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1.
Bioorg Chem ; 149: 107487, 2024 Aug.
Artigo em Inglês | MEDLINE | ID: mdl-38805910

RESUMO

The peel of Trichosanthes kirilowii Maxim, is considered one of the primary sources for Trichosanthis pericarpium in traditional Chinese medicine, exhibiting lipid-lowering properties. The impact on hyperlipidemia mice of the crude polysaccharide from the peel of T. Kirilowii (TRP) was investigated in this study. The findings revealed that TRP exhibited a significant improvement in hepatic lipid deposition. Moreover, it significantly decreased serum levels of TC, TG, and LDL-C, while concurrently increasing HDL-C. 16S rRNA amplicon sequencing technique revealed that TRP group exhibited an increased relative abundance of Actinobacteria, a down-regulated relative abundance of Ruminiclostridium, and an up-regulated relative abundance of Ileibacterium. Therefore, TRP might play a role in anti-hyperlipidemia through regulation of the intestinal milieu and enhancement of microbial equilibrium. Consequently, targeted fractionation of TRP resulted in the isolation of a homogeneous acidic polysaccharide termed TRP-1. The TRP-1 polysaccharide, with an average molecular weight of 1.00 × 104 Da, and was primarily composed of Rha, GlcA, GalA, Glc, Gal and Ara. TRP-1 possessed a backbone consisting of alternating connections between â†’ 6)-α-Galp-(1 â†’ 4)-α-Rhap-(1 â†’ 6)-α-Galp-(2 â†’ 6)-ß-Galp-(1 â†’ 6)-α-Galp-(2 â†’ 6)-ß-Galp-(1 â†’ units and branched chain containing â†’ 6)-α-Glcp-(1→, 2,4)-ß-Glcp-(1, and â†’ 4)-α-GlapA-(1→. Both TRP and TRP-1 exhibited significant disruption of cholesterol micelles, highlighting their potential as lipid-lowering agents that effectively inhibit cholesterol absorption pathways.


Assuntos
Colesterol , Microbioma Gastrointestinal , Hiperlipidemias , Polissacarídeos , Trichosanthes , Animais , Microbioma Gastrointestinal/efeitos dos fármacos , Trichosanthes/química , Camundongos , Hiperlipidemias/tratamento farmacológico , Polissacarídeos/farmacologia , Polissacarídeos/química , Polissacarídeos/isolamento & purificação , Colesterol/metabolismo , Colesterol/sangue , Hipolipemiantes/farmacologia , Hipolipemiantes/química , Hipolipemiantes/isolamento & purificação , Masculino , Estrutura Molecular , Relação Estrutura-Atividade , Relação Dose-Resposta a Droga
2.
Zhongguo Zhong Yao Za Zhi ; 48(23): 6396-6402, 2023 Dec.
Artigo em Chinês | MEDLINE | ID: mdl-38211996

RESUMO

A quantitative proton nuclear magnetic resonance(qHNMR) method was established to determine the glucose content in commercially available Massa Medicata Fermentata(MMF) products and explore the variations of glucose content in MMF products during processing. The qHNMR spectrum of MMF in deuterium oxide was obtained with 2,2,3,3-d_4-3-(trimethylsilyl) propionate sodium salt as the internal standard substance. With the doublet peaks of terminal hydrogen of glucose with chemical shift at δ 4.65 and δ 5.24 as quantitative peaks, the content of glucose in MMF samples was determined. The glucose content showed a good linear relationship within the range of 0.10-6.44 mg·mL~(-1). The relative standard deviations(RSDs) of precision, stability, repeatability, and recovery for determination were all less than 2.3%. The glucose content varied in different commercially available MMF samples, which were associated with the different fermentation days, wheat bran-to-flour ratios, and processing methods. The glucose content in MMF first increased and then decreased over the fermentation time. Compared with the MMF products fermented with wheat bran or flour alone, the products fermented with both wheat bran and flour had increased glucose. The glucose content of bran-fried MMF was slightly lower than that of raw MMF, while the glucose content in charred MMF was extremely low. In conclusion, the qHNMR method established in this study is simple, fast, and accurate, serving as a new method for determining the glucose content in MMF. Furthermore, this study clarifies the variations of glucose content in MMF during processing, which can not only indicate the processing degree but also provide a scientific basis for revealing the fermentation mechanism and improving the quality control of MMF.


