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1.
J Pharm Biomed Anal ; 177: 112843, 2020 Jan 05.
Artigo em Inglês | MEDLINE | ID: mdl-31509788

RESUMO

An UHPLC method was developed for the determination of 15 prenylflavonoids from aerial parts of Epimedium grandiflorum and related species (Berberidaceae). The separation was achieved using a reverse phased column and water/acetonitrile gradient as a mobile phase at a temperature of 40°C. The developed analytical method was validated for linearity, limits of detection (LOD) and limits of quantification (LOQ), stability and repeatability. The LOD and LOQ were found to be in the range from 0.1-0.5 µg/mL and 0.3-1 µg/mL, respectively. The wavelength used for quantification with the photodiode array detector was 269 nm. The total content of 15 prenylflavonoids was 9.1-20.6 mg/g for E. grandiflorum (except for sample #2899 and #20862), 5.6-35.4 mg/g for E. brevicornu and 10.8-30.5 mg/g for E. sagittatum. Twenty dietary supplements contained in the range from 0.1 to 81.7 mg/day. The developed method is simple, rapid and especially suitable for quality assessment of E. grandiflorum and dietary supplements containing E. grandiflorum. Liquid chromatography quadrupole time-of-flight-mass spectrometry (LC-QToF) is described for the identification and confirmation of compounds in plant samples and dietary supplements. This technique is also used for chemical profiling of Epimedium samples. This method involved the use of protonated ions in the positive ion mode and deprotonated ions in the negative ion mode with extracted ion chromatogram (EIC). Chemometric analytical tools for visualizing the plant and commercial samples quality were used for discriminating between Epimedium species and dietary supplements with regards to the relative content or presence of components. A HPTLC method was also developed for the fast chemical fingerprint analysis of Epimedium species.


Assuntos
Suplementos Nutricionais/análise , Epimedium/química , Flavonoides/análise , Controle de Qualidade , Cromatografia Líquida de Alta Pressão/métodos , Suplementos Nutricionais/normas , Estudos de Viabilidade , Flavonoides/química , Cromatografia Gasosa-Espectrometria de Massas/métodos , Limite de Detecção , Componentes Aéreos da Planta/química , Reprodutibilidade dos Testes , Espectrometria de Massas por Ionização por Electrospray/métodos
2.
Zhongguo Zhong Yao Za Zhi ; 44(18): 4048-4052, 2019 Sep.
Artigo em Chinês | MEDLINE | ID: mdl-31872744

RESUMO

Osteoporosis is a systematic bone disease,characterized by deterioration in bone mass or micro-architecture,and increasing risk of fragility and fractures. With the development of aging problems,osteoporosis has been a global health problem. At present,due to the undesirable side effects of synthetic osteoporosis inhibitors,more efforts are made in treatment of osteoporosis by traditional Chinese medicine and its prescriptions. Epimedii Folium,one of the most common herbs for osteoporosis,has attracted great attentions worldwide.In this study,network pharmacology was employed to analyze the active components and potential molecular mechanism of Epimedii Folium on osteoporosis. Component-target network analysis showed that those with higher molecular network degree were flavonoids,with estrogen-like activity,antioxidation and free radical-scavenging activities,playing certain roles in preventing and treating osteoporosis. On the other hand,the targets with high degree were mostly related with sex hormone,osteoclast differentiation,bone matrix degradation,and reactive oxygen species in drug-target network. Multiple components of Epimedii Folium could be interacted with these targets. This study shows that Epimedium could prevent and treat osteoporosis through multiple active ingredients acting on multiple targets.


Assuntos
Medicamentos de Ervas Chinesas/farmacologia , Epimedium/química , Osteoporose/tratamento farmacológico , Humanos , Medicina Tradicional Chinesa , Folhas de Planta/química , Plantas Medicinais/química
3.
BMC Complement Altern Med ; 19(1): 316, 2019 Nov 19.
Artigo em Inglês | MEDLINE | ID: mdl-31744482

