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1.
J Ethnopharmacol ; 264: 113212, 2021 Jan 10.
Artigo em Inglês | MEDLINE | ID: mdl-32768643

RESUMO

ETHNOPHARMACOLOGICAL RELEVANCE: Cerebral ischemia-reperfusion (CIR) injury is one of the main diseases leading to death and disability. Acanthopanax senticosus (Rupr. & Maxim.) Harms (AS), also known as Panax ginseng, has neuroprotective effects on anti-CIR injury. However, the underlying molecular mechanism of its therapeutic effects is not clear. AIM OF THE STUDY: To systematically study and explore the mechanism of Acanthopanax senticosus (Rupr. & Maxim.) Harms extract (ASE) in the treatment of CIR injury based on metabolomics and transcriptomics. MATERIALS AND METHODS: The pharmacological basis of ASE in the treatment of CIR was evaluated, and samples were used in plasma metabolomics and brain tissue transcriptomics to reveal potential biomarkers. Finally, according to online database, we analyzed biomarkers identified by the two technologies, explained reasons for the therapeutic effect of ASE, and identify therapeutic targets. RESULTS: A total of 53 differential metabolites (DMs) were identified in plasma and 3138 differentially expressed genes (DEGs) were identified in brain tissue from three groups of rats, including sham, ischemia-reperfusion (I/R), and ASE groups. Enrichment analysis showed that Nme6, Tk1, and Pold1 that are involved in the production of deoxycytidine and thymine were significantly up-regulated and Dck was significantly down-regulated by the intervention with ASE. These findings indicated that ASE participates in the pyrimidine metabolism by significantly regulating the balance between dCTP and dTTP. In addition, ASE repaired and promoted the lipid metabolism in rats, which might be due to the significant expression of Dgkz, Chat, and Gpcpd1. CONCLUSIONS: The findings of this study suggest that ASE regulates the significant changes in gene expression in metabolites pyrimidine, and lipid metabolism in CIR rats and plays an active role in the treatment of CIR injury through multiple targets and pathways.

2.
Food Funct ; 11(8): 7104-7114, 2020 Aug 01.
Artigo em Inglês | MEDLINE | ID: mdl-32744543

RESUMO

A water-soluble neutral homopolysaccharide (PLP-1) was obtained from the roots of Pueraria lobata by DEAE cellulose and Sephadex G-200 gel chromatography purification. The average molecular weight of PLP-1 was 16.2 kDa. Monosaccharide composition analysis showed that PLP-1 was composed of glucose as a glucan. The structure of PLP-1 was characterized on the basis of extensive physical and chemical analysis, which indicated that the backbone of PLP-1 was mainly composed of →3)-α-d-Glcp(1→ and →4)-ß-d-Glcp(1→ with a molar ratio of 7.0 : 1.0. Moreover, the hypoglycemic activity of PLP-1 was investigated by palmitic acid and high glucose induced insulin resistant HepG2 cells. The results elucidated that PLP-1 could decrease the glucose concentration by up-regulating the expression of PI3K and AKT, and down-regulating the expression of FoxO1, PCK2, and G6Pase in insulin resistant cells. Therefore, PLP-1 could serve as a dietary supplement to ameliorate insulin resistance for diabetic patients.

3.
Chin J Nat Med ; 18(7): 508-516, 2020 Jul.
Artigo em Inglês | MEDLINE | ID: mdl-32616191

RESUMO

Lung cancer is the leading cause of cancer death and the most common malignant tumor, the long-term survival of which has stagnated in the past several decades. Pileostegia tomentella Hand. Mazz is a traditional Chinese medicine called "Zhongliuteng" (ZLT) in the pharmacopeia, which has been proved to possess a potent anti-tumor effect on various cancers. In this study, the effects of ZLT N-butanol extraction (ZLTN) and ZLT ethyl acetate extraction (ZLTE) on the viability of non-small cell lung cancer cell (NSCLC) lines H1299 and A549 were evaluated. Here, we firstly reported that ZLTE significantly inhibited H1299 cells growth without affecting the release of lactate dehydrogenase (LDH). In addition, ZLTE induced caspase-dependent apoptosis in a concentration-dependent manner and increased the expression cleaved-PARP and decreased pro-caspase-3, pro-caspase-7, pro-caspase-8, and pro-caspase-9. Moreover, ZLTE increased the level of cellular reactive oxygen species (ROS) in H1299 cells to lead to apoptosis, which was reversed by N-acetyl-cysteine (NAC). Taken together, our results revealed that ZLTE induced caspase-dependent apoptosis via ROS generation, suggesting that ZLTE is a promising herbal medicine for the treatment of NSCLC.

