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1.
Zhongguo Zhong Yao Za Zhi ; 44(15): 3323-3329, 2019 Aug.
Artigo em Chinês | MEDLINE | ID: mdl-31602890

RESUMO

To study the correlation between ultra high performance liquid chromatography( UPLC) fingerprint of Smilax china and its anti-pelvic inflammatory effect,and to explore the pharmacodynamic material basis of S. china against pelvic inflammatory disease.UPLC fingerprints of 10 batches of S. china from different habitats were established,and the values of SOD,MDA,TNF-α,and IL-6 in rats with pelvic inflammation were measured. The weight of each single pharmacodynamics index to the total efficacy was determined by analytic hierarchy process,and the contribution of each peak in fingerprints to the each single pharmacodynamics index and total efficacy was analyzed by the grey relational analysis. Then the structures of chemical constituents at the identified peaks were confirmed by comparing with the reference substance. The 27 common characteristic peaks of UPLC fingerprints were all related to the anti-pelvic inflammation effect of S. china,of which 13 peaks were identified as peak 2( 3,5-dihydroxy-2-methylbenzoic acid-3-O-glucoside),peak 3( chlorogenic acid),peak 5( 2,7,4-trihydroxydihydroflavone-5-O-glucoside),peak 6( 7,4-dihydroxydihydroflavonol-5-O-glucoside),peak 7( taxifolin-7-O-glucoside),peak 9( taxifolin),peak 10( polydatin),peak 11( oxyresveratrol),peak 12( astilbin),peak15( resveratrol),peak 16( quercitrin),peak 18( engeletin) and peak 24( kaempferol). The correlation degree of 21 peaks and the total efficacy was greater than 0. 8,and the top 10 ranked by correlation degree were as follows: peak 1,3,7,19,18,17,4,11,16,and 21. The results showed that the anti-pelvic inflammation effect of S. china was achieved by the combined action of pharmacodynamic substances. In order to control the quality of S. china and its prepared slices more effectively,the index components of content detection should be selected reasonably.


Assuntos
Doença Inflamatória Pélvica/tratamento farmacológico , Extratos Vegetais/farmacologia , Smilax/química , Animais , China , Cromatografia Líquida de Alta Pressão , Feminino , Compostos Fitoquímicos/farmacologia , Ratos
2.
Zhongguo Zhong Yao Za Zhi ; 44(17): 3745-3748, 2019 Sep.
Artigo em Chinês | MEDLINE | ID: mdl-31602948

RESUMO

A new isobenzofuranone derivative was isolated from Chaenomeles sinensis by using various chromatographic techniques,including silica gel,Sephadex LH-20,MCI-gel resin and RP-HPLC. This compound was determined as 2,2-dimethyl-5-( 2-oxopropyl)-2 H-furo[3,4-h]chromen-7( 9 H)-one( 1) by NMR,MS,IR and UV spectra,and was also evaluated for its antibacterial activity. The results showed that it showed prominent antibacterial activity with MIC90 value of( 53. 7±4. 5) mg·L-1 for methicillin resistant Staphylococcus aureus( MRSA) strain. This value is close to that of levofloxacin [with MIC90 value( 50. 2± 4. 2) mg·L-1].


Assuntos
Antibacterianos/farmacologia , Benzofuranos/farmacologia , Staphylococcus aureus Resistente à Meticilina/efeitos dos fármacos , Rosaceae/química , Antibacterianos/isolamento & purificação , Benzofuranos/isolamento & purificação , Cromatografia Líquida de Alta Pressão , Testes de Sensibilidade Microbiana , Compostos Fitoquímicos/isolamento & purificação , Compostos Fitoquímicos/farmacologia
3.
Adv Exp Med Biol ; 1152: 293-310, 2019.
Artigo em Inglês | MEDLINE | ID: mdl-31456191

RESUMO

Epigenetics refers to alterations in gene expression due to differential histone modifications and DNA methylation at promoter sites of genes. Epigenetic alterations are reversible and are heritable during somatic cell division, but do not involve changes in nucleotide sequence. Epigenetic regulation plays a critical role in normal growth and embryonic development by controlling transcriptional activities of several genes. In last two decades, these modifications have been well recognized to be involved in tumor initiation and progression, which has motivated many investigators to incorporate this novel field in cancer drug development. Recently, growing number of epigenetic changes have been reported that are involved in the regulations of genes involved in breast tumor growth and metastasis. Drugs possessing epigenetic modulatory activities known as epi-drugs, mainly the inhibitors of histone deacetylases (HDACs) and DNA methyltransferases (DNMTs). Some of these drugs are undergoing different clinical trials for breast cancer treatment. Several phytochemicals such as green tea polyphenols, curcumin, genistein, resveratrol and sulforaphane have also been shown to alter epigenetic modifications in multiple cancer types including breast cancer. In this chapter, we summarize the role of epigenetic changes in breast cancer progression and metastasis. We have also discussed about various epigenetic modulators possessing chemopreventive and therapeutic efficacy against breast cancer with future perspectives.