Assuntos
Medicamentos de Ervas Chinesas , Prótons , Medicamentos de Ervas Chinesas/química , Fibras na Dieta , Espectroscopia de Ressonância Magnética
3.
Phytochem Anal ; 33(7): 1068-1085, 2022 Oct.
Artigo em Inglês | MEDLINE | ID: mdl-35778370

RESUMO

INTRODUCTION: Alkaloids exist in various herbal medicine widely and exhibit diverse biological and pharmacological activities. p-Sulphonatocalix[6]arenes (SC6A) and p-sulphonatocalix[8]arenes (SC8A) are water-soluble supramolecular macrocycles and are applied to the extraction of alkaloids from herbal products. OBJECTIVE: In this study, an innovative method of SC6A/SC8A assisted extraction of the alkaloids from herbs was established. METHODS: SC6A and SC8A were designed to extract 27 alkaloids from seven herbal medicines. Based on the significant solubilisation and extraction effect, Stephaniae Tetrandrae Radix (Fangji, FJ) was selected to obtain the optimal extraction process by adopting single factor test and orthogonal experiment. Then, the alkaloids and SC6A/SC8A were separated by one-step alkalisation and SCnA were reused. The host-guest complexes between alkaloids and SCnA were determined by competitive fluorescence titration, differential scanning calorimetry (DSC), Fourier-transform infrared (FTIR) and proton nuclear magnetic resonance (1 H-NMR) analysis. RESULTS: The optimum condition for SC6A assisted extraction was 5:1:80 (g/g/mL) for herbs/SC6A/solution ratio, 355-250 µm particle size and ultrasonicate 0.5 h, whilst 10:1:40 (g/g/mL) for herbs/SC8A/solution ratio, 355-250 µm particle size and ultrasonicate 0.5 h for SC8A assisted extraction. The total yield of alkaloids (fangchinoline and tetrandrine) from FJ was increased by 4.87 times and 5.97 times with SC6A and SC8A. Moreover, a good reusability of SC6A/SC8A was achieved by alkalisation dissociation. Host-guest complexes were determined by competitive fluorescence titration at a molar ratio of 1:1 between most alkaloids (25/27, except evodiamine and rutaecarpine) and SC6A/SC8A. The complex structure was proved by DSC, FTIR and 1 H-NMR analysis. CONCLUSION: The study provided an effective eco-friendly and energy-saving extraction method of alkaloids from herbal medicine.


Assuntos
Alcaloides , Medicamentos de Ervas Chinesas , Plantas Medicinais , Alcaloides/química , Medicamentos de Ervas Chinesas/química , Medicina Herbária , Plantas Medicinais/química , Prótons , Água
4.
Nat Commun ; 12(1): 4091, 2021 07 02.
Artigo em Inglês | MEDLINE | ID: mdl-34215748

RESUMO

Little is known about the transcriptomic plasticity and adaptive mechanisms of circulating tumor cells (CTCs) during hematogeneous dissemination. Here we interrogate the transcriptome of 113 single CTCs from 4 different vascular sites, including hepatic vein (HV), peripheral artery (PA), peripheral vein (PV) and portal vein (PoV) using single-cell full-length RNA sequencing in hepatocellular carcinoma (HCC) patients. We reveal that the transcriptional dynamics of CTCs were associated with stress response, cell cycle and immune-evasion signaling during hematogeneous transportation. Besides, we identify chemokine CCL5 as an important mediator for CTC immune evasion. Mechanistically, overexpression of CCL5 in CTCs is transcriptionally regulated by p38-MAX signaling, which recruites regulatory T cells (Tregs) to facilitate immune escape and metastatic seeding of CTCs. Collectively, our results reveal a previously unappreciated spatial heterogeneity and an immune-escape mechanism of CTC, which may aid in designing new anti-metastasis therapeutic strategies in HCC.


Assuntos
Carcinoma Hepatocelular/genética , Carcinoma Hepatocelular/imunologia , Heterogeneidade Genética , Evasão da Resposta Imune , Neoplasias Hepáticas/genética , Neoplasias Hepáticas/imunologia , Células Neoplásicas Circulantes/imunologia , Idoso , Animais , Biomarcadores Tumorais/metabolismo , Ciclo Celular , Linhagem Celular Tumoral , Quimiocina CCL5/metabolismo , Regulação Neoplásica da Expressão Gênica , Humanos , Masculino , Camundongos , Camundongos Endogâmicos C57BL , Pessoa de Meia-Idade , Metástase Neoplásica , Células Neoplásicas Circulantes/metabolismo , Prognóstico , RNA-Seq , Transcriptoma , Microambiente Tumoral
5.
Phytochem Anal ; 32(6): 1141-1151, 2021 Nov.
Artigo em Inglês | MEDLINE | ID: mdl-33949013