RESUMO

BACKGROUND: Icariin (ICA) is the major active ingredient extracted from Chinese herbal medicine Epimedium, which has the effects of improving cardiovascular function, inducing tumor cell differentiation and increasing bone formation. It is still rarely reported that ICA can exert its therapeutic potential in asthma via anti-airway remodeling. The point of the study was to estimate the role of ICA in anti-. airway remodeling and its possible mechanism of action in a mouse ovalbumin. (OVA)-induced asthma model. METHODS: Hematoxylin and Eosin Staining were performed for measuring airway remodeling related indicators. ELISA, Western blot and Immunohistochemistr-. y (IHC) were used for analyzing the level of protein. RT-PCR was used for analyzing the level of mRNA. RESULTS: On days 1 and 8, mice were sensitized to OVA by intraperitoneal injection. From day 16 to day 43, previously sensitized mice were exposed to OVA once daily by nebulizer. Interventions were performed orally with ICA (ICA low, medium and high dose groups) or dexamethasone 1 h prior to each OVA exposure. ICA improves pulmonary function, attenuates pulmonary inflammation and airway remodeling in mice exposed to OVA. Histological and Western blot analysis of the lungs show that ICA suppressed transforming growth factor beta 1 and vascular endothelial growth factor expression. Increase in interleukin 13 and endothelin-1 in serum and bronchoalveolar lavage fluid in OVA-induced asthmatic mice are also decreased by ICA. ICA attenuates airway smooth muscle cell proliferation, as well as key factors in the MAPK/Erk pathway. CONCLUSIONS: The fact that ICA can alleviate OVA-induced asthma at least partly through inhibition of ASMC proliferation via MAPK/Erk pathway provides a solid theoretical basis for ICA as a replacement therapy for asthma. These data reveal the underlying reasons of the use of ICA-rich herbs in Traditional Chinese Medicine to achieve good results in treating asthma.


Assuntos
Remodelação das Vias Aéreas/efeitos dos fármacos , Asma/tratamento farmacológico , Medicamentos de Ervas Chinesas/administração & dosagem , Epimedium/química , Flavonoides/administração & dosagem , Animais , Asma/genética , Asma/metabolismo , Asma/fisiopatologia , Endotelina-1/genética , Endotelina-1/metabolismo , Feminino , Humanos , Interleucina-13/genética , Interleucina-13/metabolismo , Camundongos , Camundongos Endogâmicos BALB C , Fator A de Crescimento do Endotélio Vascular/genética , Fator A de Crescimento do Endotélio Vascular/metabolismo
4.
Zhongguo Zhong Yao Za Zhi ; 44(9): 1857-1861, 2019 May.
Artigo em Chinês | MEDLINE | ID: mdl-31342713

RESUMO

The change of icariin( ICA) content in thirty-three samples of five Epimedium species listed in the Chinese Pharmacopoeia( 2015 edition),including E. brevicornu,E. sagittatum,E. pubescens,E. koreanum,and E. wushanense has been investigated in this study. The results indicated that the optimized process procedure was baking at 150 ℃ for 30 min,and 3'''-carbonyl-2″-ß-L-quinovosyl icariin( CQICA) could not be translated into ICA and ICA could be converted under this heating process condition. ICA increased remarkably after the heating process by 1-3 times in E. brevicornu,E. wushanense and E. koreanum,and increased lightly in E. brevicornum and E. pubescens,while ICA slightly increased or decreased in E. sagittatum and E. wushanense.


Assuntos
Medicamentos de Ervas Chinesas/química , Epimedium/química , Flavonoides/análise , Temperatura Alta , Compostos Fitoquímicos/análise , Manejo de Espécimes
5.
Breast Cancer ; 26(6): 766-775, 2019 Nov.
Artigo em Inglês | MEDLINE | ID: mdl-31172425

RESUMO

BACKGROUND: Icariin is a major component isolated from Epimedium brevicornum Maxim and has been reported to exhibit anti-tumor activity. However, whether icariin could reverse the acquired drug resistance in breast cancer remains largely unclear. Therefore, this study was designed to explore the antitumor effects of icariin and its underlying mechanisms in a tamoxifen-resistant breast cancer cell line MCF-7/TAM. METHODS: 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) assay and Lactate dehydrogenase (LDH) assay were performed to determine the effects of icariin on cell viability and cell death. Cell cycle progression and apoptosis were detected by flow cytometry analysis. Transmission electron microscopy (TEM) assay was utilized to observe cell autophagy. The downstream protein levels were measured using western blotting. RESULTS: Here, we observed that icariin treatment not only inhibited the growth of MCF-7 but also has a potential function to overcome tamoxifen resistance in MCF-7/TAM. Moreover, icariin significantly induced cell cycle G0/G1 phase arrest and apoptosis, as well as suppressed autophagy. At molecular levels, icariin treatment remarkably down-regulated the expression levels of CDK2, CDK4, Cyclin D1, Bcl-2, LC3-1, LC3-II, AGT5, Beclin-1, but upregulated the expression levels of caspase-3, PARP and p62. Most importantly, we found inhibition of autophagy via 3-MA treatment could significantly enhance the effects of icariin on cell viability and apoptosis. Enhanced autophagy via autophagy related 5 (ATG5) overexpression could partially reverse the effects of icariin on cell viability and apoptosis. CONCLUSION: These results revealed that icariin might potentially be useful as an adjuvant agent in cancer chemotherapy to enhance the effect of tamoxifen through suppression of autophagy in vitro and provide insight into the therapeutic potential of icariin for the treatment of chemo-resistant breast cancer.


