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1.
Food Chem Toxicol ; 150: 112075, 2021 Apr.
Artigo em Inglês | MEDLINE | ID: mdl-33617964

RESUMO

Medicinal or herbal plants are widely used for their many favourable properties and are generally safe without any side effects. Saponins are sugar conjugated natural compounds which possess a multitude of biological activities such as medicinal properties, antimicrobial activity, antiviral activity, etc. Saponin production is a part of the normal growth and development process in a lot of plants and plant extracts such as liquorice and ginseng which are exploited as potential drug sources. Herbal compounds have shown a great potential against a wide variety of infectious agents, including viruses such as the SARS-CoV; these are all-natural products and do not show any adverse side effects. This article reviews the various aspects of saponin biosynthesis and extraction, the need for their integration into more mainstream medicinal therapies and how they could be potentially useful in treating viral diseases such as COVID-19, HIV, HSV, rotavirus etc. The literature presents a close review on the saponin efficacy in targeting mentioned viral diseases that occupy a high mortality rate worldwide. This manuscript indicates the role of saponins as a source of dynamic plant based anti-viral remedies and their various methods for extraction from different sources.


Assuntos
Antivirais/isolamento & purificação , Saponinas/isolamento & purificação , Anti-Infecciosos/farmacologia , Antifúngicos/farmacologia , Antivirais/farmacologia , HIV/efeitos dos fármacos , Estrutura Molecular , Orthomyxoviridae/efeitos dos fármacos , Extratos Vegetais/isolamento & purificação , Extratos Vegetais/farmacologia , Saponinas/biossíntese , Saponinas/química , Saponinas/farmacologia
2.
J Ethnopharmacol ; 266: 113398, 2021 Feb 10.
Artigo em Inglês | MEDLINE | ID: mdl-32971162

RESUMO

ETHNOPHARMACOLOGICAL RELEVANCE: Chiang-Da, Gymnema inodorum (Lour.) Decne. (GI), is an ethnomedicinal plant that has been used for diabetic treatment since ancient times. One of the anti-diabetic mechanisms is possibly related to the actions of triterpene glycoside, (3ß, 16ß)-16,28-dihydroxyolean-12-en-3-yl-O-ß-D-glucopyranosyl-ß-D-glucopyranosiduronic acid (GIA1) in decreasing carbohydrate digestive enzymes and intestinal glucose absorption in the gut system. AIMS OF THE STUDY: To observe the amount of GIA1 in GI leaf extracts obtained from different ethanol concentrations and to investigate the anti-hyperglycemic mechanisms of the extracts and GIA1. MATERIALS AND METHODS: The crude extracts were prepared using 50%v/v to 95%v/v ethanol solutions and used for GIA1 isolation. The anti-hyperglycemic models included in our study examined the inhibitory activities of α-amylase/α-glucosidase and intestinal glucose absorption related to sodium glucose cotransporter type 1 (SGLT1) using Caco-2 cells. RESULTS: GIA1 was found about 8%w/w to 18%w/w in the GI extract depending on ethanol concentrations. The GI extracts and GIA1 showed less inhibitory activities on α-amylase. The extracts from 75%v/v and 95%v/v ethanol and GIA1 significantly delayed the glycemic absorption by lowering α-glucosidase activity and glucose transportation of SGLT1. However, the 50%v/v ethanolic extract markedly decreased the α-glucosidase activity than the SGLT1 function. CONCLUSION: Differences in the GIA1 contents and anti-glycemic properties of the GI leaf extract was dependent on ethanol concentrations. Furthermore, the inhibitory effects of the 75%v/v and 95%v/v ethanolic extracts on α-glucosidase and SGLT1 were relevant to GIA1 content.


Assuntos
Gymnema/química , Extratos Vegetais/farmacologia , Saponinas/farmacologia , Triterpenos/farmacologia , Células CACO-2 , Metabolismo dos Carboidratos/efeitos dos fármacos , Digestão/efeitos dos fármacos , Glucose/metabolismo , Humanos , Hipoglicemiantes/isolamento & purificação , Hipoglicemiantes/farmacologia , Absorção Intestinal/efeitos dos fármacos , Folhas de Planta , Saponinas/isolamento & purificação , Triterpenos/isolamento & purificação , alfa-Amilases/antagonistas & inibidores , alfa-Glucosidases/efeitos dos fármacos , alfa-Glucosidases/metabolismo
3.
J Ethnopharmacol ; 266: 113446, 2021 Feb 10.
Artigo em Inglês | MEDLINE | ID: mdl-33031902

RESUMO

ETHNOPHARMACOLOGICAL RELEVANCE: Hepatocellular carcinoma (HCC) is an aggressive malignancy with increasing mortality in China. Screening and identifying effective anticancer compounds from active traditional Chinese herbs for HCC are in demand. Akebia trifoliata (Thunb) Koidz, with pharmacological anti-HCC activities in clinical, has been shown in previous research. In the present research, we elucidated a potential anticancer effect of Akebia saponin E (ASE), which is isolated from the immature seeds of Akebia trifoliata (Thunb.) Koidz, and revealed that ASE could induce severe expanded vacuoles in HCC cells. But the potential mechanism of vacuole-formation and the anti-HCC effects by ASE remain uncover. AIM OF THIS STUDY: To elucidate the potential mechanism of vacuole-formation and the proliferation inhibition effects by ASE in HCC cell lines. MATERIALS AND METHODS: MTT assay, colony formation assay and flow cytometry were performed to detect cell viability. Immunofluorescence analysis was used to examine the biomarkers of endomembrane. Cells were infected with tandem mRFP-GFP-LC3 lentivirus to assess autophagy flux. RNA-seq was conducted to analyze the genome-wide transcriptional between treatment cell groups. In vitro PIKfyve kinase assay is detected by the ADP-GloTM Kinase Assay Kit. RESULTS: ASE could inhibit the proliferation of HCC with severe expanded vacuoles in vitro, and could significantly reduce the size and weight of xenograft tumor in vivo. Further, the vacuoles induced by ASE were aberrant enlarged lysosomes instead of autophagosome or autolysosomes. With cytoplasmic vacuolation, ASE induced a mTOR-independent TFEB activation for lysosomal biogenesis and a decrement of cholesterol levels in HCC cells. Furthermore, ASE could reduce the activity of PIKfyve (phosphoinositide kinase containing a FYVE-type finger), causing aberrant lysosomal biogenesis and cholesterol dyshomeostasis which triggered the expanded vacuole formation. CONCLUSION: ASE can prospectively inhibit the kinase activity of PIKfyve to induce lysosome-associated cytoplasmic vacuolation, and may be utilized as an alternative candidate to treat human HCC.


