; 104: 104211, 2020 11.
Artigo em Inglês | MEDLINE | ID: mdl-32920357

RESUMO

The root of Dendropanax dentiger (Harms) Merr. is a traditional Chinese medicine that has been used to treat inflammation-related diseases with little scientific validation. In this study, a bioassay-guided phytochemical investigation of D. dentiger led to the isolation of 19 phenylpropanoid derivatives including one new compound (1) and 18 known ones (2-19). Their structures were elucidated by NMR and HRMS as well as comparison with literature data. The ability of cyclooxygenase-2 (COX-2) inhibition and antioxidant of all isolated compounds were measured in vitro. Chlorogenic acid derivatives (14-19) exhibited outstanding COX-2 inhibitory (IC50 = 5.1-93.4 µM) and antioxidant (IC50 = 13.2-31.9 µM) activities. Moreover, the tight structure-activities relationships were proposed. This is the first report on the COX-2 inhibitory activity of phenylpropanoids and D. dentiger.


Assuntos
Anti-Inflamatórios não Esteroides/farmacologia , Antioxidantes/farmacologia , Araliaceae/química , Inibidores de Ciclo-Oxigenase 2/farmacologia , Fenilpropionatos/farmacologia , Extratos Vegetais/farmacologia , Anti-Inflamatórios não Esteroides/química , Anti-Inflamatórios não Esteroides/isolamento & purificação , Antioxidantes/química , Antioxidantes/isolamento & purificação , Compostos de Bifenilo/antagonistas & inibidores , Ciclo-Oxigenase 2/metabolismo , Inibidores de Ciclo-Oxigenase 2/química , Inibidores de Ciclo-Oxigenase 2/isolamento & purificação , Relação Dose-Resposta a Droga , Humanos , Estrutura Molecular , Fenilpropionatos/química , Fenilpropionatos/isolamento & purificação , Picratos/antagonistas & inibidores , Extratos Vegetais/química , Extratos Vegetais/isolamento & purificação , Raízes de Plantas/química , Relação Estrutura-Atividade
14.
Food Chem Toxicol ; 145: 111605, 2020 Nov.
Artigo em Inglês | MEDLINE | ID: mdl-32750447

RESUMO

The aim of this study was to investigate the protective effects of dendropanoxide (DPx) isolated from Dendropanax morbifera against cis-diamminedichloroplatinum (II) (CDDP)-induced nephrotoxicity in NRK-52E cells and in Sprague-Dawley rats. DPx was administered to Sprague-Dawley rats by oral gavage (5 and 10 mg/kg) for 7 consecutive days, 24 h after intraperitoneal injection with CDDP (6 mg/kg). All rats were euthanized 24 h after the last DPx administration, and histopathological damage, acute kidney injury (AKI) biomarkers, inflammatory cytokines, and oxidative damages were evaluated. DPx (5 and 10 µg/mL) was found to protect against CDDP-induced cytotoxicity and apoptotic cell death in NRK-52E cells. CDDP-induced serum blood urea nitrogen (BUN), creatinine (sCr), and pro-inflammatory cytokines levels were significantly ameliorated by DPx in a dose-dependent manner. Furthermore, excretion of kidney injury molecules (KIM-1), selenium binding protein-1 (SBP-1), and neutrophil gelatinase-associated lipocalin (NGAL) in the urine was significantly reduced in response to DPx administration in CDDP-treated rats. Activities of antioxidant enzymes and lipid peroxidation levels were markedly altered in the kidney of CDDP-treated rats in response to DPx administration. Serum pro-inflammatory cytokine levels were dramatically suppressed by DPx in CDDP-treated rats. DPx also restored renal-cell apoptosis via regulation of AMPK/mTOR signaling in CDDP-treated rats. Our results clearly suggest that DPx ameliorates CDDP-induced nephrotoxicity in vitro and in vivo by inhibiting oxidative stress, inflammation, and apoptosis. Overall, our data demonstrates that DPx may serve as a therapeutic agent in patients with solid tumors to prevent CDDP-induced AKI.