Assuntos
Apoptose/efeitos dos fármacos , Autofagia/efeitos dos fármacos , Neoplasias da Mama/patologia , Resistencia a Medicamentos Antineoplásicos/efeitos dos fármacos , Flavonoides/farmacologia , Extratos Vegetais/farmacologia , Tamoxifeno/efeitos adversos , Proteína 5 Relacionada à Autofagia/genética , Proteína 5 Relacionada à Autofagia/metabolismo , Neoplasias da Mama/tratamento farmacológico , Caspase 3/metabolismo , Pontos de Checagem do Ciclo Celular/efeitos dos fármacos , Sobrevivência Celular/efeitos dos fármacos , Epimedium/química , Feminino , Humanos , Células MCF-7 , Poli(ADP-Ribose) Polimerases/metabolismo , Proteínas Proto-Oncogênicas c-bcl-2/metabolismo , Moduladores Seletivos de Receptor Estrogênico/efeitos adversos , Moduladores Seletivos de Receptor Estrogênico/uso terapêutico , Transdução de Sinais/efeitos dos fármacos , Tamoxifeno/uso terapêutico , Transfecção
6.
Nutrients ; 11(5)2019 May 18.
Artigo em Inglês | MEDLINE | ID: mdl-31109081

RESUMO

Atherosclerosis is the key factor responsible for cardiovascular events, which is a major cause of morbidities and mortalities worldwide. It is well known that high-density lipoprotein (HDL) oxidation and glycation increases the risk for atherosclerosis. Epimedium koreanum has been used as a traditional oriental medicine for treating erectile dysfunction, kidney diseases, osteoporosis, and breast cancer. However, no reports on the effects of E. koreanum on HDL modification exist. In this study, we investigated the inhibitory effects of E. koreanum extract and its eight flavonoids, which are: (1) anhydroicaritin 3-O-rhamnoside, (2) ß-anhydroicaritin, (3-5) epimedins A-C, (6) epimedoside A, (7) icariin, and (8) des-O-methyl-ß-anhydroicaritin, against HDL modification. HDLs obtained from pooled human plasma samples were incubated in vitro with E. koreanum extract or each compound in the presence of copper sulfate or fructose. The HDL modifications were evaluated by measuring generation of conjugated dienes, production of thiobarbituric acid reactive substances, change in electrophoretic mobility of apoA-I, advanced glycation end products formation, and apoA-I aggregation. Consequently, E. koreanum extract and compound 8 suppressed HDL modification through inhibition of lipid peroxidation, apoA-I aggregation, negative charge increase, and AGEs formation. In particular, compound 8 showed more potent inhibitory effect on HDL modification than the extracts, suggesting its protective role against atherosclerosis via inhibition of HDL oxidation and glycation.


Assuntos
Aterosclerose/prevenção & controle , HDL-Colesterol/metabolismo , Epimedium/química , Flavonoides/farmacologia , Fitoterapia , Extratos Vegetais/farmacologia , Apolipoproteína A-I/metabolismo , Flavonoides/química , Fluoresceínas , Produtos Finais de Glicação Avançada , Humanos , Estrutura Molecular , Oxirredução/efeitos dos fármacos , Componentes Aéreos da Planta , Substâncias Reativas com Ácido Tiobarbitúrico
7.
Zhongguo Zhong Yao Za Zhi ; 44(8): 1715-1723, 2019 Apr.
Artigo em Chinês | MEDLINE | ID: mdl-31090340