5.
J Asian Nat Prod Res ; 22(4): 303-315, 2020 Apr.
Artigo em Inglês | MEDLINE | ID: mdl-30843729

RESUMO

Three new saponins (1-3), a new natural product (4) and six other known compounds (5-10) were isolated from the whole Reineckia carnea plant. Their structures were established by comparison of their NMR spectra and MS data with literature data. In addition, all the isolated compounds were evaluated in vitro for anti-inflammatory activities against LPS-stimulated nitric oxide (NO) production in RAW 264.7 macrophages. Compounds 1-4 exhibited anti-inflammatory activities with IC50 values of 37.5 µM, 31.4 µM, 34.6 µM, and 56.1 µM, respectively. Furthermore, compounds 5-10 showed anti-inflammatory activities with IC50 values ranging from 20.3 to 42.9 µM.


Assuntos
Anti-Inflamatórios , Saponinas , Lipopolissacarídeos , Macrófagos , Estrutura Molecular , Óxido Nítrico , Extratos Vegetais
6.
J Nat Prod ; 82(11): 3065-3073, 2019 11 22.
Artigo em Inglês | MEDLINE | ID: mdl-31718182

RESUMO

Natural triterpenoids, such as oleanolic acid (OA) and hederagenin, display anti-lung cancer effects, and nitric oxide (NO) is associated with some oncogenic signaling pathways. Accordingly, 17 OA/hederagenin-NO donor hybrids were designed, synthesized, and evaluated against tumor cells. The most potent compound, 13, significantly inhibited the proliferation of five tumor cell lines (IC50 4.6-5.2 µM), while hederagenin inhibited the growth of only A549 tumor cells (IC50 > 10 µM). Furthermore, compound 13 showed stronger inhibitory effects on EGFR-LTC kinase activity (IC50 0.01 µM) than hederagenin (IC50 > 20 µM) and inhibited the proliferation of gefitinib-resistant H1975 (IC50 8.1 µM) and osimertinib-resistant H1975-LTC (IC50 7.6 µM) non-small-cell lung cancer (NSCLC) cells. Moreover, compound 13 produced the most NO in H1975 tumor cells, which indicated that NO may play a synergistic role. Collectively, compound 13, a novel hederagenin-NO donor hybrid with a different chemical structure from those of the current FDA-approved EGFR-targeted anti-NSCLC drugs, may be a promising lead compound for the treatment of NSCLC expressing gefitinib-resistant EGFR with a T790 M mutation or osimertinib-resistant EGFR-LTC with an L858R/T790M/C797S mutation. This work should shed light on the discovery of new anti-NSCLC drugs targeting EGFR from natural products.

7.
Artigo em Inglês | MEDLINE | ID: mdl-31275420

RESUMO

Anemoside B4 (B4) isolated from Radix Pulsatilla has anti-inflammatory activities in the colon and antitumor effects. However, its role in the prevention and treatment of kidney injury has not been reported. Here, we reported the effects of B4 on chronic kidney injury (CKI) and studied its related mechanism based on an adenine-induced kidney injury model in rats. The results showed that serum BUN (blood urea nitrogen), Crea (creatinine), and urinary proteins increased significantly after oral administration of adenine. Meanwhile, the adenine contents in both renal tissue and urine increased markedly compared with those of normal rats. Moreover, IL-1ß, IL-6, TNFα, and NFκB expression was upregulated in the kidney. Simultaneously, the expression of NLRP3 (the nucleotide-binding and oligomerization domain-like receptor, leucine-rich repeat and pyrin domain-containing 3) in the inflammasome, which consists of Caspase 1, ASC (apoptosis-associated speck-like protein containing a caspase recruitment domain), and IL-18, was significantly upregulated. B4 could significantly decrease BUN and Crea; reduce urinary proteins in rats; suppress the expression of IL-6, IL-1ß, NFκB, NLRP3, Caspase 1, ASC, and IL-18; and increase urinary adenine contents and promote its excretion. In addition, B4 also upregulated the expression of podocin and nephrin, two major podocyte proteins, and reduced the fiber collagen in the renal interstitial, suggesting that B4 could protect the glomerular matrix from adenine injury in addition to its anti-inflammatory effects. The results of this study show new perspective of B4 as a potential drug against adenine-induced renal injury.