Assuntos
Neoplasias da Mama/tratamento farmacológico , Neoplasias da Mama/genética , Epigênese Genética , DNA (Citosina-5-)-Metiltransferase 1/antagonistas & inibidores , Metilação de DNA , Feminino , Inibidores de Histona Desacetilases/farmacologia , Histona Desacetilases , Humanos , Compostos Fitoquímicos/farmacologia
4.
Int J Nanomedicine ; 14: 4911-4929, 2019.
Artigo em Inglês | MEDLINE | ID: mdl-31456637

RESUMO

Background: Apocynin (APO) is a bioactive phytochemical with prominent anti-inflammatory and anti-oxidant activities. Designing a nano-delivery system targeted to potentiate the gastric antiulcerogenic activity of APO has not been investigated yet. Chitosan oligosaccharide (COS) is a low molecular weight chitosan and its oral nanoparticulate system for potentiating the antiulcerogenic activity of the loaded APO has been described here. Methods: COS-nanoparticles (NPs) loaded with APO (using tripolyphosphate [TPP] as a cross-linker) were prepared by ionic gelation method and fully characterized. The chosen formula was extensively evaluated regarding in vitro release profile, kinetic analysis, and stability at refrigerated and room temperatures. Ultimately, the in vivo antiulcerogenic activity against ketoprofen (KP)-induced gastric ulceration in rats was assessed by macroscopic parameters including Paul's index and antiulcerogenic activity, histopathological examination, immunohistochemical (IHC) evaluation of cyclooxygenase-2 (COX-2) expression level in ulcerated gastric tissue, and biochemical measurement of oxidative stress markers and nitric oxide (NO) levels. Results: The selected NPs formula with COS (0.5 % w/v) and TPP (0.1% w/v) was the most appropriate one with drug entrapment efficiency percentage of 35.06%, particle size of 436.20 nm, zeta potential of +38.20 mV, and mucoadhesive strength of 51.22%. It exhibited a biphasic in vitro release pattern as well as high stability at refrigerated temperature for a 6-month storage period. APO-loaded COS-NPs provoked marvelous antiulcerogenic activity against KP-induced gastric ulceration in rats compared with free APO treated group, which was emphasized by histopathological, IHC, and biochemical studies. Conclusion: In conclusion, APO-loaded COS-NPs could be considered as a promising oral phytopharmaceutical nanoparticulate system for management of gastric ulceration.


Assuntos
Acetofenonas/administração & dosagem , Acetofenonas/farmacologia , Quitosana/química , Mucosa Gástrica/efeitos dos fármacos , Nanopartículas/química , Oligossacarídeos/química , Compostos Fitoquímicos/administração & dosagem , Compostos Fitoquímicos/farmacologia , Acetofenonas/uso terapêutico , Administração através da Mucosa , Animais , Biomarcadores/metabolismo , Varredura Diferencial de Calorimetria , Ciclo-Oxigenase 2/metabolismo , Liberação Controlada de Fármacos , Cinética , Masculino , Nanopartículas/ultraestrutura , Óxido Nítrico/metabolismo , Estresse Oxidativo/efeitos dos fármacos , Tamanho da Partícula , Ratos Wistar , Espectroscopia de Infravermelho com Transformada de Fourier , Eletricidade Estática , Estômago/efeitos dos fármacos , Estômago/patologia , Úlcera Gástrica/tratamento farmacológico , Úlcera Gástrica/patologia , Suínos , Difração de Raios X
5.
Fitoterapia ; 137: 104285, 2019 Sep.
Artigo em Inglês | MEDLINE | ID: mdl-31386897