Assuntos
Injúria Renal Aguda/prevenção & controle , Anti-Inflamatórios/uso terapêutico , Antioxidantes/uso terapêutico , Transdução de Sinais/efeitos dos fármacos , Triterpenos/uso terapêutico , Proteínas Quinases Ativadas por AMP/metabolismo , Injúria Renal Aguda/induzido quimicamente , Injúria Renal Aguda/patologia , Animais , Apoptose/efeitos dos fármacos , Araliaceae/química , Linhagem Celular , Cisplatino , Rim/patologia , Masculino , Estresse Oxidativo/efeitos dos fármacos , Componentes Aéreos da Planta/química , Proteínas Proto-Oncogênicas c-akt/metabolismo , Ratos Sprague-Dawley , Serina-Treonina Quinases TOR/metabolismo
15.
J Nat Prod ; 83(5): 1453-1460, 2020 05 22.
Artigo em Inglês | MEDLINE | ID: mdl-32319765

RESUMO

An enantiomeric pair of rare cyperane-type sesquiterpenoids, (+)- and (-)-gracilistones C (1a, 1b), together with a novel norsesquiterpenoid, gracilistone D (2), bearing a bicyclic lactone system were isolated from the root bark of Acanthopanax gracilistylus using LC-MS-IT-TOF analyses. The structures and absolute configurations of 1a, 1b, and 2 were elucidated by 1D and 2D NMR spectroscopy, X-ray diffraction, and ECD spectroscopic methods. Intermediate 1b suggests a possible biosynthesis process involving compound 2. The bioassay results showed that compounds 1a, 1b, and 2 exhibited significant inhibitory effects against lipopolysaccharide-induced nitric oxide production in RAW 264.7 cells, with IC50 values of 7.7 ± 0.6, 6.8 ± 1.5, and 2.6 ± 0.4 µM, respectively. Additional docking analyses provided some perspective of this activity in human inducible nitric oxide synthase.


Assuntos
Araliaceae/química , Óxido Nítrico/antagonistas & inibidores , Casca de Planta/química , Sesquiterpenos/química , Sesquiterpenos/farmacologia , Animais , Inibidores Enzimáticos/química , Inibidores Enzimáticos/farmacologia , Humanos , Camundongos , Simulação de Acoplamento Molecular , Estrutura Molecular , Óxido Nítrico/biossíntese , Óxido Nítrico Sintase Tipo II/antagonistas & inibidores , Células RAW 264.7 , Difração de Raios X
16.
Acta Pharmacol Sin ; 41(4): 523-534, 2020 Apr.
Artigo em Inglês | MEDLINE | ID: mdl-32203085

RESUMO

Ginsenoside Rg1 is one of the most active ingredients in ginseng, which has been reported to protect dopaminergic neurons and improve behavioral defects in MPTP model, 6-OHDA model and rotenone model. However, it is unclear whether Rg1 exerted neuroprotection in LPS-induced sub-acute PD model. In this study, we investigated the neuroprotective effect of Rg1 in the sub-acute PD mouse model and explored the related mechanisms. Rg1 (10, 20, 40 mg·kg-1·d-1) was orally administered to mice for 18 days. A sub-acute PD model was established in the mice through LPS microinjection into the substantia nigra (SN) from D8 to D13. We found that Rg1 administration dose-dependently inhibited LPS-induced damage of dopaminergic neurons and activation of glial cells in the substantia nigra pars compacta (SNpc). The neuroprotective effects of Rg1 were associated with the reduction of pro-inflammatory cytokines and the improvement of anti-inflammatory cytokines and neurotrophin in the midbrain. Rg1 shifted the polarization of microglia towards the M2 phenotype from M1, evidenced by decreased M1 markers (inducible NO synthase, CD16, etc.) and increased M2 markers (arginase 1 (Arg1), CD206, etc) in the midbrain. Furthermore, Rg1 administration markedly inhibited nuclear translocation of NF-κB in midbrain microglia. In conclusion, Rg1 protects PD mice induced by continuous LPS injection by inhibiting the nuclear entry of NF-κB and regulating the polarization balance of microglia, shedding new light on a disease-modifying therapy of PD.