RESUMO

Epimedii Folium,a commonly used traditional Chinese medicine,has the effect of tonifying kidney Yang,strengthening bones and treating rheumatism. However,in recent years,the number of reports on adverse reactions of Epimedii Folium and its Chinese patent medicines such as Xianling Gubao Capsules and Zhuanggu Guanjie Pills has been gradually increased,and the toxicity of Epimedii Folium has attracted more and more attention. In this article,the ancient and modern literature on Epimedii Folium was traced through a comprehensive and systematic literature analysis method. According to the 2015 edition of the Chinese Pharmacopoeia,Epimedii Folium refers to the dried leaves of Epimedii Folium brevicomu,E. sugittutum,E. pubescens or E. koreuuum. The Chinese Pharmacopoeia also includes E. wushanense of Wushan Epimedium,which is the same plant variety as Epimedium. The study showed that there were differences in the geographical distribution,composition and toxicity among five species of Epimedium. This paper also explained the toxicity mechanism as well as efficacy enhancing and toxicity reducing effects of Epimedii Folium,and reported its related adverse reaction cases. Through a retrospective comparative study on the toxicity of the modern Chinese patent medicines Xianling Gubao Capsules and Zhuanggu Guanjie Pills containing Epimedii Folium,it was believed that Epimedii Folium had cardiovascular system toxicity,neurotoxicity,hepatotoxicity,long-term toxicity,acute toxicity,genotoxicity and special toxicity; its safe medication factors included patient syndrome,doctor factors,drug factors,processing and compatibility factors. Meanwhile,strategies were proposed to improve patient safety medication awareness,standardize Epimedii Folium varieties and quality supervision,and the toxicity of Epimedii Folium was studied,hoping to draw attention from scholars to the safety of Epimedii Folium,improve the safe use of Epimedii Folium,and prevent adverse reactions.


Assuntos
Medicamentos de Ervas Chinesas/efeitos adversos , Epimedium/química , Humanos , Medicina Tradicional Chinesa , Folhas de Planta/química , Estudos Retrospectivos
9.
Georgian Med News ; (287): 137-140, 2019 Feb.
Artigo em Russo | MEDLINE | ID: mdl-30958306

RESUMO

One of the most famous aphrodisiac plants and remedy for recoveryerectile dysfunction is Estrellita Epimedium (Epimedium sagittatum). On this basis, development of the new dosage form (capsules with dry extract of Epimedium strelolist) is one of the promising directions in phytotherapy of erectile dysfunction in men. The main task in development of a new dosage form is the study of the physical-chemical and technological active pharmaceutical substance's (API) characteristics, such as crystal form, solubility, flowability, angle of repose, tap density, water. In this study, the dry extract of Epimedium strelolist is an API. Research of above characteristics will determine the choice of excipients and technology of dosage form.


Assuntos
Química Farmacêutica , Epimedium/química , Disfunção Erétil/tratamento farmacológico , Excipientes , Preparações Farmacêuticas/química , Tecnologia Farmacêutica , Cristalização , Formas de Dosagem , Medicamentos de Ervas Chinesas , Humanos , Masculino , Fitoterapia , Preparações de Plantas
10.
Molecules ; 24(7)2019 Apr 01.
Artigo em Inglês | MEDLINE | ID: mdl-30939785

RESUMO

Herba Epimedii, a commonly used Chinese medicine, has attracted much attention recently because of its potential hepatotoxic effects. 2″-O-Rhamnosyl icariside II, baohuoside I and baohuoside II are the main components of Herba Epimedii, and previous research indicates that these three compounds are related to the hepatotoxicity of Herba Epimedii. To test this idea, in this study, HL-7702 and HepG2 cells were chosen as the in vitro models and the influences of these three compounds on a series of cytotoxicity indices, including ALT, AST, LDH, SOD, GSH, MDA, ROS and MMP, were determined. The results showed that at certain concentrations, the three compounds had different effects on the indices. Among them, baohuoside I at high concentration (32 µg/mL) displayed more significant cytotoxicity than the other two compounds; therefore, it was inferred to be more closely correlated with the liver injury induced by Herba Epimedii combined with the previous study, and its toxic mechanisms may be involved in increasing oxidative stress and inducing apoptosis. The findings of this study may provide evidence of the toxic composition of Herba Epimedii to preliminarily discuss the toxic mechanisms and provide improved guidance for its clinical safety.


Assuntos
Apoptose/efeitos dos fármacos , Carcinoma Hepatocelular/patologia , Epimedium/química , Flavonoides/farmacologia , Glicosídeos/farmacologia , Hepatócitos/patologia , Carcinoma Hepatocelular/tratamento farmacológico , Carcinoma Hepatocelular/metabolismo , Células Cultivadas , Hepatócitos/efeitos dos fármacos , Humanos , Neoplasias Hepáticas/tratamento farmacológico , Neoplasias Hepáticas/metabolismo , Neoplasias Hepáticas/patologia , Fitoterapia , Extratos Vegetais/farmacologia
11.
Biomed Res Int ; 2019: 4860268, 2019.
Artigo em Inglês | MEDLINE | ID: mdl-31032347