RESUMO

Botanical-based natural products are an important resource for medicinal drug discovery and continue to provide diverse pharmacophores with therapeutic potential against cancer and other human diseases. A prototype Traditional Chinese Medicine (TCM) plant extract library has been established at the US National Cancer Institute, which contains both the organic and aqueous extracts of 132 authenticated medicinal plant species that collectively represent the potential therapeutic contents of most commonly used TCM herbal prescriptions. This library is publicly available in 96- and 384- well plates for high throughput screening across a broad array of biological targets, as well as in larger quantities for isolation of active chemical ingredients. Herein, we present the methodology used to generate the library and the preliminary assessment of the anti-proliferative activity of this crude extract library in NCI-60 human cancer cell lines screen. Particularly, we report the chemical profiling and metabolome comparison analysis of four commonly used TCM plants, namely Brucea javanica, Dioscorea nipponica, Cynanchum atratum, and Salvia miltiorrhiza. Bioassay-guided isolation resulted in the identification of the active compounds, and different extraction methods were compared for their abilities to extract cytotoxic compounds and to concentrate biologically active natural products.


Assuntos
Antineoplásicos Fitogênicos/farmacologia , Compostos Fitoquímicos/farmacologia , Extratos Vegetais/química , Plantas Medicinais/química , Antineoplásicos Fitogênicos/isolamento & purificação , Brucea/química , Linhagem Celular Tumoral , China , Cynanchum/química , Dioscorea/química , Descoberta de Drogas , Humanos , Medicina Tradicional Chinesa , National Cancer Institute (U.S.) , Compostos Fitoquímicos/isolamento & purificação , Salvia miltiorrhiza/química , Estados Unidos
6.
Fitoterapia ; 137: 104287, 2019 Sep.
Artigo em Inglês | MEDLINE | ID: mdl-31386898

RESUMO

Phytochemical investigation of the fruit of Crataegus pinnatifida led to the isolation of four pairs of dihydrobenzofuran neolignan enantiomers (1a/1b-4a/4b) including six new compounds (1a/1b, 2a/2b, 3a and 4a). The enantioseparations of the racemates were achieved successfully by chiral chromatographic column. Their structures were established by comprehensive spectroscopic analyses and the absolute configurations were determined by quantum mechanical calculation of electronic circular dichroism (ECD) spectra. All compounds were evaluated in vitro for their cytotoxicity using human hepatocellular carcinoma Hep3B and HepG2 cells. Among them, it was found that 2a had a selective cytotoxicity against Hep3B cells with IC50 value of 25.47 µM, while the IC50 value of its enantiomer 2b on Hep3B cells was 59.37 µM. These results implied that the absolute configurations of 2a and 2b possessed remarkable influences on their cytotoxicity. Further flow cytometry analysis indicated that 2a performed more significant effect on cell apoptosis compared with its enantiomer 2b.


Assuntos
Antineoplásicos Fitogênicos/farmacologia , Apoptose/efeitos dos fármacos , Crataegus/química , Frutas/química , Lignanas/farmacologia , Antineoplásicos Fitogênicos/isolamento & purificação , China , Células Hep G2 , Humanos , Lignanas/isolamento & purificação , Estrutura Molecular , Compostos Fitoquímicos/isolamento & purificação , Compostos Fitoquímicos/farmacologia , Estereoisomerismo
7.
An Acad Bras Cienc ; 91(3): e20180621, 2019 Aug 12.
Artigo em Inglês | MEDLINE | ID: mdl-31411258

RESUMO

Aristolochia triangularis Cham., is one of the most frequently used medicinal plant in Southern Brazil. Preparations containing the leaves and/or stems are traditionally used as anti-inflammatory, diuretic, as well as antidote against snakebites. This study screened A. triangularis extracts, fractions and isolated compounds for different bioactivities. A weak antiproliferative activity against human lung cancer cell line (A549) was observed only for chloroform fraction obtained from stems (CFstems - CC50: 2.93 µg/mL). Also, a moderate antimicrobial activity against Staphylococcus aureus was detected just for chloroform fraction obtained from leaves (CFleaves -13-16 mm inhibition zone). Additionally, two semi-purified fractions (CFstems-4 and CFleaves-4) selectively inhibited HSV-1 replication (IC50 values of 0.40 and 2.61 µg/mL, respectively), while only CFleaves showed promising results against Leishmania amazonensis. Fractionation of extracts resulted in the isolation of one neolignan (-) cubebin and one lignan (+) galbacin. However, these compounds are not responsible for the in vitro bioactivities herein detected. The presence of aristolochic acid I and aristolochic acid II in the crude ethanol extract of stems (CEEstems) and leaves (CEEleaves) was also investigated. The HPLC analysis of these extracts did not display any peak with retention time or UV spectra comparable to aristolochic acids I and II.