Assuntos
Ginsenosídeos/farmacologia , Microglia/efeitos dos fármacos , NF-kappa B/antagonistas & inibidores , Fármacos Neuroprotetores/farmacologia , Transtornos Parkinsonianos/tratamento farmacológico , Administração Oral , Animais , Araliaceae/química , Citocinas/antagonistas & inibidores , Citocinas/metabolismo , Modelos Animais de Doenças , Relação Dose-Resposta a Droga , Ginsenosídeos/administração & dosagem , Ginsenosídeos/isolamento & purificação , Lipopolissacarídeos/administração & dosagem , Lipopolissacarídeos/antagonistas & inibidores , Lipopolissacarídeos/farmacologia , Masculino , Camundongos , Camundongos Endogâmicos C57BL , Microglia/metabolismo , NF-kappa B/metabolismo , Fármacos Neuroprotetores/administração & dosagem , Fármacos Neuroprotetores/isolamento & purificação , Transtornos Parkinsonianos/induzido quimicamente , Fenótipo , Transdução de Sinais/efeitos dos fármacos
17.
Molecules ; 25(5)2020 Feb 28.
Artigo em Inglês | MEDLINE | ID: mdl-32121158

RESUMO

Traditional medicinal plants are an important source of active compounds with potential antimutagenic activity. Polyscias filicifolia Bailey (Araliaceae) is a South Asian traditional herb used as an adaptogenic and cardiac drug. Extracts of P. filicifolia contain a wide range of biologically active compounds like phenolic acids and triterpenoid saponins. In the present study. antigenotoxic potential of three naturally occurring phenolic acids and extracts of P. filicifolia growing in vitro with the addition of elicitors was evaluated against direct (4-nitroquinoline-N-oxide (4NQO) and mitomycin C (MMC)) and indirect mutagens (2-aminoanthracene (2AA)). The evaluation was made using a bacterial umu-test. Moreover, the ability to prevent photogenotoxicity induced by chlorpromazine (CPZ) under UVA irradiation was measured. The phytochemical profiling of examined extracts revealed the presence of numerous compounds with the prevelance of chlorogenic, caffeic, and ferulic acid derivatives; however, saponin fractions were also determined. The antioxidant potential of extracts strictly correlated with their composition. The tested extracts exhibited high antigenotoxic activity if the assay was performed with 2AA and metabolic activation. Moreover, the extracts slightly decreased the MMC-induced genotoxicity. However, an increase of the genotoxic effect was observed in the assay performed with 4NQO. In addition, photo-antigenotoxic activity was observed. In our study, phenolic acids exhibited lower activity than the extracts.


Assuntos
Antimutagênicos/farmacologia , Antioxidantes/farmacologia , Araliaceae/química , Dano ao DNA , Extratos Vegetais/farmacologia , Brotos de Planta/química , Animais , Antimutagênicos/química , Antioxidantes/química , Clorpromazina/efeitos adversos , Clorpromazina/farmacologia , Masculino , Mitomicina/efeitos adversos , Mitomicina/farmacologia , Extratos Vegetais/química , Ratos , Ratos Sprague-Dawley
18.
Nat Prod Res ; 34(9): 1250-1255, 2020 May.
Artigo em Inglês | MEDLINE | ID: mdl-30663359

RESUMO

For the first time, the phytochemical constituents of the leaves of Polyscias fruticosa (L.) Harms. cultivating in An Giang Province, Viet Nam were investigated and led to purify two new oleanane-type triterpenoid saponins, named polyscioside J (1) and polyscioside K (2) together with two known saponins, ladyginoside A (3) and chikusetsusaponin IVa (4) using variously chromatographic methods. Saponin (4) was reported for the first time from this species. Their structures were verified by IR, UV, HR-ESI-MS, NMR 1D and 2D experiments and compared with previous literatures.