Assuntos
Carcinoma Hepatocelular/tratamento farmacológico , Neoplasias Hepáticas/tratamento farmacológico , Ranunculales/química , Saponinas/farmacologia , Animais , Autofagia/efeitos dos fármacos , Linhagem Celular Tumoral , Proliferação de Células/efeitos dos fármacos , Sobrevivência Celular/efeitos dos fármacos , Humanos , Lisossomos/metabolismo , Masculino , Camundongos , Camundongos Endogâmicos BALB C , Camundongos Nus , Fosfatidilinositol 3-Quinases/efeitos dos fármacos , Inibidores de Fosfoinositídeo-3 Quinase/isolamento & purificação , Inibidores de Fosfoinositídeo-3 Quinase/farmacologia , Saponinas/isolamento & purificação , Vacúolos/efeitos dos fármacos , Vacúolos/metabolismo , Ensaios Antitumorais Modelo de Xenoenxerto
4.
J Ethnopharmacol ; 269: 113691, 2021 Apr 06.
Artigo em Inglês | MEDLINE | ID: mdl-33321190

RESUMO

ETHNOPHARMACOLOGICAL RELEVANCE: Ilex cornuta Lindl. et Paxt. (Aquifoliaceae family) belongs to the Ilex genus. The leaves of this plant are used for the popular herbal tea "Ku-Ding-Cha" in China due to their health benefits for sore throat, obesity and hypertension. Our previous studies have shown that the extract of Ilex cornuta root exerts cardioprotective effects in rat models of myocardial ischaemic injury, and several new kinds of triterpenoid saponins from Ilex cornuta (TSIC) have protective effects against hydrogen peroxide (H2O2)-induced cardiomyocyte injury. AIM OF THE STUDY: The aim of this study was to clarify the underlying mechanisms by which TSIC protect against H2O2-induced cardiomyocyte injury. MATERIALS AND METHODS: An H2O2-treated H9c2 cardiomyocyte line was used as an in vitro model of oxidation-damaged cardiomyocytes to evaluate the effects of TSIC. Apoptosis was detected with CCK-8 and annexin V assays and via analysis of the levels of apoptosis-associated proteins or genes. The underlying mechanisms related to Akt signalling, Ezh2 expression and activity, and ROS were clarified by Western blotting, quantitative PCR, flow cytometry and rescue experiments. RESULTS: TSIC protected H9c2 cells from H2O2-induced apoptosis. This effect of TSIC was attributable to inhibition of Ezh2 activity, as exhibited by attenuation of H2O2-induced Akt signalling-dependent phosphorylation of Ezh2 at serine 21 (pEzh2S21) upon TSIC pretreatment. In addition, feedback pathway between Akt-dependent Ezh2 phosphorylation and ROS was involved in TSIC-mediated protection of H9c2 cells from apoptosis. CONCLUSIONS: Our findings indicate a pivotal role of the pEzh2S21 network in TSIC-mediated protection against cardiomyocyte apoptosis, potentially providing evidence of the mechanism of TSIC in the treatment and prevention of cardiovascular diseases.


Assuntos
Proteína Potenciadora do Homólogo 2 de Zeste/metabolismo , Peróxido de Hidrogênio/toxicidade , Ilex , Miócitos Cardíacos/metabolismo , Saponinas/farmacologia , Triterpenos/farmacologia , Animais , Apoptose/efeitos dos fármacos , Apoptose/fisiologia , Cardiotônicos/isolamento & purificação , Cardiotônicos/farmacologia , Linhagem Celular , Miócitos Cardíacos/efeitos dos fármacos , Fosforilação/efeitos dos fármacos , Fosforilação/fisiologia , Ratos , Saponinas/isolamento & purificação , Triterpenos/isolamento & purificação
5.
J Ethnopharmacol ; 265: 113389, 2021 Jan 30.
Artigo em Inglês | MEDLINE | ID: mdl-32920134

RESUMO

ETHNOPHARMACOLOGICAL RELEVANCE: In traditional Chinese medicine (TCM) theory, "Qi" is classified as energetic essence supporting the life activities in human. "Blood" is categorized as nourishing essence and circulating in the body. "Blood" and "Qi" have an intimate relationship. Astragali Radix (AR; root of Astragalus membranaceus (Fisch.) Bge. Var. mongholicus (Bge.) Hsiao) has a broad spectrum of application for "Qi-Blood" enrichment. Astragaloside IV, a major saponin in AR, has therapeutic functions in erythropoietic, cardiovascular and immune systems. However, the efficacy of astragaloside IV in erythrophagocytosis has not been elucidated. AIM OF THE STUDY: The possible functions of astragaloside IV in heme iron recycling during erythrophagocytosis in cultured macrophage were elucidated. METHODS: The translational and transcriptional expressions of heme recycling enzymes were determined after incubating of astragaloside IV for 24 h in cultured macrophage. RESULTS: In astragaloside IV-treated macrophage, the expressions, both RNA and protein levels, of regulators of heme recycling, e.g. heme oxygenase-1 (HO-1), ferroportin (FPN), biliverdin reductase A and B (BVRA, BVRB), were markedly induced in dose-dependent manners. In parallel, the transcriptional activity of antioxidant response element, cloned within an expression vector as pARE-Luc and transfected in cultured macrophages, was markedly induced after a challenge with astragaloside IV in a dose-dependent manner. Moreover, the translocation of Nrf2, a transcriptional factor in regulating expression of heme recycling protein, was induced by astragaloside IV, leading to an enrichment at nucleus fraction. CONCLUSION: Astragaloside IV shed lights in enhancing the expression of heme recycle proteins via Nrf2/ARE signaling pathway.