RESUMO

INTRODUCTION: With the wide application of Scutellaria barbata D. Don for hepatitis and mastitis, its quality control issues have also received increasing attention. Based on the multi-component and multi-target characteristics of traditional Chinese medicine, there is an urgent need to establish a quality evaluation system. OBJECTIVES: This study intends to integrate the "quality-activity-quantification" strategy and establish an activity-related quality control method to ensure the safety and effectiveness of S. barbata. MATERIAL AND METHODS: Ultra-high performance liquid chromatography/ion mobility-quadrupole time-of-flight mass spectrometry (UPLC/IM-QTOF-MS) was used to characterize the chemical components of S. barbata, and network pharmacological analysis was carried out on the identified components. The index components were determined on the basis of comprehensive activity prediction results and content information. At the same time, the contents of 16 batches of S. barbata from different origins were determined. RESULTS: A total of 94 compounds were identified according to mass spectrometric data, 12 of which were isolated and structure-confirmed by nuclear magnetic resonance technology. Network pharmacological analysis was applied to predict their key targets and the major pathways mediating their anti-inflammatory effects. On the basis of comprehensive activity prediction and content information, five components were chosen as crucial quality indicators of S. barbata, including scutellarin, scutellarein, luteolin, apigenin, and hispidulin. CONCLUSION: In this study, 16 different S. barbata batches were compared, and five quality indicators were determined on the basis of qualitative and activity results. The present study provides useful information for evaluating the quality of S. barbata in different areas, and also provides a new basis for the development of quality evaluation methods.


Assuntos
Scutellaria , Anti-Inflamatórios/farmacologia , Cromatografia Líquida de Alta Pressão , Extratos Vegetais , Controle de Qualidade
6.
Phytomedicine ; 69: 152690, 2020 Apr.
Artigo em Inglês | MEDLINE | ID: mdl-30389273

RESUMO

BACKGROUND: Rhodioloside is a glucoside of tyrosol isolated from Rhodiola rosea. However, its regulating effect on hepatic dyslipidemia of atherogenic mice has rarely been studied. PURPOSE: The specific aims of current study included to clarify lipidomic perturbation in liver tissues of apolipoprotein E deficient (apoE-/-) mice fed with high-fat diet, and to examine the effects of rhodioloside against atherosclerosis and dyslipidemia. STUDY DESIGN: The comparisons of hepatic lipidome were executed between wide type (WT) mice fed with normal diet (NDC) and apoE-/- mice fed with high-fat diet (Model), WT mice fed with high-fat diet (HFDC) versus the model mice, as well as the model mice versus rhodioloside-treated atherosclerotic mice. METHODS: Ultra high performance liquid chromatography coupled with a Q exactive hybrid quadrupole-orbitrap mass spectrometry (UPLC-MS/MS) was employed to provide an unbiased and simultaneous measurement of individual lipid species in liver tissues. RESULTS: Multivariate statistical analysis derived from LC-MS spectra revealed that high-fat diet and apoE deficiency caused a series of disturbances on glyerolipid metabolism, glycerophospholipid metabolism and sphingolipid metabolism. Rhodioloside administration showed atheroprotective effects on the apoE-/- mice with regulating the levels of 1 phosphatidylcholine, 2 phosphatidylserines, 5 alkyldiacylglycerols and 3 alkenyldiacylglycerols back to normal. In particular, PC (4:0/15:0) was positively associated with high-density lipoprotein cholesterol in blood, both of which could be ameliorated by rhodioloside. CONCLUSION: Our results identified the abnormal hepatic lipids in atherosclerosis progression that could efficiently improved by rhodioloside. These lipids contributed to biological understanding of atherogenic dyslipidemia in liver and could also served as sensitive indicators for drug target screening.


Assuntos
Apolipoproteínas E/genética , Dieta Hiperlipídica/efeitos adversos , Dislipidemias/tratamento farmacológico , Glucosídeos/farmacologia , Fígado/efeitos dos fármacos , Fenóis/farmacologia , Animais , Aterosclerose/tratamento farmacológico , Aterosclerose/metabolismo , Aterosclerose/patologia , Cromatografia Líquida , Dislipidemias/genética , Dislipidemias/metabolismo , Metabolismo dos Lipídeos/efeitos dos fármacos , Lipídeos/sangue , Fígado/metabolismo , Masculino , Camundongos Endogâmicos C57BL , Camundongos Knockout , Camundongos Knockout para ApoE , Espectrometria de Massas em Tandem
7.
Proteomics ; 19(15): e1900092, 2019 08.
Artigo em Inglês | MEDLINE | ID: mdl-31294914

RESUMO

Odoroside A (OA) is an active ingredient extracted from the leaves of Nerium oleander Linn. (Apocynaceae). This study aims to examine the anticancer bioactivity of OA against CRC cells and to investigate the action mechanisms involved. As a result, OA can significantly inhibit cellular ability and induce apoptosis of CRC cells in a concentration-dependent manner without any obvious cytotoxicity in normal colorectal epithelial cells. Then, quantitative proteomics combined with bioinformatics is adopted to investigate the alterations of proteins and signaling pathways in response to OA treatment. As suggested by the proteomic analysis, flow cytometry and Western blotting analyses validate that exposure of CRC cells to OA causes cell cycle arrest and apoptosis, accompanied with the activation of the ROS/p53 signaling pathway. This observation demonstrates that OA, as a natural product, can induce oxidative stress to suppress tumor cell growth, implicating a novel therapeutic agent against CRC without obvious side effects.