Assuntos
Aristolochia/química , Compostos Fitoquímicos/química , Antibacterianos/farmacologia , Antifúngicos/farmacologia , Antiprotozoários/farmacologia , Antivirais/farmacologia , Ácidos Aristolóquicos/química , Brasil , Fracionamento Químico , Cromatografia Líquida de Alta Pressão/métodos , Humanos , Compostos Fitoquímicos/farmacologia , Extratos Vegetais/farmacologia
8.
Fitoterapia ; 137: 104262, 2019 Sep.
Artigo em Inglês | MEDLINE | ID: mdl-31284018

RESUMO

Eight undescribed 9,19-cycloartane type triterpenoid glycosides (cimdalglnoside A-H) and ten known analogues were obtained from the phytochemical research on the roots of Actaea dahurica (syn. Cimicifuga dahurica). All compounds were characterised by spectroscopic experiments, and chemical method. All the compounds isolated were assayed for cytotoxicity to five human cancer cell lines. Cimdalglnoside G showed promising cytotoxicities against Hela, and MCF-7 cell lines with IC50 values at 7.7 and 12.2 µM.


Assuntos
Actaea/química , Glicosídeos/farmacologia , Raízes de Plantas/química , Triterpenos/farmacologia , Antineoplásicos Fitogênicos/isolamento & purificação , Antineoplásicos Fitogênicos/farmacologia , China , Glicosídeos/isolamento & purificação , Células HeLa , Humanos , Células MCF-7 , Estrutura Molecular , Compostos Fitoquímicos/isolamento & purificação , Compostos Fitoquímicos/farmacologia , Triterpenos/isolamento & purificação
9.
Fitoterapia ; 137: 104261, 2019 Sep.
Artigo em Inglês | MEDLINE | ID: mdl-31284019

RESUMO

Three new sesquilignans, zijusesquilignans A-C (1-3), together with fifteen known compounds (4-18), were isolated from fruits of Ziziphus jujuba var. inermis Rehder (Rhamnaceae). Their chemical structures were established using spectroscopic analyses including 1D- and 2D-NMR, HR-EIMS, and ECD spectra. These compounds were assessed for their inhibitory effects on nitric oxide (NO) production. Of these compounds, 1-3 and 17 displayed inhibitory effects on NO production, with IC50 values ranging from 18.1 to 66.4 µM. Pretreatment with 1 and 17 significantly suppressed LPS-induced expression of nitric oxide synthase (iNOS) and cyclooxygenase-2 (COX-2) protein in cells. Moreover, compounds 1-3, 7, 9, and 17 exhibited cytotoxic activities against three human tumor cell lines, with IC50 values ranging from 8.4 to 44.9 µM.


Assuntos
Anti-Inflamatórios/farmacologia , Frutas/química , Lignanas/farmacologia , Ziziphus/química , Animais , Anti-Inflamatórios/isolamento & purificação , Antineoplásicos Fitogênicos/isolamento & purificação , Antineoplásicos Fitogênicos/farmacologia , Linhagem Celular Tumoral , Ciclo-Oxigenase 2/metabolismo , Humanos , Lignanas/isolamento & purificação , Camundongos , Estrutura Molecular , Óxido Nítrico/metabolismo , Óxido Nítrico Sintase Tipo II/metabolismo , Compostos Fitoquímicos/isolamento & purificação , Compostos Fitoquímicos/farmacologia , Células RAW 264.7 , República da Coreia
10.
Fitoterapia ; 137: 104263, 2019 Sep.
Artigo em Inglês | MEDLINE | ID: mdl-31295512

RESUMO

Chemical examination of the gum-resin of Boswellia carterii resulted in the isolation and characterization of eighteen new cembrane-type diterpenoids, named as Boscartins P-AG (1-18) and eight known ones. Their structures were established on the basis of extensive spectroscopic (2D NMR, IR, CD, MS and X-ray) analysis in combination with modified Mosher's method. All compounds featured unusual 1,12-oxygenated tetrahydrofuran functionalities, and were evaluated for hepatoprotective activity against D-galactosamine-induced HL-7702 cell damage and cytotoxic activity against MCF-7 human breast cancer cell in vitro. Compounds 1, 6-10, 12-13, 16-17 and 21-25 (10 µM) showed some hepatoprotective activity against D-galactosamine-induced HL-7702 cell damage.