Assuntos
Medicamentos de Ervas Chinesas/farmacologia , Macrófagos/efeitos dos fármacos , Saponinas/farmacologia , Triterpenos/farmacologia , Animais , Elementos de Resposta Antioxidante/efeitos dos fármacos , Células Cultivadas , Relação Dose-Resposta a Droga , Medicamentos de Ervas Chinesas/administração & dosagem , Medicamentos de Ervas Chinesas/química , Heme/metabolismo , Heme Oxigenase-1/metabolismo , Macrófagos/metabolismo , Medicina Tradicional Chinesa , Camundongos , Fator 2 Relacionado a NF-E2/metabolismo , Células RAW 264.7 , Saponinas/isolamento & purificação , Transdução de Sinais/efeitos dos fármacos , Triterpenos/isolamento & purificação
6.
Biomed Pharmacother ; 134: 111165, 2021 Feb.
Artigo em Inglês | MEDLINE | ID: mdl-33370633

RESUMO

High platelet reactivity and gastric mucosal injury after aspirin (ASA) treatment are associated with poor compliance and an increased risk of cardiovascular events. Panax notoginseng saponins (PNS) have been widely used for the treatment of coronary heart disease (CHD) in addition to antiplatelet drugs in China; however, the joint effect and possible mechanism of PNS in addition to ASA on platelet activation and gastric injury remain unclear. This study was designed to investigate the combinational effects of PNS with ASA, and to explore the underlying mechanism via arachidonic acid (AA) metabolism pathway using lipidomic analysis. In a randomized, assessor-blinded trial, 42 patients with stable coronary heart disease (SCHD) and chronic gastritis were randomly assigned to receive ASA (n = 21) or PNS + ASA (n = 21) for 2 months. Compared with ASA alone, PNS + ASA further inhibited CD62p expression, GPIIb-IIIa activation and platelet aggregation and led to increased platelet inhibition rate. PNS + ASA suppressed the activity of platelet cyclooxygenase (COX)-1, and decreased the production of TXB2, PGD2, PGE2, 11-HETE, the downstream oxylipids of AA/COX-1 pathway in platelets, compared with ASA alone. The severity of dyspepsia assessment (SODA) results showed that patients in PNS + ASA group exhibited relieved dyspeptic symptoms as compared with those in ASA group, which might be associated with enhanced secretion of gastrin and motilin. In vivo study of myocardial infarction rats demonstrated that PNS attenuated ASA-induced gastric mucosal injury, which was related to markedly boosted gastric level of 6,15-diketo-13,14-dihydro-prostaglandin (PG)F1α, 13,14-dihydro-15-keto-PGE2 and PGE2 from AA/PG pathway in response to PNS + ASA compared with ASA alone. In summary, our study demonstrated that the combination of PNS and ASA potentiated the antiplatelet effect of ASA via AA/COX-1/TXB2 pathway in platelets, and mitigated ASA-related gastric injury via AA/PG pathway in gastric mucosa.


Assuntos
Ácido Araquidônico/metabolismo , Aspirina/uso terapêutico , Plaquetas/efeitos dos fármacos , Doença das Coronárias/tratamento farmacológico , Mucosa Gástrica/efeitos dos fármacos , Gastrite/tratamento farmacológico , Fármacos Gastrointestinais/uso terapêutico , Panax notoginseng , Extratos Vegetais/uso terapêutico , Ativação Plaquetária/efeitos dos fármacos , Inibidores da Agregação de Plaquetas/uso terapêutico , Saponinas/uso terapêutico , Adulto , Idoso , Animais , Aspirina/efeitos adversos , Pequim , Plaquetas/metabolismo , Doença Crônica , Doença das Coronárias/diagnóstico , Doença das Coronárias/metabolismo , Citoproteção , Sinergismo Farmacológico , Feminino , Mucosa Gástrica/metabolismo , Mucosa Gástrica/patologia , Gastrite/diagnóstico , Gastrite/metabolismo , Fármacos Gastrointestinais/efeitos adversos , Fármacos Gastrointestinais/isolamento & purificação , Humanos , Lipidômica , Masculino , Pessoa de Meia-Idade , Panax notoginseng/química , Extratos Vegetais/efeitos adversos , Extratos Vegetais/isolamento & purificação , Inibidores da Agregação de Plaquetas/efeitos adversos , Ratos Wistar , Saponinas/efeitos adversos , Saponinas/isolamento & purificação , Fatores de Tempo , Resultado do Tratamento
7.
PLoS One ; 15(12): e0244654, 2020.
Artigo em Inglês | MEDLINE | ID: mdl-33382809