8.
Biosci Biotechnol Biochem ; 83(11): 2016-2026, 2019 Nov.
Artigo em Inglês | MEDLINE | ID: mdl-31272310

RESUMO

Exposure of PC12 cells to 10 mM glutamate caused significant viability loss, cell apoptosis, decreased activities of superoxide dismutase (SOD) and glutathione peroxidase (GSH-Px) as well as increased levels of malondialdehyde (MDA). In parallel, glutamate significantly increased the intracellular levels of ROS and intracellular calcium. However, pretreatment of the cells with acteoside and isoacteoside significantly suppressed glutamate-induced cellular events. Moreover, acteoside and isoacteoside reduced the glutamate-induced increase of caspase-3 activity and also ameliorated the glutamate-induced Bcl-2/Bax ratio reduction in PC12 cells. Furthermore, acteoside and isoacteoside significantly inhibited glutamate-induced DNA damage. In the mouse model, acteoside significantly attenuated cognitive deficits in the Y maze test and attenuated neuronal damage of the hippocampal CA1 regions induced by glutamate. These data indicated that acteoside and isoacteoside play neuroprotective effects through anti-oxidative stress, anti-apoptosis, and maintenance of steady intracellular calcium.


Assuntos
Antioxidantes/química , Antioxidantes/farmacologia , Ácido Glutâmico/toxicidade , Glicosídeos/química , Glicosídeos/farmacologia , Neurotoxinas/toxicidade , Álcool Feniletílico/química , Animais , Apoptose/efeitos dos fármacos , Cálcio/metabolismo , Sobrevivência Celular/efeitos dos fármacos , Hipocampo/citologia , Hipocampo/efeitos dos fármacos , Hipocampo/fisiologia , Espaço Intracelular/efeitos dos fármacos , Espaço Intracelular/metabolismo , Malondialdeído/metabolismo , Memória/efeitos dos fármacos , Fármacos Neuroprotetores/química , Fármacos Neuroprotetores/farmacologia , Células PC12 , Ratos , Espécies Reativas de Oxigênio/metabolismo
11.
Pharmacol Res ; 142: 102-114, 2019 04.
Artigo em Inglês | MEDLINE | ID: mdl-30794925