Assuntos
Cardenolídeos/farmacologia , Pontos de Checagem da Fase G2 do Ciclo Celular/efeitos dos fármacos , Proteômica/métodos , Espécies Reativas de Oxigênio/metabolismo , Proteína Supressora de Tumor p53/metabolismo , Apoptose/efeitos dos fármacos , Pontos de Checagem do Ciclo Celular/efeitos dos fármacos , Linhagem Celular Tumoral , Proliferação de Células/efeitos dos fármacos , Biologia Computacional , Células HT29 , Humanos , Transdução de Sinais/efeitos dos fármacos
8.
Zhongguo Dang Dai Er Ke Za Zhi ; 21(7): 663-669, 2019 Jul.
Artigo em Chinês | MEDLINE | ID: mdl-31315765

RESUMO

OBJECTIVE: To investigate the composition of gut microbiota and its correlation with the severity of behavior symptoms in children with autism spectrum disorder (ASD). METHODS: A total of 30 children with ASD were enrolled as the ASD group, and 20 healthy children matched for age and sex were enrolled as the healthy control group. Related clinical data were analyzed. The V3-V4 hypervariable regions of the bacterial 16S rRNA gene in fecal samples were sequenced. The severity of behavior symptoms in children with ASD was assessed using the autism behavior checklist. The Spearman's correlation analysis was used to investigate the correlation between gut microbiota and the severity of behavior symptoms in children with ASD. RESULTS: There was a significant difference in the composition of gut microbiota between the two groups. Compared with the healthy control group, the ASD group had significant reductions in Shannon index and Shannoneven index (P<0.05), as well as a significant reduction in the percentage of Firmicutes and a significant increase in the percentage of Acidobacteria in feces (P<0.05). In the ASD group, the dominant bacteria were Megamonas, Megasphaera, and Barnesiella, while in the healthy control group, the dominant bacteria were Eubacterium_rectale_group, Ezakiella, and Streptococcus. In the children with ASD, the abundance of Megamonas was positively correlated with the scores of health/physical/behavior and language communication (P<0.05). CONCLUSIONS: The development of ASD and the severity of behavior symptoms are closely associated with the composition of gut microbiota.


Assuntos
Transtorno do Espectro Autista , Microbioma Gastrointestinal , Bactérias , Criança , Fezes , Humanos , RNA Ribossômico 16S
9.
Phytomedicine ; 57: 352-363, 2019 Apr.
Artigo em Inglês | MEDLINE | ID: mdl-30831484

RESUMO

BACKGROUND: Nerigoside (NG), a cardenolide isolated from a commonfolk medicine, Nerium oleander Linn. (Apocynaceae), has not been explored for its biological effects. To date, cardenolides have received considerable attention in pharmacology studies due to their direct effects of apoptosis-induction or growth-inhibitory against tumor in vitro and in vivo. Whether and how NG exerts anticancer effects against colorectal cancer remains to be elucidated. PURPOSE: The aim of this study was to investigate the anticancer effect of NG in human colorectal cancer cells. METHODS: To test anticancer effect, we compared potency of NG in two colorectal cancer cell lines, HT29 and SW620 by WST-1 and colony proliferation assays. And we investigated mechanism of anticancer activities by analyzing players in apoptotic and ERK/GSK3ß/ß-catenin signaling pathways in HT29 and SW620 cells treated with NG. RESULTS: In this study, we showed that NG markedly suppressed the cell viability and colony formation of colorectal cancer cells HT29 and SW620, with no significant toxic effect on non-cancer cells NCM460. Annexin V-FITC/PI and CFSE labeling results revealed that NG suppressed cell proliferation in low concentration, along with reducing expression of PCNA, while NG induced apoptosis in high concentration,. Meanwhile, NG significantly arrested cell migration by reversal of EMT and cell cycle on G2/M. Then, we found that the ERK and GSK3ß/ß-catenin signaling pathway were noticeably blocked in CRC cells after treatment with NG. According to western blot, NG upregulated the expression of p-GSK3ß/GSK3ß and decreased especially the expression of ß-catenin in nuclear. In addition, Wnt signaling and its target genes were suppressed in response to NG. Then, the Ser9 phosphorylation of GSK3ß can be reduced / raised by GÖ 6983 / LiCl, respectively. Thus, we further confirmed that the GSK3ß/ß-catenin axis is involved in NG-prevented cell proliferation. CONCLUSION: NG inhibited the growth of colorectal cancer cells by suppressing ERK/GSK3ß/ß-catenin signaling pathway. And the GSK3ß/ß-catenin axis is involved in preventing cell proliferation and migration by NG-treatment. These results suggest that NG may be used to treat colorectal cancer, with better outcome by combining with GSK3ß inhibitor to block Wnt pathway.