RESUMO

Hematological malignancies including leukemia and lymphoma can severely impact human health. With the current therapies combined with chemotherapy, stem cell transplantation, radiotherapy, and immunotherapy, the prognosis of hematologic malignancies improved significantly. However, most hematological malignancies are still incurable. Therefore, research for novel treatment options was continuing with the natural product as one source. Icaritin is a compound extracted from a traditional Chinese herb, Epimedium Genus, and demonstrated an antitumor effect in various neoplasms including hematological malignancies such as leukemia, lymphoma, and multiple myeloma. In hematological malignancies, icaritin showed multiple cytotoxic effects to induce apoptosis, arrest the cell cycle, inhibit proliferation, promote differentiation, restrict metastasis and infiltration, and suppress the oncogenic virus. The proved underlying mechanisms of the cytotoxic effects of icaritin are different in various cell types of hematological malignancies but associated with the critical cell signal pathway, including PI3K/Akt, JAK/STAT3, and MAPK/ERK/JNK. Although the primary target of icaritin is still unspecified, the existing evidence indicates that icaritin is a potential novel therapeutic agent for neoplasms as with hematological malignancies. Here, in the field of hematology, we reviewed the reported activity of icaritin in hematologic malignancies and the underlying mechanisms and recognized icaritin as a candidate for therapy of hematological malignancies.


Assuntos
Produtos Biológicos/uso terapêutico , Epimedium/química , Flavonoides/uso terapêutico , Neoplasias Hematológicas/tratamento farmacológico , Produtos Biológicos/química , Proliferação de Células/efeitos dos fármacos , Flavonoides/química , Humanos , Leucemia/tratamento farmacológico , Linfoma/tratamento farmacológico , Medicina Tradicional Chinesa , Mieloma Múltiplo/tratamento farmacológico
12.
Chem Biol Interact ; 303: 7-13, 2019 Apr 25.
Artigo em Inglês | MEDLINE | ID: mdl-30731080

RESUMO

Exposure to lead (Pb) poses a threat to human bone health, including changes in bone mineral composition and the inhibition of skeletal growth and bone maturation. However, little is known about how Pb directly affects osteoblasts. In this work, we found that sub-toxic Pb concentrations suppressed bone nodule formation and inhibited differentiation in MC3T3-E1 subclone 14 cells, as shown by decreased expression levels of the differentiation markers alkaline phosphatase (ALP), type 1 collagen (COL1), osteocalcin (OC), and runt-related transcription factor 2 (RUNX2). Moreover, Pb inactivated the canonical Wnt pathway by regulating key components, such as Wnt3a, Dkk-1, pGSK3ß, and ß-catenin. Icaritin (ICT), a hydrolytic product of icariin from the genus Epimedium, attenuates the inhibitory effect of Pb on osteoblastic differentiation, as well as activate the canonical Wnt signal pathway. Taken together, the results suggest ICT as a potential bone protectant that may be used to prevent bone damage caused by Pb and can activate the canonical Wnt signal pathway.


Assuntos
Flavonoides/uso terapêutico , Chumbo/toxicidade , Via de Sinalização Wnt/efeitos dos fármacos , Células 3T3 , Animais , Osso e Ossos/patologia , Diferenciação Celular/efeitos dos fármacos , Epimedium/química , Camundongos , Osteoblastos/citologia , Substâncias Protetoras/farmacologia
13.
Molecules ; 24(2)2019 Jan 16.
Artigo em Inglês | MEDLINE | ID: mdl-30654565

RESUMO

In this study, the inhibitory potential of bacterial neuraminidase (NA) was observed on the leaves of Epimedium koreanum Nakai, which is a popular ingredient in traditional herbal medicine. This study attempted to isolate the relevant, responsible metabolites and elucidate their inhibition mechanism. The methanol extraction process yielded eight flavonoids (1⁻8), of which compounds 7 and 8 were new compounds named koreanoside F and koreanoside G, respectively. All the compounds (1⁻8) showed a significant inhibition to bacterial NA with IC50 values of 0.17⁻106.3 µM. In particular, the prenyl group on the flavonoids played a critical role in bacterial NA inhibition. Epimedokoreanin B (compound 1, IC50 = 0.17 µM) with two prenyl groups on C8 and C5' of luteolin was 500 times more effective than luteolin (IC50 = 85.6 µM). A similar trend was observed on compound 2 (IC50 = 0.68 µM) versus dihydrokaempferol (IC50 = 500.4 µM) and compound 3 (IC50 = 12.6 µM) versus apigenin (IC50 = 107.5 µM). Kinetic parameters (Km, Vmax, and Kik/Kiv) evaluated that all the compounds apart from compound 5 showed noncompetitive inhibition. Compound 5 was proven to be a mixed type inhibitor. In an enzyme binding affinity experiment using fluorescence, affinity constants (KSV) were tightly related to inhibitory activities.