RESUMO

BACKGROUND: Saponins are secondary metabolites from plants added to shampoos and beverages to make them foam, and the sapogenins released from them upon acid hydrolysis are commonly used as starting materials for steroidal drugs. However, current methods embed the saponin in a thick "gum" material consisting of multiple impurities. This gum limits access to the saponin, reducing the efficiency of hydrolysis and requiring large amounts of heat, organic solvents and effort to recover the sapogenin. For centuries, herbalists have been making tinctures by soaking plant materials at room temperature, in mixtures of alcohol and water. Many herbal tinctures contain saponins floating freely in solution, gum free. The saponin from sarsaparilla (Smilax spp), sarsasaponin, yields the sapogenin, sarsasapogenin, upon acid hydrolysis. The retail price of sarsasapogenin is very high but would be lower if the "gum problem" could be avoided. MATERIALS AND METHODS: We incubated sarsaparilla tincture under different conditions of temperature, acidity and duration then used quantitative nuclear magnetic resonance (qNMR) to measure the amount of sarsasapogenin produced by hydrolysis as well as the amount of its epimer, smilagenin. RESULTS AND DISCUSSION: Most, if not all the sarsasaponin in sarsaparilla root powder is extracted into a solution of 45% ethanol (55% water) at room temperature and stays suspended without formation of any particles (gum). Acid hydrolysis of the saponin in this solution is very efficient, approaching 100%. The sarsasapogenin released by hydrolysis and the smilagenin produced by its epimerisation, migrate into the chloroform phase. CONCLUSION: Sarsaparilla saponin diffuses into and disperses in a solution of alcohol:water (45:55) at room temperature. Hydrolysis of saponins in tincture provides a simple, inexpensive and environmentally friendly alternative.


Assuntos
Saponinas/química , Smilax/química , Ácidos/química , Hidrólise , Raízes de Plantas/química , Sapogeninas/química , Saponinas/isolamento & purificação , Metabolismo Secundário
8.
Am J Chin Med ; 48(6): 1331-1351, 2020.
Artigo em Inglês | MEDLINE | ID: mdl-32907361

RESUMO

Panax notoginseng is the most widely used Chinese medicinal herb for the prevention and treatment of ischemic diseases. Its main active ingredients are saponins, including ginsenoside Rb1, ginsenoside Rg1, and notoginsenoside R1, among others. This review provides an up-to-date overview on the pharmacological roles of P. notoginseng constituents in cerebral ischemia. The saponins of P. notoginseng induce a variety of pharmacological effects in the multiscale mechanisms of cerebral ischemic pathophysiology, including anti-inflammatory activity, reduction of oxidative stress, anti-apoptosis, inhibition of amino acid excitotoxicity, reduction of intracellular calcium overload, protection of mitochondria, repairing the blood-brain barrier, and facilitation of cell regeneration. Regarding cell regeneration, P. notoginseng not only promotes the proliferation and differentiation of neural stem cells, but also protects neurons, endothelial cells and astrocytes in cerebral ischemia. In conclusion, P. notoginseng may treat cerebrovascular diseases through multiple pharmacological effects, and the most critical ones need further investigation.


Assuntos
Isquemia Encefálica/tratamento farmacológico , Ginsenosídeos/farmacologia , Ginsenosídeos/uso terapêutico , Panax notoginseng/química , Fitoterapia , Saponinas/farmacologia , Saponinas/uso terapêutico , Aminoácidos/toxicidade , Animais , Anti-Inflamatórios , Antioxidantes , Apoptose/efeitos dos fármacos , Barreira Hematoencefálica/patologia , Isquemia Encefálica/etiologia , Isquemia Encefálica/patologia , Isquemia Encefálica/prevenção & controle , Cálcio/metabolismo , Autorrenovação Celular/efeitos dos fármacos , Depuradores de Radicais Livres , Ginsenosídeos/isolamento & purificação , Humanos , Fármacos Neuroprotetores , Estresse Oxidativo/efeitos dos fármacos , Saponinas/isolamento & purificação
9.
Am J Chin Med ; 48(4): 1021-1034, 2020.
Artigo em Inglês | MEDLINE | ID: mdl-32471314

RESUMO

Codonopsis lanceolata roots have been widely used in Korean cuisine and traditional medicine. This study aimed to investigate the antimetastatic effects of lancemaside A, a major triterpenoid saponin, isolated from the roots of C. lanceolata, in human ovarian cancer cells. Lancemaside A significantly suppressed the migration and invasion and the expression of matrix metalloproteinases (MMPs)-2 and -9 in ovarian cancer A2780 and SKOV3 cells. Treatment with lancemaside A generated reactive oxygen species (ROS) in ovarian cancer cells. However, treatment with anti-oxidant N-acetyl-L-cysteine (NAC) significantly negated the anti-invasive activity of lancemaside A. Additionally, lancemaside A activated p38 MAP kinase, which is mediated by ROS generation. This is the first study, to our knowledge, to reveal that lancemaside A isolated from the roots of C. lanceolata exerts antimetastatic activity through inhibition of MMP expression and cancer cell invasion via activation of the ROS-mediated p38 pathway.


Assuntos
Codonopsis/química , Sistema de Sinalização das MAP Quinases/efeitos dos fármacos , Sistema de Sinalização das MAP Quinases/genética , Invasividade Neoplásica/genética , Invasividade Neoplásica/patologia , Neoplasias Ovarianas/patologia , Raízes de Plantas/química , Espécies Reativas de Oxigênio/metabolismo , Saponinas/farmacologia , Proteínas Quinases p38 Ativadas por Mitógeno/metabolismo , Antineoplásicos Fitogênicos , Linhagem Celular Tumoral , Feminino , Expressão Gênica , Humanos , Saponinas/isolamento & purificação , Proteínas Quinases p38 Ativadas por Mitógeno/genética
10.
J Chromatogr A ; 1620: 461010, 2020 Jun 07.
Artigo em Inglês | MEDLINE | ID: mdl-32173025