RESUMO

Dihydrotanshinone (DHT), one of the major ingredients of Salvia miltiorrhiza Bunge (Danshen), displays many bioactivities. However, the activity and underlying mechanism of DHT in anti-inflammation have not yet been elucidated. In this study, we investigated the anti-inflammatory activity and molecular mechanism of action of DHT both in vitro and in vivo. Our data showed that DHT significantly decreased the release of inflammatory cytokines tumor necrosis factor-α (TNF-α), interleukin-6 (IL-6), and IL-1ß in lipopolysaccharide (LPS)-stimulated RAW264.7 cells, THP-1 cells, and bone marrow-derived macrophages (BMDMs), and altered the expression of cyclooxygenase-2 (COX-2) and inducible nitric oxide synthase (iNOS). In addition, flow cytometry results indicated that DHT reduced the calcium influx, and generation of reactive oxygen species (ROS), and nitric oxide (NO) generation in LPS-stimulated RAW264.7 cells. Moreover, DHT suppressed the transcription of nuclear factor-κB (NF-κB), the expressions of NF-κB proteins, and nuclear translocation of NF-κB/p65, thereby suggesting that the NF-κB pathway played a role in the anti-inflammatory action of DHT. In addition, DHT attenuated LPS-challenged activator protein-1 (AP-1) activity, resulting from interference of the mitogen-activated protein kinase (MAPK) pathway. The molecular docking simulation of DHT to toll-like receptor 4 (TLR4) suggested that DHT binds to the active sites of TLR4 to block TLR4 dimerization, which was further corroborated by cellular thermal shift assay and co-immunoprecipitation (Co-IP) experiments. Furthermore, the recruitment of myeloid differentiation primary response gene 88 (MyD88) and the expression of transforming growth factor-b (TGF-b)-activated kinase 1 (p-TAK1) were disturbed by the inhibition of TLR4 dimerization. Thus, investigating the molecular mechanism of DHT indicated that TLR4-MyD88-NF-κB/MAPK signaling cascades were involved in the anti-inflammatory activity of DHT in vitro. In in vivo mouse models, DHT significantly ameliorated LPS-challenged acute kidney injury, inhibited dimethylbenzene-induced mouse ear oedema, and rescued LPS-induced sepsis in mice. Taken together, our results indicated that DHT exhibited significant anti-inflammatory activity both in vitro and in vivo, suggesting that DHT may be a potential therapeutic agent for inflammatory diseases.


Assuntos
Anti-Inflamatórios/farmacologia , Fenantrenos/farmacologia , Receptor 4 Toll-Like/metabolismo , Lesão Renal Aguda/induzido quimicamente , Lesão Renal Aguda/tratamento farmacológico , Animais , Anti-Inflamatórios/uso terapêutico , Citocinas/genética , Citocinas/metabolismo , Dimerização , Edema/induzido quimicamente , Edema/tratamento farmacológico , Células HEK293 , Humanos , Lipopolissacarídeos , Masculino , Camundongos , Camundongos Endogâmicos BALB C , Proteínas Quinases Ativadas por Mitógeno/metabolismo , NF-kappa B/metabolismo , Fenantrenos/uso terapêutico , Células RAW 264.7 , Sepse/induzido quimicamente , Sepse/tratamento farmacológico , Células THP-1 , Xilenos
12.
J Pharm Biomed Anal ; 165: 213-223, 2019 Feb 20.
Artigo em Inglês | MEDLINE | ID: mdl-30553111

RESUMO

TongFengTangSan (TFTS), a traditional Tibetan medicine comprising of Tinospora sinensis (TS), Terminalia chebula Retz (TC) and Trogopterori faeces (TF), is used to treat joint diseases like gout, gout arthritis, swelling, pain etc. Despite the significant therapeutic effects of TFTS, its pharmacological components have not been analyzed so far. Therefore, the chemical composition of the effective part of TFTS was analyzed by ultra-high-performance liquid chromatography coupled with quadrupole time-of-flight mass spectrometry (UHPLC-Q-TOF-MS/MS). The results show that the ethanol extract (EE) of TFTS was more effective in reducing the serum uric acid (SUA) and XOD (Serum and Liver) levels in a hyperuricemic rats model compared to the TFTS raw powder (RP). UHPLC-Q-TOF-MS/MS identified a total of 106 compounds in the positive and negative ion mode, of which 87 were from TC, 13 from TS and 6 from TF. In addition, 106 compounds contained 57 tannins, 6 triterpenoids, 10 alkaloids, 7 flavonoids, 22 organic acids and 4 phenylpropanoids. The preliminary results indicate that the EE of TFTS includes the active anti hyperuricemic substances. The present study first investigated the efficacy and the active components of TFTS in hyperuricemic treatment, and further summarized the diagnostic ion and neutral loss patterns of MS/MS cracking of tannic compounds. These findings lay the foundation for the further study and clinical application of TFTS.