Assuntos
Boswellia/química , Diterpenos/farmacologia , Resinas Vegetais/química , Linhagem Celular , China , Diterpenos/isolamento & purificação , Humanos , Células MCF-7 , Estrutura Molecular , Compostos Fitoquímicos/isolamento & purificação , Compostos Fitoquímicos/farmacologia
11.
Fitoterapia ; 137: 104264, 2019 Sep.
Artigo em Inglês | MEDLINE | ID: mdl-31299275

RESUMO

Five undescribed triterpene-type saponins, parkibicolorosides A-E, a cassane-type diterpene, and a known trimethoxy benzene glucoside were isolated from the roots of Parkia bicolor A. Chev. Their structures were elucidated by different spectroscopic methods including 1D- and 2D-NMR experiments as well as HR-ESI-MS analysis. Their cytotoxic activity against the chronic myeloid leukemia (K562) cell line was evaluated. The monosaccharides saponins exhibited a moderate antiproliferative activity with IC50 ranging from 48.49 ±â€¯0.16 to 81.66 ±â€¯0.17 µM.


Assuntos
Antineoplásicos Fitogênicos/farmacologia , Fabaceae/química , Raízes de Plantas/química , Saponinas/farmacologia , Triterpenos/farmacologia , Antineoplásicos Fitogênicos/isolamento & purificação , Costa do Marfim , Humanos , Células K562 , Estrutura Molecular , Compostos Fitoquímicos/isolamento & purificação , Compostos Fitoquímicos/farmacologia , Saponinas/isolamento & purificação , Triterpenos/isolamento & purificação
12.
Fitoterapia ; 137: 104265, 2019 Sep.
Artigo em Inglês | MEDLINE | ID: mdl-31302252

RESUMO

The aromatic plants of Vitex negundo var. heterophylla are not only herb medicine but also a functional food and an industrial crop. Its leaves can be used as a functional food for improving human's health, but the previous studies mainly focused on the volatile constituents, lignans, and iridoids. Our research led to the isolation of four new terpenoids (1-4), together with fifteen known compounds including seven flavonoids (9-15), two jasmonates (7-8) and six terpenoids (5-6, 16-19) from the leaves. Among all these compounds, 1, 2, 11, and 19 exhibited strong inhibitory activity against NO production in lipopolysaccharide (LPS)-induced RAW264.7 macrophage. The anti-inflammatory mechanism of the most active compound (2) is related to the inhibition of iNOS and COX-2, and the suppression of NF-κB pathway. Therefore, terpenoids and flavonoids from the leaves of Vitex negundo var. heterophylla might be used as potential anti-inflammatory candidates for developing medicine or value-added functional food.


Assuntos
Anti-Inflamatórios/farmacologia , Diterpenos/farmacologia , Norisoprenoides/farmacologia , Vitex/química , Animais , Anti-Inflamatórios/isolamento & purificação , China , Ciclo-Oxigenase 2/metabolismo , Diterpenos/isolamento & purificação , Interleucinas/metabolismo , Camundongos , Estrutura Molecular , Óxido Nítrico Sintase Tipo II/metabolismo , Norisoprenoides/isolamento & purificação , Compostos Fitoquímicos/isolamento & purificação , Compostos Fitoquímicos/farmacologia , Folhas de Planta/química , Células RAW 264.7
13.
Fitoterapia ; 137: 104268, 2019 Sep.
Artigo em Inglês | MEDLINE | ID: mdl-31306720

RESUMO

Solanum nigrum L. (also called as European black nightshade) has been traditionally used as folk medicine and food in some regions. Phytochemical investigations of the immature fruits of S. nigrum yielded five steroidal alkaloid glycosides (1-5), including an unprecedented nor-spirosolane type steroidal alkaloid with a five-membered ring A (1) and two novel spirosolane type steroidal alkaloid glycosides (2, 3), together with eight known phenolic compounds (6-13). Their structures were elucidated on the basis of spectroscopic and chemical methods, including IR, NMR, HR-ESI-MS, and GC analyses. Five steroidal alkaloid glycosides were tested for their potential antiproliferative effects against HL-60, U-937, Jurkat, K562, and HepG2 cell lines and inhibitory activities on nitric oxide (NO) production induced by lipopolysaccharide (LPS) in a macrophage cell line RAW 264.7. Compound 1 exhibited significant inhibition on NO production with an IC50 value of 23.4 ±â€¯2.0 µM, compared to positive control indomethacin (IC50, 47.40 ±â€¯4.50 µM). Compound 4 exhibited significant cytotoxicity against all tested cell lines.