RESUMO

In this paper, adsorption mechanism of triterpenoid saponins in reversed-phase liquid chromatography (RPLC) and hydrophilic interaction liquid chromatography (HILIC) was proposed based on the study of the retention behavior of mogroside V as test substance. The change of peak shape of mogroside V and its influencing factors was first investigated. As the increase of sample loading, a tailing peak of mogroside V was observed in MeOHH2O of both two modes. It was the fronting peak in ACNH2O of HILIC while there was a transition from fronting peak to tailing peak in ACNH2O of RPLC that was largely affected by column temperature and ACN concentration. The adsorption isotherm of mogroside V in ACNH2O of RPLC was fitted by Moreau model, where a monolayer adsorption with large inter-molecular interaction was formed on the C18 surface. While in ACNH2O of HILIC, the adsorption of mogroside V was in accordance with BET model, showing multilayer adsorption behavior. In MeOHH2O of both HILIC and RPLC, there was always monolayer adsorption, which was fitted by Langmuir model. At last, by choosing the suitable chromatographic mode, controlling the key factors such as the solvent concentration and column temperature, and predicting the broadening trend of peak, three methods were screened out, namely, C18 column with 22% ACN (30 °C), Click XIon column with 90% MeOH or 70% ACN, to get mogroside V of purity greater than 98% from Siraitia grosvenorii extract. Among them, the RPLC method of 22% ACN that showed the highest loading sample per hour (1.92%) and the lowest solvent consumption emerged as the best approach.


Assuntos
Cromatografia Líquida/métodos , Cromatografia de Fase Reversa/métodos , Interações Hidrofóbicas e Hidrofílicas , Saponinas/isolamento & purificação , Triterpenos/isolamento & purificação , Adsorção , Saponinas/química , Solventes , Temperatura , Triterpenos/química
11.
Ecotoxicol Environ Saf ; 193: 110318, 2020 Apr 15.
Artigo em Inglês | MEDLINE | ID: mdl-32105945

RESUMO

The current study aimed to examine, for the first time, the relationship between exposure to deltamethrin (DLM) and atherogenic lipid profile disorders in adult Wistar rats, as well as, to verify the mechanism of the beneficial role of Zygophyllum album leaves extracts (ZALE). The experimental study was assessed using DLM (4 mg/kg b.w) either alone or co administered with ZALE (400 mg/kg b.w) orally for 90 days in rats. RP-HPLC-DAD-ESI-QTOF-MS was used to identify the bioactive metabolites present in ZALE. Plasmatic and aortic total cholesterol (TC), LDL-cholesterol (LDL-C), native LDL (LDL-apo B-100) and oxidized LDL (ox-LDL) were evaluated using auto-analyzer and a sandwich ELISA, respectively. The protein expressions of LDLR (native LDL receptor) and CD36 (Scavenger receptor class B) were evaluated in aorta or liver with a Western blot. The pathology has been confirmed with lipid stain (Oil Red O). Phytochemicals analysis revealed the presence of fifteen saponins in ZALE. Rats intoxicated with DLM revealed a significant increase in plasmatic and aortic lipid profile (TC, LDL-C, LDL-apo B-100 and ox-LDL), as well as, the concentration of the plasmatic cytokines include TNF-α, IL-2 and IL-6, compared to control. Hepatic native LDL and aortic CD36 receptor expression were increased in DLM treated group, however aortic LDL-R does not present any modification, when compared to control. The detected disturbances in lipid parameters were supported by Oil Red O applied. Due to their antioxidant activity, the bioactive compounds in ZALE as powerful agents able to prevent the pro-atherogenic effect observed in DLM-treated animals. These metabolites modulated most of inflammatory markers, prevented accumulation of lipid and lipoprotein biomarkers, regulated the major receptor regulators of hepatic cholesterol metabolism, as well as normalize lipid distribution in liver and aorta tissue.


Assuntos
Aorta/efeitos dos fármacos , Aterosclerose/prevenção & controle , Poluentes Ambientais/toxicidade , Lipoproteínas LDL/sangue , Nitrilos/toxicidade , Piretrinas/toxicidade , Saponinas/farmacologia , Zygophyllum/química , Animais , Aorta/imunologia , Aorta/metabolismo , Aterosclerose/imunologia , Aterosclerose/metabolismo , Antígenos CD36/metabolismo , Colesterol/metabolismo , Metabolismo dos Lipídeos/efeitos dos fármacos , Fígado/efeitos dos fármacos , Fígado/imunologia , Fígado/metabolismo , Masculino , Folhas de Planta/química , Ratos , Ratos Wistar , Receptores de LDL/metabolismo , Saponinas/isolamento & purificação , Fator de Necrose Tumoral alfa/metabolismo
12.
IET Nanobiotechnol ; 14(1): 25-32, 2020 Feb.
Artigo em Inglês | MEDLINE | ID: mdl-31935674

RESUMO

In this study, saponin capped triangular silver nanocrystals have been synthesised using fenugreek seed extract, where the extract acts both as a reducing and capping agent. X-ray diffraction study confirms the purity and crystalline nature of the prepared nanocrystals and transmission electron microscopic study shows the triangular morphology with the average edge length of 72 nm, along with the atomic force microscopy study for the height or the width of the triangular nanocrystals. These nanocrystals have been investigated against a few pulses (seeds) such as Pisum sativum, Cicer arietinum and Vigna radiata for their effect on the germination as well as growth of root and shoot. Considering different concentration of silver nanocrystals solution, it has been found that 25 × 10-4 and 80 × 10-4 µg/ml are the minimum and maximum concentrations of silver nanocrystals, within this range, germination and subsequent growth of root and shoot are effective. The result shows significant positive influence on the growth of root and shoot of all seeds in comparison to those of unexposed control germination. Therefore, the result of this experiment has confirmed that the use of saponin capped silver nanocrystals enhances the germination and growth of plants.