Assuntos
Antineoplásicos Fitogênicos/farmacologia , Neoplasias Colorretais/tratamento farmacológico , Neoplasias Colorretais/patologia , Glicogênio Sintase Quinase 3 beta/metabolismo , beta Catenina/metabolismo , Antineoplásicos Fitogênicos/química , Apoptose/efeitos dos fármacos , Ciclo Celular/efeitos dos fármacos , Linhagem Celular Tumoral , Movimento Celular/efeitos dos fármacos , Proliferação de Células/efeitos dos fármacos , Sobrevivência Celular/efeitos dos fármacos , Neoplasias Colorretais/metabolismo , Glicogênio Sintase Quinase 3 beta/antagonistas & inibidores , Células HT29 , Humanos , Sistema de Sinalização das MAP Quinases/efeitos dos fármacos , Terapia de Alvo Molecular/métodos , Nerium/química , Fosforilação/efeitos dos fármacos , Transdução de Sinais/efeitos dos fármacos , beta Catenina/antagonistas & inibidores
10.
Regul Toxicol Pharmacol ; 103: 1-9, 2019 Apr.
Artigo em Inglês | MEDLINE | ID: mdl-30634019

RESUMO

Isopsoralen is a major active and quality-control component of Fructus Psoraleae, but lacks a full safety evaluation. We evaluated the oral toxicity of isopsoralen in Wistar rats treated for 3 months at doses of 0, 3.5, 7.0, and 14 mg/kg. Additionally, the plasma metabolomics of isopsoralen in male and female rats treated for 3 months at doses of 0 and 14 mg/kg were investigated by gas chromatography-mass spectrometry. Many abnormalities were observed in the isopsoralen-treated rats, including suppression of body weight gain, and changes in serum biochemical parameters and visceral coefficients. Histopathological changes in liver, pancreatic, and reproductive system tissues were also observed in the isopsoralen-treated rats. The metabolomic analyses showed alterations in many metabolites (19 in female rats; 28 in male rats) after isopsoralen administration. The significant changes in these metabolites revealed metabolomic alterations in the isopsoralen-treated rats, especially in amino acid metabolism regardless of sex, including phenylalanine, tyrosine, and tryptophan biosynthesis and glycine, serine, and threonine metabolism. Furthermore, fatty acid metabolism comprised the main affected pathways in female rats, while lipid metabolism and energy metabolism were the main affected pathways in male rats.


Assuntos
Sistema Digestório/efeitos dos fármacos , Sistema Digestório/metabolismo , Furocumarinas/toxicidade , Caracteres Sexuais , Sistema Urogenital/efeitos dos fármacos , Sistema Urogenital/metabolismo , Animais , Peso Corporal/efeitos dos fármacos , Sistema Digestório/patologia , Relação Dose-Resposta a Droga , Feminino , Furocumarinas/administração & dosagem , Furocumarinas/metabolismo , Cromatografia Gasosa-Espectrometria de Massas , Masculino , Ratos , Ratos Wistar , Testes de Toxicidade , Sistema Urogenital/patologia
11.
Chem Res Toxicol ; 31(9): 852-860, 2018 09 17.
Artigo em Inglês | MEDLINE | ID: mdl-30132663

RESUMO

Psoralen is the main active component of Psoralea corylifolia and is used as a marker to assess its quality. The effects of psoralen on animals have been well characterized. However, the molecular pathway of its toxicity is not fully understood. In this study, the toxic effects of psoralen administration (60 mg/kg) for 7 days in Sprague-Dawley rats were observed. Serum biochemistry and liver histopathology were further investigated. Proton nuclear magnetic resonance was applied to characterize the metabolic profile of liver toxicity induced by psoralen and to find changed metabolites in rat serum and liver. It was revealed that visceral coefficients and serum biochemistry indexes were significantly changed in rats with psoralen-induced liver injury. Furthermore, the histopathological examination exhibited that the liver might be the target organ for psoralen. Metabolic analysis of both serum and liver samples further proved the liver was the target of toxicity of psoralen. Multivariate analysis identified 7 metabolites in serum samples and 15 in liver samples as potential biomarkers in liver injury induced by psoralen. In addition, our results suggest that psoralen can cause a disturbance in amino acid metabolism, especially valine, leucine, and isoleucine biosynthesis in both serum and liver samples. In conclusion, we combined the results of toxicity and metabolomics induced by psoralen and provide useful information about the safety and potential risks of psoralen and Psoralea corylifolia.