Assuntos
Cromatografia Líquida de Alta Pressão/métodos , Hiperuricemia/tratamento farmacológico , Medicina Tradicional Tibetana/métodos , Espectrometria de Massas em Tandem/métodos , Animais , Etanol/química , Masculino , Materia Medica/análise , Materia Medica/química , Materia Medica/farmacologia , Ratos , Ratos Sprague-Dawley , Terminalia/química , Tinospora/química , Ácido Úrico/sangue
13.
Mol Brain ; 12(1): 118, 2019 12 30.
Artigo em Inglês | MEDLINE | ID: mdl-31888678

RESUMO

Chronic corticosterone (CORT) stress is an anxiety and depression inducing factor that involves the dysfunction of glucocorticoid receptor (GR), brain-derived neurotrophic factor (BDNF), and neuronal plasticity. However, the regulation of proteomic profiles in neurons suffering CORT stress is remaining elusive. Thus, the proteomic profiles of mouse neuronal C17.2 stem cells were comprehensively investigated by TMT (tandem mass tag)-labeling quantitative proteomics. The quantitative proteomics conjugated gene ontology analysis revealed the inhibitory effect of CORT on the expression of mitochondrial oxidative phosphorylation-related proteins, which can be antagonized by berberine (BBR) treatment. In addition, animal studies showed that changes in mitochondria by CORT can affect neuropsychiatric activities and disturb the physiological functions of neurons via disordering mitochondrial oxidative phosphorylation. Thus, the mitochondrial energy metabolism can be considered as one of the major mechanism underlying CORT-mediated depression. Since CORT is important for depression after traumatic stress disorder, our study will shed light on the prevention and treatment of depression as well as posttraumatic stress disorder (PTSD).


Assuntos
Comportamento Animal , Berberina/farmacologia , Depressão/metabolismo , Neurônios/metabolismo , Fosforilação Oxidativa/efeitos dos fármacos , Proteômica , Animais , Berberina/administração & dosagem , Sobrevivência Celular/efeitos dos fármacos , Corticosterona/administração & dosagem , Depressão/genética , Depressão/patologia , Modelos Animais de Doenças , Regulação para Baixo/efeitos dos fármacos , Regulação da Expressão Gênica/efeitos dos fármacos , Masculino , Camundongos Endogâmicos C57BL , Mitocôndrias/efeitos dos fármacos , Mitocôndrias/metabolismo , Neurônios/efeitos dos fármacos , RNA Mensageiro/genética , RNA Mensageiro/metabolismo , Reprodutibilidade dos Testes , Regulação para Cima/efeitos dos fármacos
14.
Zhongguo Zhong Yao Za Zhi ; 43(21): 4182-4191, 2018 Nov.
Artigo em Chinês | MEDLINE | ID: mdl-30583615

RESUMO

Internal environment of metabolism of traditional Chinese medicine (TCM) is a dynamic process, which is in line with the "holistic-dynamic-comprehensive-analytic" characteristics of metabonomics, therefore metabonomics have a unique advantage to reveal the metabolic pattern of TCM. The application of metabonomics in TCM has great practical significance in understanding the pharmacodynamic/toxic effect material basis, mechanisms and guiding for determination of dosage and treatment course; At the same time, the scientific compatibility of TCM prescription, the germplasm resources of TCM and the preclinical safety/toxicity can be widely researched. At present, metabolomics has become a leading technology in many industries and fields including the research and development of TCM. The core of metabolomics is analytical technology, because comprehensive metabolite profiles or accurate identification of known metabolites can be obtained from complex biological samples only by appropriate analytical techniques. At the same time, a series of bioinformatics/chemical informatics/stoichiometry methods are needed to process the data, so as to obtain the potential law and information in the mass data. In this paper, the concept of metabolomics, relevant analytical techniques, data processing methods and applications were explained and analyzed clearly. In addition, the core problems and countermeasures of metabolomics were summarized, and the future development of metabolomics was prospected as well.