Assuntos
Fabaceae/efeitos dos fármacos , Germinação/efeitos dos fármacos , Nanopartículas Metálicas/química , Saponinas , Prata , Fabaceae/química , Extratos Vegetais/química , Raízes de Plantas/efeitos dos fármacos , Brotos de Planta/efeitos dos fármacos , Saponinas/isolamento & purificação , Saponinas/farmacologia , Prata/química , Prata/farmacologia
13.
J Agric Food Chem ; 68(7): 2041-2053, 2020 Feb 19.
Artigo em Inglês | MEDLINE | ID: mdl-31967813

RESUMO

Cyclocarya paliurus is commonly used for the prevention and treatment of hypertension, diabetes, and inflammation in South China. Although research on the anti-inflammatory effects of C. paliurus leaves has been reported, no active anti-inflammatory compounds have been identified. In the present study, RAW 264.7 cells were used to establish a bioactivity-guided identification model to verify the inhibitory effects of C. paliurus leaves on inflammation and identify the anti-inflammatory constituents. The active fraction was isolated to yield 18 dammarane triterpenoid saponins, including 11 new 3,4-seco-dammarane triterpenoid saponins (1-11), the structures of which were identified on the basis of analyses of nuclear magnetic resonance (NMR) spectroscopy and mass spectrometry (MS) and comparison with literature data. Compounds 7, 8, 10, and 11 showed strong inhibition on nitric oxide (NO) productions, with IC50 values ranging from 8.23 to 11.23 µM. These four compounds significantly decreased the secretion of tumor necrosis factor-alpha (TNF-α), prostaglandin E2 (PGE2), and interleukin 6 (IL-6) in lipopolysaccharide-activated RAW 264.7 cells. Furthermore, compound 7 decreased the expression of the proteins cyclooxygenase-2 (COX-2), inducible nitric-oxide synthase (iNOS), and nuclear factor kappa-B (NF-κB/p65). In addition, the structure-activity relationships of the isolates were investigated. The results suggest that 3,4-seco-dammarane triterpenoid saponins may be used as potential anti-inflammatory drugs and warrant further investigation.


Assuntos
Anti-Inflamatórios/farmacologia , Juglandaceae/química , Extratos Vegetais/farmacologia , Saponinas/farmacologia , Triterpenos/farmacologia , Animais , Anti-Inflamatórios/química , Anti-Inflamatórios/isolamento & purificação , Interleucina-6/genética , Interleucina-6/imunologia , Macrófagos/efeitos dos fármacos , Camundongos , NF-kappa B/genética , NF-kappa B/imunologia , Óxido Nítrico Sintase Tipo II/genética , Óxido Nítrico Sintase Tipo II/imunologia , Extratos Vegetais/química , Extratos Vegetais/isolamento & purificação , Folhas de Planta/química , Células RAW 264.7 , Saponinas/química , Saponinas/isolamento & purificação , Triterpenos/química , Triterpenos/isolamento & purificação , Fator de Necrose Tumoral alfa/genética , Fator de Necrose Tumoral alfa/imunologia
14.
Biomed Pharmacother ; 124: 109935, 2020 Apr.
Artigo em Inglês | MEDLINE | ID: mdl-31986407

RESUMO

Intimal hyperplasia, the key event of arterial restenosis, is a result of vascular smooth muscle cell (VSMC) proliferation and migration. Previous studies have demonstrated that total Panax notoginseng saponin (TPNS) represses intimal hyperplasia and inhibits the proliferation of VSMCs following balloon injury. However, the underlying roles of TPNS in intimal hyperplasia remain unclear. In this study, we first found that TPNS inhibited the intimal hyperplasia and reversed the reduced m6A quantity in balloon catheter-injured rat carotid artery. Then, we measured the expression profiles of m6A "writers" (i.e., methyltransferase like 3 (METTL3), methyltransferase like 14 (METTL14), and WT1 associated protein (WTAP)) and "erasers" (i.e., FTO alpha-ketoglutarate dependent dioxygenase (FTO) and alkB homolog 5, RNA demethylase (ALKBH5)) in vivo and found that TPNS up-regulated the reduced the WTAP expression in balloon catheter-injured rat carotid artery. Furthermore, we illustrated that TPNS inhibited the viability, proliferation, and migration potential of VSMCs via promotion of WTAP expression and suppression of WTAP restored the TPNS-induced inhibition of cell viability, proliferation and migration potential of VSMCs. In addition, we found that p16 was up-regulated in VSMCs treated with TPNS and repression of p16 restored the TPNS-induced inhibition of cell viability, proliferation and migration potential of VSMCs. Finally, we elucidated that, mechanistically, WTAP exerted its role by regulating p16 via m6A modification. Collectively, our results reveal the WTAP-p16 signaling axis and highlight the critical roles of m6A modification in intimal hyperplasia. Thus, this study provided a potential biomarker for the assessment of intimal hyperplasia risk following angioplasty as well as a novel therapeutic target for this disease.


Assuntos
Proliferação de Células/efeitos dos fármacos , Músculo Liso Vascular/efeitos dos fármacos , Panax notoginseng/química , Saponinas/farmacologia , Adenosina/análogos & derivados , Adenosina/metabolismo , Animais , Lesões das Artérias Carótidas/tratamento farmacológico , Lesões das Artérias Carótidas/patologia , Movimento Celular/efeitos dos fármacos , Células Cultivadas , Inibidor p16 de Quinase Dependente de Ciclina/metabolismo , Humanos , Hiperplasia/tratamento farmacológico , Masculino , Músculo Liso Vascular/citologia , Ratos , Ratos Sprague-Dawley , Saponinas/isolamento & purificação , Transdução de Sinais/efeitos dos fármacos , Túnica Íntima/efeitos dos fármacos , Túnica Íntima/patologia , Proteínas WT1/metabolismo
15.
Phytother Res ; 34(4): 788-795, 2020 Apr.
Artigo em Inglês | MEDLINE | ID: mdl-31782210