Assuntos
Doença Hepática Induzida por Substâncias e Drogas/sangue , Doença Hepática Induzida por Substâncias e Drogas/metabolismo , Ficusina/toxicidade , Fígado/efeitos dos fármacos , Espectroscopia de Ressonância Magnética/métodos , Metabolômica , Animais , Biomarcadores/sangue , Biomarcadores/metabolismo , Fígado/lesões , Fígado/metabolismo , Ratos , Ratos Sprague-Dawley
12.
Fitoterapia ; 127: 293-300, 2018 Jun.
Artigo em Inglês | MEDLINE | ID: mdl-29540313

RESUMO

Six new cardenolides (1-6), including three 14-hydroxylated cardenolides and three 14-carbonylated cardenolides were isolated from the dried aerial parts of Nerium oleander Linn in addition to twenty-seven known compounds (7-33). Their structures were elucidated on the basis of extensive spectroscopic evidences and single-crystal X-ray diffraction analysis. Compounds 1, 4, 7-10 and 13 exhibited significant cytotoxicity against four colon cancer cell lines (HCT116, HT29, SW620, RKO), one gastric cancer cell line (GT) and one cervical cancer cell line (HeLa) in vitro.


Assuntos
Antineoplásicos Fitogênicos/isolamento & purificação , Cardenolídeos/isolamento & purificação , Nerium/química , Folhas de Planta/química , Antineoplásicos Fitogênicos/farmacologia , Cardenolídeos/farmacologia , Linhagem Celular Tumoral , Humanos , Estrutura Molecular , Extratos Vegetais/química
13.
J Pharm Biomed Anal ; 131: 183-187, 2016 Nov 30.
Artigo em Inglês | MEDLINE | ID: mdl-27596830

RESUMO

In this study, a new approach using 1H NMR spectroscopy combined with chemometrics method was developed for qualitative and quantitative analyses of extracts of Compound Danshen Dripping Pills (CDDP). For the qualitative analysis, some metabolites presented in Compound Danshen extract (CDE, extraction intermediate of CDDP) were detected, including phenolic acids, saponins, saccharides, organic acids and amino acids, by the proposed 1H NMR method, and metabolites profiles were further analyzed by selected chemometrics algorithms to define the threshold values for product quality evaluation. Moreover, three main phenolic acids (danshensu, salvianolic acid B, and procatechuic aldehyde) in CDE were determined simultaneously, and method validation in terms of linearity, precision, repeatability, accuracy, and stability of the dissolved target compounds in solution was performed. The average recoveries varied between 84.20% and 110.75% while the RSDs were below 6.34% for the three phenolic acids. This 1H NMR method offers an integral view of the extract composition, allows the qualitative and quantitative analysis of CDDP, and has the potential to be a supplementary tool to UPLC/HPLC for quality assessment of Chinese herbal medicines.


Assuntos
Medicamentos de Ervas Chinesas/química , Espectroscopia de Prótons por Ressonância Magnética/métodos , Controle de Qualidade , Benzofuranos/análise , Catequina/análogos & derivados , Catequina/análise , Estabilidade de Medicamentos , Lactatos/análise , Reprodutibilidade dos Testes , Salvia miltiorrhiza
14.
Phytomedicine ; 23(6): 641-53, 2016 Jun 01.
Artigo em Inglês | MEDLINE | ID: mdl-27161405

RESUMO

BACKGROUND: Catharanthus roseus (L.) G. Don consists of a range of dimeric indole alkaloids with significant antitumor activities. These alkaloids have been found to possess apoptosis-inducing activity against tumor cells in vitro and in vivo mediated by nuclear factor kappa-light-chain-enhancer of activated B cells (NF-κB) and c-Jun N-terminal kinase (JNK) pathways, in which DNA damage and mitochondrial dysfunction play important roles. In this study, a unique bisindole alkaloid named cathachunine, along with five known dimeric indole alkaloids, was obtained from C. roseus and investigated in vitro. PURPOSE: The aim of this study was to investigate the antitumor activity of isolated alkaloids and the mechanism through which cathachunine exerts its antitumor effect. STUDY DESIGN AND METHODS: Cell growth inhibition was assessed by WST-1 and lactate dehydrogenase (LDH) assays in HL60, K562 leukemia cells and EA.hy926 umbilical vein cells. Induction of apoptosis in HL60 cells was confirmed by observation of nuclear morphology, a caspase-3 activity assay and annexin V-fluorescein isothiocyanate/propidium iodide (FITC/PI) double staining. The intrinsic apoptotic pathway induced by cathachunine was evidenced by B-cell lymphoma 2/Bcl-2-associated X protein (Bcl-2/Bax) dysregulation, loss of mitochondrial membrane potential, translocation of cytochrome c, and cleavage of caspase-3 and poly-ADP ribose polymerase (PARP). Reactive oxygen species (ROS) production after cathachunine treatment was determined by 2',7'-dichlorodihydrofluorescein diacetate (DCFH-DA) staining. Cell cycle arrest of the S phase was also observed in HL60 cells after cathachunine treatment. RESULTS: The WST-1 and LDH assays showed that Catharanthus alkaloids were cytotoxic toward human leukemia cells to a greater extent than toward normal human endothelial cells, and the anti-proliferation and pro-apoptosis abilities of cathachunine were much more potent than other previously reported alkaloids. The induction of apoptosis by cathachunine occurred through an ROS-dependent mitochondria-mediated intrinsic pathway rather than an extrinsic pathway, and was regulated by the Bcl-2 protein family. CONCLUSION: An unprecedented bisindole alkaloid cathachunine which lost C-18' and C-19' was isolated from C. roseus. It exerted a potent antitumor effect toward human leukemia cells through the induction of apoptosis via an intrinsic pathway. Thus, this study provides evidence for a new lead compound from a natural source for anti-cancer investigations.