Assuntos
Araliaceae/química , Saponinas/isolamento & purificação , Glicosídeos/química , Glicosídeos/isolamento & purificação , Estrutura Molecular , Ácido Oleanólico/análogos & derivados , Ácido Oleanólico/isolamento & purificação , Extratos Vegetais/química , Folhas de Planta/química , Saponinas/química , Análise Espectral , Triterpenos/química , Triterpenos/isolamento & purificação , Vietnã
19.
Nat Prod Res ; 34(6): 859-862, 2020 Mar.
Artigo em Inglês | MEDLINE | ID: mdl-30289000

RESUMO

The stem bark of Cussonia bancoensis is used traditionally for the treatment of different types of infection and pain. A bioassay guided fractionation of the methanol stem bark extract led to the isolation of five pentacyclic triterpenes and glycosides identified based on spectroscopic data as 23-hydroxyursolic acid (CB1), hederagenin (CB2), 3-O-α-L-arabinopyranosyl-echinocystic acid (CB3), 3-O-α-L-arabinopyranosyl- oleanolic acid (CB4) and 3-O-α-L-arabinopyranosyl-ursolic acid (CB5). CB2 - CB5 are being reported for the first time from this species. The compounds were evaluated for antimicrobial activity against ten microorganisms using the HT-SPOTi method. CB3 demonstrated remarkable antimicrobial activity against S. aureus, S. pyogens, E. faecalis, S. typhi and C. albicans at MICs between 3.12 and 12.5 µg/mL. Among the studied compounds, it was observed that hydroxylation of position C-16 of the oleanane skeleton may enhance antimicrobial activity. This study gives insight into the anti-infective constituents of the stem bark of C. bancoensis and justifies its use in ethnomedicine.[Formula: see text].


Assuntos
Anti-Infecciosos/isolamento & purificação , Araliaceae/química , Glicosídeos/farmacologia , Triterpenos Pentacíclicos/isolamento & purificação , Casca de Planta/química , Anti-Infecciosos/química , Anti-Infecciosos/farmacologia , Bactérias/efeitos dos fármacos , Fungos/efeitos dos fármacos , Glicosídeos/química , Glicosídeos/isolamento & purificação , Ácido Oleanólico/análogos & derivados , Triterpenos Pentacíclicos/química , Triterpenos Pentacíclicos/farmacologia , Saponinas , Triterpenos , Ácido Ursólico
20.
Nat Prod Res ; 34(10): 1373-1379, 2020 May.
Artigo em Inglês | MEDLINE | ID: mdl-30445878

RESUMO

The fresh leaves of Metapanax delavayi (Araliaceae) have been used as a common wild vegetable for salad and soup, and also herbal tea by the local people living in its growing areas of Yunnan province, China. Detailed chemical investigation led to the identification of a new triterpenoid saponin, 3-O-α-L-arabinopyranosyl-28-O-ß-D-glucopyranosyl-(1→6)-O-ß-D-glucopyranosyl-3ß-hydroxyolean-12-ene-28,29-dioic acid (1) from the fresh leaves, together with 11 known compounds, including six triterpenoid saponins (2-7), two caffeoylquinic acid derivatives (8-9), and three flavonoid glycosides (10-12). Their structures were determined on the basis of spectroscopic analysis and acidic hydrolysis. Compounds 3-5 and 8-12 were isolated from M. delavayi for the first time. Moreover, the known saponins 3-O-ß-D-xylopyranosyl-3ß-hydroxyolean-12-ene-28,29-dioic acid (3) and yiyeliangwanoside IV (5) exhibited protective effects on HepG2 cells damaged by the alcohol intakes, at a concentration of 1.0 µg/mL. The results indicated M. delavayi is an ideal dietary vegetable and herbal tea with potential hepatoprotective activity.[Formula: see text].


Assuntos
Araliaceae/química , Folhas de Planta/química , Substâncias Protetoras/isolamento & purificação , Saponinas/isolamento & purificação , Triterpenos/isolamento & purificação , China , Glicosídeos/análise , Células Hep G2/efeitos dos fármacos , Humanos , Estrutura Molecular , Extratos Vegetais/química , Substâncias Protetoras/química , Substâncias Protetoras/farmacologia , Saponinas/química , Saponinas/farmacologia , Triterpenos/análise , Triterpenos/química , Triterpenos/farmacologia
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