RESUMO

Neuropathic pain is associated with an increased sensitivity to painful stimuli or abnormal sensitivity to otherwise innocuous stimuli. However, in addition to adverse effects, currently available drugs have shown limited response in patients with neuropathic pain, which provides a rationale to explore new drug classes acting on novel targets and with better efficacy and safety profiles. Here, we found that saikosaponins potently inhibit agonist-induced activation of the transient receptor potential A1 (TRPA1) channel, which has been reported to mediate neuropathic pain by sensing a variety of chemical irritants. Molecular docking and site-directed mutagenesis analyses suggested that saikosaponins bind to the hydrophobic pocket in TRPA1 near the Asn855 residue, which, when mutated to Ser, was previously associated with enhanced pain perception in humans. In support of these findings, saikosaponin D significantly attenuated agonist-induced nociceptive responses and vincristine-induced mechanical hypersensitivity in mice. These results indicate that saikosaponins are TRPA1 antagonists and provide a basis for further elaboration of saikosaponin derivatives for the development of new therapeutics for neuropathic pain.


Assuntos
Ácido Oleanólico/análogos & derivados , Saponinas/farmacologia , Canal de Cátion TRPA1/antagonistas & inibidores , Animais , Avaliação Pré-Clínica de Medicamentos , Células HEK293 , Humanos , Hiperalgesia/diagnóstico , Hiperalgesia/tratamento farmacológico , Hiperalgesia/metabolismo , Masculino , Camundongos , Camundongos Endogâmicos ICR , Simulação de Acoplamento Molecular , Neuralgia/diagnóstico , Neuralgia/tratamento farmacológico , Ácido Oleanólico/química , Ácido Oleanólico/isolamento & purificação , Ácido Oleanólico/metabolismo , Ácido Oleanólico/farmacologia , Medição da Dor , Saponinas/química , Saponinas/isolamento & purificação , Saponinas/metabolismo , Canal de Cátion TRPA1/química , Canal de Cátion TRPA1/metabolismo
16.
Food Chem ; 309: 125786, 2020 Mar 30.
Artigo em Inglês | MEDLINE | ID: mdl-31704078

RESUMO

The ultrasonic-assisted extraction of total saponins from alfalfa leaves was optimised by the simultaneous maximization of the yield and bioaccessibility as a factor with increasingly great relevance in the biological activity by Response Surface Methodology. The kinetics of total saponins and bioaccessibility were investigated for the optimum ultrasound-assisted method compared to conventional method by the pseudo-first order model. The optimum extraction conditions were of solvent/raw material ratio of 11.4 mL/g, extraction time of 2.84 h, extraction temperature of 76.8 °C, ultrasound power of 112.0 w and ethanol concentration of 78.2%. The yield of total saponins and bioaccessibility was 1.61 and 18.6%, respectively. The yield rate constant for the ultrasound extraction was almost two times more than that of the heat-reflux method. Ultrasonic-assisted extraction, comparing to conventional method, had greater efficiency for the extraction yield and bioaccessibility of total saponins.


Assuntos
Medicago sativa/química , Saponinas/análise , Sonicação , Etanol/química , Cinética , Medicago sativa/metabolismo , Extratos Vegetais/química , Folhas de Planta/química , Folhas de Planta/metabolismo , Saponinas/isolamento & purificação , Solventes/química
17.
Phytochemistry ; 169: 112162, 2020 Jan.
Artigo em Inglês | MEDLINE | ID: mdl-31627115