Assuntos
Alcaloides/farmacologia , Antineoplásicos/farmacologia , Apoptose/efeitos dos fármacos , Leucemia/tratamento farmacológico , Extratos Vegetais/farmacologia , Antineoplásicos/uso terapêutico , Catharanthus/química , China , Humanos , Células K562/efeitos dos fármacos
15.
J Asian Nat Prod Res ; 18(7): 656-61, 2016 Jul.
Artigo em Inglês | MEDLINE | ID: mdl-26999269

RESUMO

A new phenyldihydronaphthalene-type lignan, (3R,4S)-6-hydroxy-4-(4-hydroxy- 3-methoxyphenyl)-5,7-dimethoxy-3,4-dihydro-2-naphthaldehyde-3a-O-ß-d-glucopyranoside (1), and a new phenylnaphthalene-type lignan, 6,7,4'-trihydroxy-3'-methoxy-2,3- cycloligna-1,4-dien-2a,3a-olide (2), along with 10-known lignan derivatives (3-12) were isolated from the aerial part of Vitex negundo var. heterophylla. Their structures were established by comprehensive 1D- and 2D-NMR spectroscopic analyses.


Assuntos
Medicamentos de Ervas Chinesas/isolamento & purificação , Glucosídeos/isolamento & purificação , Lignanas/isolamento & purificação , Componentes Aéreos da Planta/química , Vitex/química , Medicamentos de Ervas Chinesas/química , Glucosídeos/química , Lignanas/química , Estrutura Molecular , Ressonância Magnética Nuclear Biomolecular
16.
J Nat Prod ; 79(1): 38-50, 2016 Jan 22.
Artigo em Inglês | MEDLINE | ID: mdl-26714048

RESUMO

Investigation of the seeds of Thevetia peruviana resulted in the isolation of 15 new (2-16) and 18 known (1 and 17-33) cardiac glycosides. Eight 19-nor-cardenolides (1-8), including two rare 19-nor-10-hydroperoxycardenolides, were obtained from T. peruviana for the first time. All the structures were characterized by NMR spectroscopy and chemical derivatization. The inhibitory effects of cardiac glycosides 1-33 against three cancer cell lines (human lung cancer cells, P15; human gastric cancer cells, MGC-803; and human pancreatic cancer cells, SW1990) and one normal hepatocyte cell line, LO2, were evaluated, and a preliminary structure-activity relationship is discussed. In addition, cardiac glycosides 1, 22, 26, and 28 were evaluated for their apoptosis-inducing activities in MGC-803 cells, showing IC50 values in the range 0.02-0.53 µM.


Assuntos
Antineoplásicos Fitogênicos/isolamento & purificação , Cardenolídeos/isolamento & purificação , Glicosídeos Cardíacos/isolamento & purificação , Medicamentos de Ervas Chinesas/isolamento & purificação , Sementes/química , Thevetia/química , Antineoplásicos Fitogênicos/química , Antineoplásicos Fitogênicos/farmacologia , Cardenolídeos/química , Cardenolídeos/farmacologia , Glicosídeos Cardíacos/química , Glicosídeos Cardíacos/farmacologia , Ensaios de Seleção de Medicamentos Antitumorais , Medicamentos de Ervas Chinesas/química , Medicamentos de Ervas Chinesas/farmacologia , Humanos , Concentração Inibidora 50 , Estrutura Molecular , Ressonância Magnética Nuclear Biomolecular , Relação Estrutura-Atividade
17.
Zhongguo Zhong Yao Za Zhi ; 40(13): 2629-33, 2015 Jul.
Artigo em Inglês | MEDLINE | ID: mdl-26697690

RESUMO

Nuclear magnetic resonance (1H-NMR) fingerprint of Rhodiola rosea medicinal materials was established, and used to distinguish the quality of raw materials from different sources. Pulse sequence for water peak inhibition was employed to acquire 1H-NMR spectra with the temperature at 298 K and spectrometer frequency of 400.13 MHz. Through subsection integral method, the obtained NMR data was subjected to similarity analysis and principal component analysis (PCA). 10 batches raw materials of Rhodiola rosea from different origins were successfully distinguished by PCA. The statistical results indicated that rhodiola glucoside, butyl alcohol, maleic acid and alanine were the main differential ingredients. This method provides an auxiliary method of Chinese quality approach to evaluate the quality of Rhodiola crenulata without using natural reference substances.