Assuntos
Inibidores Enzimáticos/farmacologia , Epimedium/química , Flavonoides/farmacologia , Neuraminidase/antagonistas & inibidores , Proteínas de Bactérias/antagonistas & inibidores , Inibidores Enzimáticos/química , Flavonoides/química , Concentração Inibidora 50 , Estrutura Molecular , Neopreno/química , Extratos Vegetais/química , Extratos Vegetais/farmacologia , Folhas de Planta/química
14.
Neurosci Res ; 145: 46-53, 2019 Aug.
Artigo em Inglês | MEDLINE | ID: mdl-30145270

RESUMO

The radioprotective effect of herb epimedium (or yin yang huo) extract (5 g/kg, oral administration daily for 4 weeks) on neurogenesis and cognition after acute radiation exposure with 5.5 Gy was evaluated in Balb/c mice by behavioral tests and immunohistochemical study. The results indicated that epimedium extract could improve animal weight loss, locomotor activity and spatial learning and memory which are similar to pre-irradiation intraperitoneal injection (100 mg/kg) of amifostine phosphate, a well- known radioprotective drug. Immunohistochemical study showed that epimedium extract prevented the loss of proliferation cells, newly generated neurons, and interneurons in the hilus, in particular, the subgranular zone of the dentate gyrus. It suggests that herb epimedium may be a promising radio-neuro-protective drug to prevent radiation-induced neuropsychological disorders.


Assuntos
Cognição/efeitos dos fármacos , Cognição/efeitos da radiação , Medicamentos de Ervas Chinesas/farmacologia , Neurogênese/efeitos dos fármacos , Neurogênese/efeitos da radiação , Animais , Proliferação de Células/efeitos dos fármacos , Proliferação de Células/efeitos da radiação , Giro Denteado/efeitos dos fármacos , Giro Denteado/efeitos da radiação , Epimedium/química , Interneurônios , Masculino , Memória , Camundongos , Camundongos Endogâmicos BALB C , Aprendizagem Espacial/efeitos dos fármacos , Aprendizagem Espacial/efeitos da radiação , Memória Espacial/efeitos dos fármacos , Memória Espacial/efeitos da radiação
15.
Oncol Rep ; 41(2): 765-778, 2019 Feb.
Artigo em Inglês | MEDLINE | ID: mdl-30431140

RESUMO

Increased production of reactive oxygen species (ROS) is a distinct feature of various types of cancer. ROS drive tumor progression and render cancer cells vulnerable to additional oxidative insult. The various natural herb compounds have been shown to induce additional production of ROS in cancer cells, although the physiological implications of ROS under these conditions are not fully determined. In the present study, icaritin, a natural compound derived from the medicinal plants Epimedium, was demonstrated to potently suppresses the proliferation of human HeLa and SiHa cervical cancer cells, without similar affects on non-cancerous CCD­1095Sk fibroblasts and 293 cells, as measured by MTT and colony formation assays. Icaritin treatment caused a rapid increase in ROS in HeLa and SiHa cells, which was followed by a prominent increase in the number of DNA strand breaks. Consequently, the levels of the pro­apoptotic protein Bax and activated caspase 3 and 9 enzymes were increased, while the levels of the anti­apoptotic proteins Bcl­2 and XIAP were downregulated. These protein expression changes were accompanied by marked induction of apoptosis in icaritin­treated cancer cells. The results suggested that the icaritin­induced ROS overload promoted cancer cell death via induction of extensive oxidative DNA damage, which subsequently resulted in large numbers of DNA strand breaks and the activation of the intrinsic apoptotic pathway.


Assuntos
Apoptose/efeitos dos fármacos , Quebras de DNA/efeitos dos fármacos , Flavonoides/farmacologia , Espécies Reativas de Oxigênio/metabolismo , Neoplasias do Colo do Útero/tratamento farmacológico , Linhagem Celular Tumoral , DNA/efeitos dos fármacos , DNA/metabolismo , Medicamentos de Ervas Chinesas/farmacologia , Medicamentos de Ervas Chinesas/uso terapêutico , Epimedium/química , Feminino , Fibroblastos , Flavonoides/uso terapêutico , Células HEK293 , Células HeLa , Humanos , Estresse Oxidativo/efeitos dos fármacos , Neoplasias do Colo do Útero/patologia
16.
Planta Med ; 85(4): 347-355, 2019 Mar.
Artigo em Inglês | MEDLINE | ID: mdl-30522143