RESUMO

Twelve undescribed triterpenoid pentacyclic glycosides, medicagenic acid (3-O-ß-D-glucuronopyranosyl-28-O-{[ß-D-glucopyranosyl-(1 → 3)-α-L-rhamnopyranosyl-(1 → 2)]-[α-L-rhamnopyranosyl-(1 → 3)]-4-O-acetyl-ß-D-fucopyranosyl-(1→)}-2ß,3ß-dihydroxyolean-12-ene-23,28-dioic acid, 3-O-ß-D-glucuronopyranosyl-28-O-{[α-L-rhamnopyranosyl-(1 → 2)]-[ß-D-apiofuranosyl-(1 → 3)]-4-O-acetyl-ß-D-fucopyranosyl-(1→)}-2ß,3ß-dihydroxyolean-12-ene-23,28-dioic acid, 3-O-ß-D-glucuronopyranosyl-28-O-{[α-L-rhamnopyranosyl-(1 → 2)]-3,4-O-diacetyl-ß-D-fucopyranosyl-(1→)}-2ß,3ß-dihydroxyolean-12-ene-23,28-dioic acid, 28-O-{[6-O-acetyl-ß-D-glucopyranosyl-(1 → 2)]-[2-O-acetyl-α-L-rhamnopyranosyl-(1 → 4)-ß-D-glucopyranosyl-(1 → 6)]-ß-D-glucopyranosyl-(1→)}-2ß,3ß-dihydroxyolean-12-ene-23,28-dioic acid, 28-O-{[6-O-acetyl-ß-D-glucopyranosyl-(1 → 2)]-[3-O-acetyl-α-L-rhamnopyranosyl-(1 → 4)-ß-D-glucopyranosyl-(1 → 6)]-ß-D-glucopyranosyl-(1→)}-2ß,3ß-dihydroxyolean-12-ene-23,28-dioic acid, 28-O-{[6-O-acetyl-ß-D-glucopyranosyl-(1 → 2)]-[4-O-acetyl-α-L-rhamnopyranosyl-(1 → 4)-ß-D-glucopyranosyl-(1 → 6)]-ß-D-glucopyranosyl-(1→)}-2ß,3ß-dihydroxyolean-12-ene-23,28-dioic acid, 28-O-{[6-O-acetyl-ß-D-glucopyranosyl-(1 → 2)]-[ß-D-glucopyranosyl-(1 → 6)]-ß-D-glucopyranosyl-(1→)}-2ß,3ß-dihydroxyolean-12-ene-23,28-dioic acid, 28-O-{[ß-D-glucopyranosyl-(1 → 2)]-[ß-D-glucopyranosyl-(1 → 6)]-ß-D-glucopyranosyl-(1→)}-2ß,3ß-dihydroxyolean-12-ene-23,28-dioic acid), zanhic acid (3-O-ß-D-glucuronopyranosyl-28-O-{[ß-D-glucopyranosyl-(1 → 3)-α-L-rhamnopyranosyl-(1 → 2)]-[α-L-rhamnopyranosyl-(1 → 3)]-4-O-acetyl-ß-D-fucopyranosyl-(1→)}2ß,3ß,16α-trihydroxyolean-12-ene-23,28-dioic acid, 3-O-ß-D-glucuronopyranosyl-28-O-{[ß-D-glucopyranosyl-(1 → 3)-α-L-rhamnopyranosyl-(1 → 2)]-ß-D-fucopyranosyl-(1→)}-2ß,3ß,16α-trihydroxyolean-12-ene-23,28-dioic acid), 29-hydroxy-medicagenic acid (3-O-ß-D-glucuronopyranosyl-28-O-{[ß-D-glucopyranosyl-(1 → 3)-α-L-rhamnopyranosyl-(1 → 2)]-[α-L-rhamnopyranosyl-(1 → 3)]-4-O-acetyl-ß-D-fucopyranosyl-(1→)}-2ß,3ß,29ß-trihydroxyolean-12-ene-23,28-dioic acid) and herniaric acid (28-O-{[6-O-acetyl-ß-D-glucopyranosyl-(1 → 2)]-[α-L-rhamnopyranosyl-(1 → 4)-ß-D-glucopyranosyl-(1 → 6)]-ß-D-glucopyranosyl-(1→)}-2ß,3ß-dihydroxyolean-18-ene-23,28-dioic acid) were isolated from the whole plant extract of Herniaria glabra L. (Caryophyllaceae), wild growing in the Ukraine. In addition, five known triterpenoid saponins; i.e. herniariasaponins 1, 4, 5, 6, and 7 were also isolated. Their structures were elucidated by HRESIMS, 1D and 2D NMR spectroscopy, as well as by comparison with the literature data. Twelve herniariasaponins, the purified crude extract, and the saponin fraction were evaluated in vitro for their xanthine oxidase, collagenase, elastase, and tyrosinase inhibitory activity. Moreover, herniariasaponins 4, 5, and 7 were screened for their cholinesterase inhibitory potential. As a result, no or low inhibition towards the mentioned enzymes was observed.


Assuntos
Caryophyllaceae/química , Inibidores Enzimáticos/farmacologia , Extratos Vegetais/farmacologia , Saponinas/farmacologia , Animais , Colinesterases/metabolismo , Colagenases/metabolismo , Inibidores Enzimáticos/química , Inibidores Enzimáticos/isolamento & purificação , Conformação Molecular , Monofenol Mono-Oxigenase/antagonistas & inibidores , Monofenol Mono-Oxigenase/metabolismo , Elastase Pancreática/antagonistas & inibidores , Elastase Pancreática/metabolismo , Extratos Vegetais/química , Extratos Vegetais/isolamento & purificação , Saponinas/química , Saponinas/isolamento & purificação , Estereoisomerismo , Ucrânia , Xantina Oxidase/antagonistas & inibidores , Xantina Oxidase/metabolismo
18.
Planta Med ; 86(1): 70-77, 2020 Jan.
Artigo em Inglês | MEDLINE | ID: mdl-31671467

RESUMO

Four new barringtogenol C-type triterpenoid saponins, namely acerplatanosides A - D (1: -4: ), along with 22 known compounds (5: -26: ), were isolated from the stem bark of Norway maple (Acer platanoides). Their structures were elucidated on the basis of comprehensive spectroscopic analyses and chemical hydrolysis. This is the first report of triterpenoid saponins isolated from Norway maple. Compounds 1, 3: , and 4: showed cytotoxicity against 4 human cancer cell lines with IC50 values ranging from 9.4 to 39.5 µM.


Assuntos
Acer/química , Antineoplásicos Fitogênicos/isolamento & purificação , Saponinas/isolamento & purificação , Triterpenos/isolamento & purificação , Antineoplásicos Fitogênicos/química , Linhagem Celular Tumoral , Ensaios de Seleção de Medicamentos Antitumorais , Humanos , Estrutura Molecular , Casca de Planta/química , Saponinas/química , Triterpenos/química
19.
Food Chem ; 303: 125394, 2020 Jan 15.
Artigo em Inglês | MEDLINE | ID: mdl-31473455

RESUMO

A simple and effective vesicle based ultrasonic-assisted extraction (UAE) method was developed for extraction of active compounds in functional food. The target analytes were determined by ultra-high performance liquid chromatography with ultraviolet detector. Surfactant vesicle was adopted as extraction solvent. Different operating conditions including the type and concentration of vesicle, extraction time and solid to liquid ratio were investigated by single-factor experiments and response surface methodology. Optimized experimental conditions were 1% (w/v) of DTAB/SDS vesicle, 20 min of extraction time and 160 mg/mL of solid to liquid ratio. The proposed method provided good linearity in the linear range of 10-1000 µg/mL with regression coefficients larger than 0.999, low limits of detection of 27.64-55.67 ng/mL, good precision with relative standard deviations below 0.35%, and satisfactory recoveries of 83.84-90.92% for tested saponins. Consequently, the proposed vesicle based UAE method was well suited for the extraction of saponins in Panax notoginseng.


Assuntos
Fracionamento Químico/métodos , Panax notoginseng/química , Saponinas/isolamento & purificação , Ultrassom , Cromatografia Líquida de Alta Pressão , Saponinas/análise
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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