Assuntos
Espectroscopia de Ressonância Magnética/métodos , Rizoma/química , Rhodiola/química , Análise de Componente Principal
18.
Molecules ; 20(8): 13725-39, 2015 Jul 28.
Artigo em Inglês | MEDLINE | ID: mdl-26225952

RESUMO

In the present study, two new phenolic compounds 1 and 11, a pair of lignan isomers 12 and 13 with their absolute configurations established for the first time, were isolated from the ethanol extract of the roots of Rhodiola crenulata, together with 13 known phenolic compounds, and their structures were elucidated via NMR, HRESIMS, UV, IR and CD analyses. All the isolated compounds were evaluated for their in vitro antioxidant activities using the 2,2-diphenyl-1-picryhydrazyl (DPPH) and 2,2'-azino-bis (3-ethylbenzothiazoline-6-sulfonic acid) (ABTS) radical scavenging assays. Ten of them exhibited significant antioxidant activities compared to ascorbic acid. Furthermore, the inducibilities of the isolated compounds to IFN-γ production were also assessed. Compounds 1, 8, 9, 12, 13, 14 and 15 could moderately stimulate IFN-γ expression.


Assuntos
Sequestradores de Radicais Livres/farmacologia , Regulação da Expressão Gênica/efeitos dos fármacos , Indutores de Interferon/farmacologia , Interferon gama/biossíntese , Extratos Vegetais/biossíntese , Raízes de Plantas/química , Rhodiola/química , Baço/metabolismo , Animais , Células Cultivadas , Etanol/química , Sequestradores de Radicais Livres/química , Indutores de Interferon/química , Camundongos , Camundongos Endogâmicos BALB C , Baço/citologia
19.
Cell Tissue Res ; 360(2): 379-89, 2015 May.
Artigo em Inglês | MEDLINE | ID: mdl-25585987

RESUMO

Some cytokines, such as interleukin-2 (IL-2), interferon-γ (IFN-γ) and tumor necrosis factor-α (TNF-α), produced by lymphocytes might play an important role in anti-tumor immunity and their production is possibly suppressed by cancer. Amelioration of the suppression of cytokine production might contribute to cancer control. Ganoderma lucidum polysaccharides (Gl-PS), a versatile group of a component of G. lucidum and one with various bioactivities, might have this potential. In this study, analyses including reverse transcription and the polymerase chain reaction (RT-PCR), immunocytochemistry and Western blot were used to test the effects of Gl-PS on the production of IL-2, IFN-γ and TNF-α in mononuclear lymphocytes by incubating Gl-PS with mouse splenic mononuclear lymphocytes in the presence of B16F10 cell culture supernatant following activation by phytohemagglutinin. The RT-PCR, immunocytochemistry and Western blot assays showed that the production of IL-2, IFN-γ and TNF-α in mononuclear lymphocytes was suppressed by B16F10 cell culture supernatant at both the mRNA and protein levels, whereas the suppression was fully or partially ameliorated by Gl-PS. The amelioration by Gl-PS against the suppression of the production of IL-2, IFN-γ and TNF-α in mononuclear lymphocytes by B16F10 cell culture supernatant might contribute to cancer control.


Assuntos
Citocinas/imunologia , Polissacarídeos Fúngicos/farmacologia , Ativação Linfocitária/efeitos dos fármacos , Linfócitos/imunologia , Melanoma/imunologia , Reishi/química , Animais , Linhagem Celular Tumoral , Polissacarídeos Fúngicos/química , Melanoma/patologia , Camundongos
20.
Nat Prod Commun ; 9(1): 13-4, 2014 Jan.
Artigo em Inglês | MEDLINE | ID: mdl-24660450

RESUMO

One new and seven known diterpenoids were isolated from the aerial parts of Andrographis paniculata, and their structures elucidated on the basis of spectroscopic and spectrometric analysis, as well as chemical methods. The in vitro antiviral activities of these compounds against respiratory syncytial virus (RSV) were assayed.


Assuntos
Andrographis/química , Diterpenos/isolamento & purificação , Antivirais/análise , Diterpenos/química , Estrutura Molecular , Componentes Aéreos da Planta/química , Plantas Medicinais/química
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