Assuntos
Medicina Tradicional Chinesa , Metabolômica , Pesquisa/tendências , Biologia Computacional , Humanos
15.
Zhongguo Zhong Yao Za Zhi ; 43(21): 4330-4338, 2018 Nov.
Artigo em Chinês | MEDLINE | ID: mdl-30583637

RESUMO

Scopolin (SC-1), scopoletin (SC-2) and isofraxidin (IS-1) are the main active constituents in Chimonanthi Radix. However, the in vivo metabolism of SC-1, SC-2 and IS-1 have not been comprehensively clarified. In this study, the in vivo metabolic profiles of these three coumarins in the rat plasma, urine and feces were analyzed. Ultra-high performance liquid chromatography-quadrupole time of flight mass spectrometry (UHPLC-QTOF-MS/MS) method was applied to characterize the prototypes and metabolites of SC-1, SC-2 and IS-1 in rat feces, urine, and plasma after intravenous administration. A total of 11 metabolites of the three parent compounds were tentatively identified. The main metabolic pathways were analyzed by identification of metabolites, and it was found that these three coumarins underwent multiple in vivo metabolic reactions including glucuronidation, sulfonation, isomerism and reduction. In this study, the analysis of metabolites of three coumarins basically demonstrated their in vivo metabolic process, providing basis for the further pharmacokinetics and pharmacological evaluations of SC-1, SC-2 and IS-1.


Assuntos
Calycanthaceae/química , Cumarínicos/metabolismo , Medicamentos de Ervas Chinesas/metabolismo , Animais , Cromatografia Líquida de Alta Pressão , Cumarínicos/farmacocinética , Medicamentos de Ervas Chinesas/farmacocinética , Ratos , Espectrometria de Massas em Tandem
16.
J Neurol ; 265(12): 2825-2833, 2018 Dec.
Artigo em Inglês | MEDLINE | ID: mdl-30255336

RESUMO

BACKGROUND: Little is known about ping-pong gaze (PPG) outside of individual case reports. We aimed to describe PPG through an observational study and literature review. METHODS: Consecutive patients with PPG at Shanghai General Hospital (SGH) from February 2016 to March 2018 were enrolled. A literature review through March 2018 was conducted. RESULTS: Of the 14 patients with PPG in SGH, the median age was 60 years and 12 were males. The median Glasgow coma scale score was 7.5. The cycle of the PPG ranged from 1.5 to 6.5 s. The leading three etiologies were acute ischemic stroke in five patients, post-seizure state in three patients, and hypoxic-ischemic encephalopathy in two patients. A total of 88.9% (8/9) of the patients with consistent whole-field PPG had similar bilateral hemispheric damage, whereas 80.0% (4/5) of the patients with PPG in the hemifield had unilateral or extremely asymmetric bilateral hemispheric damage. The hemifiled side was the same side as the sole/dominant hemispheric lesion. The final clinical outcomes were neurologic remission for seven patients, vegetative state for one patient, and death for six patients. CONCLUSIONS: PPG is a sign with localizing value that suggests hemispheric damage and asymmetric PPG might help to predict lateralization of the lesions. Acute ischemic stroke is the most common cause of PPG. Etiology and initial outcome are likely important prognostic factors of PPG.


Assuntos
Nistagmo Patológico , Adulto , Idoso , Idoso de 80 Anos ou mais , Encéfalo/diagnóstico por imagem , Medições dos Movimentos Oculares , Feminino , Humanos , Masculino , Pessoa de Meia-Idade , Nistagmo Patológico/diagnóstico por imagem , Nistagmo Patológico/etiologia , Nistagmo Patológico/fisiopatologia , Literatura de Revisão como Assunto
17.
J Org Chem ; 83(16): 9201-9209, 2018 08 17.
Artigo em Inglês | MEDLINE | ID: mdl-29961318

RESUMO

A novel palladium-catalyzed oxidative three-component coupling of easily accessible N-substituted anthranilamides with isocyanides and arylboronic acids is achieved. This protocol offers an alternative approach toward 2,3-disubstituted quinazolinones with a wide substrate scope and good functional group tolerance.