RESUMO

Leaves of the Epimedium plant are traditionally consumed for bone health and other indications. The aim of this study was to establish the safety and pharmacokinetics of the metabolites of prenylflavonoids (icariin, icariside I, icariside II, icaritin, and desmethylicaritin) following single doses of a defined Epimedium prenylflavonoid extract in humans. A single oral dose of 370, 740, or 1110 mg of a standardized Epimedium prenylflavonoid extract was administered to 30 healthy male subjects in a randomized, placebo-controlled trial. Serum samples were collected over a 48-h period and analyzed by liquid chromatography-tandem mass spectrometry and non-compartmental pharmacokinetic modelling. Epimedium prenylflavonoid extracts were well tolerated and no adverse effects were observed. The principle metabolites detected in the serum were icariside II and desmethylicaritin. Icariside II had a T max of between 4.1 - 4.3 h, reaching a maximum AUC0→∞ of 23.0 (17.5, 29.9) h×ng/mL (median [IQR: interquartile range]) with the highest dose of the Epimedium prenylflavonoid. On the other hand, desmethylicaritin had a delayed T max of 24.1 - 24.4 h and reached a maximum AUC0→∞ of 126.1 (62.4, 202.9) h×ng/mL. The median maximum plasma concentration and AUC0→∞ of desmethyliciaritin showed an increase with higher doses of the Epimedium prenylflavonoid (p < 0.05). Icariin, icariside I, and icaritin levels were below detection limits. Levels of Epimedium prenylflavonoid metabolites observed in this study were consistent with levels demonstrated to have anti-osteoporotic effects in cellular and animal studies. Coupled with the favorable safety profile of the extract observed, further studies are required to explore the utility of Epimedium prenylflavonoid extracts to prevent osteoporosis in postmenopausal women.


Assuntos
Epimedium/química , Flavonoides/farmacocinética , Extratos Vegetais/farmacocinética , Folhas de Planta/química , Administração Oral , Adulto , Cromatografia Líquida , Relação Dose-Resposta a Droga , Flavonoides/sangue , Flavonoides/isolamento & purificação , Humanos , Masculino , Extratos Vegetais/administração & dosagem , Extratos Vegetais/sangue , Espectrometria de Massas em Tandem
17.
Nat Prod Res ; 33(13): 1936-1943, 2019 Jul.
Artigo em Inglês | MEDLINE | ID: mdl-29873273

RESUMO

A novel icariin type flavonoid glycoside with a malonaldehydic acid intramolecular ester and two known flavonoid glycosides were isolated from Epimedium pseudowushanense. Their structures were elucidated on the basis of spectroscopic analysis and comparison of their data to the values reported in the literatures. The anti-inflammatory activities of these compounds icariin 3'''-O-malonaldehydic acid intramolecular 1'''', 2''' ester (1), icariin (2) and epimedin C (3) were tested. The results indicated that compounds 1, 2 and 3 showed maximal inhibitory ratio of 27.91, 44.80 and 46.61%, respectively in in vitro anti-inflammatory activity on LPS-induced TNF-α secretion in RAW264.7 cells. Compounds icariin (2) and epimedin C (3) were found to inhibit the secretion of TNF-α to a comparable degree as quercetin.


Assuntos
Epimedium/química , Flavonoides/química , Flavonoides/farmacologia , Animais , Anti-Inflamatórios não Esteroides/química , Anti-Inflamatórios não Esteroides/farmacologia , Avaliação Pré-Clínica de Medicamentos/métodos , Flavonoides/isolamento & purificação , Lipopolissacarídeos/toxicidade , Camundongos , Estrutura Molecular , Células RAW 264.7 , Fator de Necrose Tumoral alfa/metabolismo
18.
BMC Complement Altern Med ; 18(1): 303, 2018 Nov 13.
Artigo em Inglês | MEDLINE | ID: mdl-30424767

RESUMO

BACKGROUND: Epimedium sagittatum (Sieb.et Zucc.) Maxim., Ying-Yang-Huo in Chinese has been used as a traditional Chinese medicine and is deemed to "reinforce the kidney Yang". Previous studies showed that E. sagittatum could modulate the immune system and treat some chronic disease such as rheumatic arthritis, cardiovascular diseases and osteoporosis. The aim of this study is to evaluate the anti-inflammatory effects of ethyl acetate extracts (YYHs) of E. sagittatum and its mechanisms of action. METHODS: In order to explore the composition of YYHs, YYHs was analyzed using high performance liquid chromatography-mass spectrometry-mass spectrometry (HPLC-MS/MS) and in comparison with reference standards. Anti-inflammatory model was established in LPS-induced RAW264.7 cells. The levels of nitric oxide (NO) were measured with the Griess reagent. Production of tumor necrosis factor-alpha (TNF-α) and interleukin-2 (IL-2) were measured by enzyme-linked immunosorbent assays (ELISA). In addition, expression of p-p65 protein and TLR4/MD-2 complex was detected by western blots and flow cytometric, respectively. Nuclear factor kappa B (NF-κB) nuclear translocation was observed by fluorescence microscope. RESULTS: A total of eight compounds were identified, of which icariside II was the most abundant compound. YYHs (12.5-50 µg/mL) had no obvious cytotoxic effect on cells, and remarkably inhibited LPS-induced production of NO, TNF-α and IL-2 with a dose-dependent manner. Additionally, YYHs up-regulated expression of p-p65 and TLR4/MD-2 complex. Further research showed that YYHs significantly suppressed NF-κB p65 nuclear translocation. CONCLUSION: In brief, YYHs contributed to the inhibition of LPS-induced inflammatory response through the TLR4/MD-2-mediated NF-κB pathway and may be a potential choice to combat inflammation diseases. It includes a schema of pathways at the end of the paper.