18.
Molecules ; 23(3)2018 Feb 28.
Artigo em Inglês | MEDLINE | ID: mdl-29495641

RESUMO

Ziyuglycoside I (ZGS1) is a promising drug candidate for the treatment of leucopenia. Currently, information on ZGS1 and its in vivo metabolite ziyuglycoside II (ZGS2) is limited. The objective of this study was to investigate the pharmacokinetics, tissue distribution, and excretion of ziyuglycoside I (ZGS1) and its metabolite ziyuglycoside II (ZGS2) in rats. In our study, a simple and sensitive high-performance liquid chromatography-mass spectrometry (HPLC-MS/MS) method was established for simultaneous determination of ZGS1 and its metabolite for Sprague-Dawley rat pharmacokinetics studies. The method was validated following internationally-approved guidelines. The results presented in this study indicated that subcutaneous administration of ZGS1 prolonged its extension time and increased the area under the curve (AUC0-t) of ZGS2 during 0 to t minutes. In summary, in this study, the pharmacokinetic characteristics of ZGS1 and its metabolite ZGS2 were defined and its tissue distribution, and excretion in rats were described. Our finding may be beneficial for leucopenia drug that focus on ZGS1.


Assuntos
Cromatografia Líquida de Alta Pressão , Saponinas/farmacocinética , Espectrometria de Massas em Tandem , Animais , Estrutura Molecular , Ratos , Reprodutibilidade dos Testes , Sensibilidade e Especificidade , Análise Espectral , Distribuição Tecidual
19.
J Asian Nat Prod Res ; 20(8): 793-806, 2018 Aug.
Artigo em Inglês | MEDLINE | ID: mdl-28679317

RESUMO

Camellia oleifera C. Abel has been widely cultivated in China, and a group of bioactive constituents such as triterpeniod saponin have been isolated from C. oleifera C. Abel. In the current study, a new triterpeniod saponin was isolated from the EtOH extract of the roots of C. oleifera C. Abel, named as oleiferoside W, and the cytotoxic properties of oleiferoside W were evaluated in non-small cell lung cancer A549 cells. At the same time the inducing apoptosis, the depolarization of mitochondrial membrane potential (Δψ), the up-regulation of related pro-apoptotic proteins, such as cleaved-PARP, cleaved-caspase-3, and the down-regulation of anti-apoptotic marker Bcl-2/Bax were measured on oleiferoside W. Furthermore, the function, inducing the generation of reactive oxygen species (ROS) and apoptosis, of oleiferoside W could be reversed by N-acetylcysteine (NAC). In conclusion, our findings showed that oleiferoside W induced apoptosis involving mitochondrial pathway and increasing intracellular ROS production in the A549 cells, suggesting that oleiferoside W may have the possibility to be a useful anticancer agent for therapy in lung cancer.


Assuntos
Antineoplásicos Fitogênicos/farmacologia , Apoptose/efeitos dos fármacos , Camellia/química , Pontos de Checagem do Ciclo Celular/efeitos dos fármacos , Raízes de Plantas/química , Saponinas/farmacologia , Triterpenos/farmacologia , Células A549 , Antineoplásicos Fitogênicos/administração & dosagem , Antineoplásicos Fitogênicos/química , Relação Dose-Resposta a Droga , Humanos , Estrutura Molecular , Espécies Reativas de Oxigênio , Saponinas/administração & dosagem , Saponinas/química , Triterpenos/administração & dosagem , Triterpenos/química
20.
Zhongguo Zhong Yao Za Zhi ; 42(21): 4165-4171, 2017 Nov.
Artigo em Chinês | MEDLINE | ID: mdl-29271156

RESUMO

A rapid and accurate method of UFLC-Q-TOF-MS/MS combined with multivariate statistical analysis was established for the identification of Ainsliaea fragrans from different origins in this study. The A. fragrans from different producing areas of Jiangxi, Yunnan, Henan and Jiangsu were determined by UFLC-Q-TOF-MS/MS in the negative ion mode. And the data of the study were analyzed by the Markerview and other software for the PCA and OPLS-DA cluster analysis as well as t test. The results of the principal component analysis(PCA)showed that the main components from different origins were well distinguished. And the results of multivariate statistical showed the differences and similarities between different producing areas. Besides, 40 different compounds were identified in the negative ion mode. This method for identifying A. fragrans from different producing areas has the advantages of rapid accuracy and simplicity, which laid the foundation for the evaluation of the quality of the A. fragrans.


Assuntos
Asteraceae/química , Medicamentos de Ervas Chinesas/química , China , Cromatografia Líquida de Alta Pressão , Compostos Fitoquímicos/análise , Análise de Componente Principal , Espectrometria de Massas em Tandem
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