Assuntos
Medicamentos de Ervas Chinesas/farmacologia , Epimedium/química , Antígeno 96 de Linfócito/metabolismo , NF-kappa B/metabolismo , Transdução de Sinais/efeitos dos fármacos , Receptor 4 Toll-Like/metabolismo , Animais , Anti-Inflamatórios/farmacologia , Lipopolissacarídeos , Camundongos , Fosforilação/efeitos dos fármacos , Células RAW 264.7
19.
Zhongguo Zhong Yao Za Zhi ; 43(17): 3444-3450, 2018 Sep.
Artigo em Chinês | MEDLINE | ID: mdl-30347910

RESUMO

Epimedii Folium, a famous traditional Chinese medicine made of dried leaves of Epimedium brevicomu, E. pubescens, E. sagittatum or E. koreanum, has been applied in China for several thousand years as a medicine. It has the function of reinforcing kidney Yang, strengthening muscles and bones and dispelling rheumatism. Modern studies have shown that baohuoside Ⅰ has a low content in Herba Epimedii, but it has a wide range of pharmacological effects, such as anti-osteoporosis, anti-tumor, improving cognitive dysfunction, cerebral ischemia-reperfusion injury protection, and neuroprotection. More and more attention has been paid to the preparation methods and pharmacological effects of baohuoside Ⅰ due to its many biological activities and pharmacological effects. In this present research, in order to provide references for the better mass preparation and rational exploitation of baohuoside Ⅰ, we summarized and sorted out the preparation methods and pharmacological effects of baohuoside Ⅰ which were published in recent years.


Assuntos
Epimedium/química , Flavonoides/farmacologia , China , Humanos , Folhas de Planta/química
20.
J Pharmacol Sci ; 138(1): 38-45, 2018 Sep.
Artigo em Inglês | MEDLINE | ID: mdl-30241784

RESUMO

Icariside II (ICA II), a flavonoid derived from Epimediumbrevicormum Maxin in, has multiple biological activities in Chinese traditional medicine. Our study aimed to investigate the potential activity of ICA II against cardiac remodeling and the underlying mechanism. Mice received aorta banding (AB) or sham surgery, and then were randomly divided into ICA II or vehicle (veh) group for 6 weeks. After echocardiography and pressure-volume loop examination, hearts were harvested for histopathological analysis and molecular mechanism investigation. Additionally, neonatal rat cardiomyocytes (NRCM) were used for in vitro experiments. ICA II attenuated the systolic and diastolic cardiac dysfunction, and protected mouse heart from hypertrophy and fibrosis. The underlying mechanism might involve in the regulation of Akt, AMPKα and mTORC. In in vitro experiment, ICA II prevented phenylephrine (PE) induced NRCM hypertrophy by regulating AMPKα/mTORC pathway. This protective effect was disappeared after treatment with Compound C (CpC), an AMPKα inhibitor. Moreover, ICA II activated AMPK at baseline. ICAII was superior to resveratrol in activating AMPKα and similar to AICAR. ICA II protected against cardiac remodeling and NRCM hypertrophy by regulating AMPK/mTORC pathway. ICA II may be a candidate for the treatment of malignant cardiac remodeling.


Assuntos
Proteínas Quinases Ativadas por AMP/metabolismo , Flavonoides/farmacologia , Alvo Mecanístico do Complexo 1 de Rapamicina/metabolismo , Miócitos Cardíacos/patologia , Remodelação Ventricular/efeitos dos fármacos , Remodelação Ventricular/genética , Animais , Cardiomegalia/prevenção & controle , Epimedium/química , Flavonoides/isolamento & purificação , Hipertrofia/prevenção & controle , Fenilefrina/efeitos adversos , Ratos Sprague-Dawley , Transdução de Sinais/genética , Transdução de Sinais/fisiologia
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