Assuntos
Alcaloides/farmacologia , Glicosídeos/farmacologia , Solanum nigrum/química , Esteroides/farmacologia , Alcaloides/isolamento & purificação , Animais , Anti-Inflamatórios/isolamento & purificação , Anti-Inflamatórios/farmacologia , Antineoplásicos Fitogênicos/isolamento & purificação , Antineoplásicos Fitogênicos/farmacologia , Linhagem Celular Tumoral , China , Frutas/química , Glicosídeos/isolamento & purificação , Humanos , Camundongos , Estrutura Molecular , Óxido Nítrico/metabolismo , Compostos Fitoquímicos/isolamento & purificação , Compostos Fitoquímicos/farmacologia , Extratos Vegetais/química , Células RAW 264.7 , Esteroides/isolamento & purificação
14.
Fitoterapia ; 137: 104269, 2019 Sep.
Artigo em Inglês | MEDLINE | ID: mdl-31323238

RESUMO

The genus Amoora belongs to the Meliaceae family comprising approximately 25-30 species. Many Amoora species have been used as folk medicines for the treatment of many diseases. This review focuses on diverse chemical constituents from Amoora species as well as significant pharmacological activities. Up to now, a total of 140 compounds including eight sesquiterpenoids, twenty-six diterpenoids, forty-two triterpenoids, twenty-two limonoids, seven steroids, seven alkaloids, seven rocaglamide derivatives, four flavonoids, four glycosides, two coumarins, nine phenols, and two organic acids and esters were reported from Amoora species. Triterpenoids are characteristic components for Amoora species. The extracts and chemical constituents of Amoora species exhibit a broad spectrum of pharmacological activities including cytotoxic, anti-inflammatory, antibacterial and antifungal activity. The present review may provide useful evidence for reasonable utilization of Amoora species as folk medicines and further research in drug discovery.


Assuntos
Meliaceae/química , Compostos Fitoquímicos/farmacologia , Plantas Medicinais/química , Medicina Tradicional
15.
Fitoterapia ; 137: 104271, 2019 Sep.
Artigo em Inglês | MEDLINE | ID: mdl-31326416

RESUMO

Three new neolignan glycosides, (7R,8S)-4-hydroxy-3,3'-dimethoxy-8,4'-oxyneoligna-7,9,9'-triol-4-O-ß-d-glucopyranosyl-(1 → 4)-ß-D-glucopyranoside (1), (7R,8S)-4-hydroxy-3,5'-dimethoxy-4',7-epoxy-8,3'-neoligna-9,9'-diol-9'-O-ß-d-glucopyranosyl-4-O-[ß-d-glucopyranosyl-(1 → 4)]-ß-D-glucopyranoside (2), and (7R,8S)-4-hydroxy-3,5,5'-trimethoxy-4',7-epoxy-8,3'-neoligna-9,9'-diol-9'-O-ß-d-glucopyranosyl-4-O-[ß-d-glucopyranosyl-(1 → 4)]-ß-D-glucopyranoside (3), one new phenolic glycoside, securiphenoside B (4) and two new hemiterpene glycosides, securiterpenoside E-F (5-6) were isolated from the stems of Securidaca inappendiculata Hassk. Their structures were elucidated on the basis of 1D and 2D NMR, HRESIMS, CD and chemical evidence. Furthermore, compound 2 showed moderate hepatoprotective activity compared with bicyclol in vitro.


Assuntos
Glicosídeos/farmacologia , Caules de Planta/química , Securidaca/química , China , Glicosídeos/isolamento & purificação , Células Hep G2 , Humanos , Estrutura Molecular , Compostos Fitoquímicos/isolamento & purificação , Compostos Fitoquímicos/farmacologia
16.
Fitoterapia ; 137: 104275, 2019 Sep.
Artigo em Inglês | MEDLINE | ID: mdl-31351126

RESUMO

The non-small cell lung cancer (NSCLC) represents a malignant type of cancer worldwide. The atalantraflavone (AFL) is a natural product isolated from leaves of Atalantia monophylla (L.) DC. However, the function of atalantraflavone in NSCLC is still elusive. In present work, we have unraveled a novel function of AFL in NSCLC. AFL significantly inhibited NSCLC cell viability and colony formation. AFL increased sub-G1 fraction and apoptotic rates in a dose-dependent manner. Furthermore, Twist-related protein 1 (Twist1) was identified as the target of AFL. The association between AFL and Twist1 markedly decreased the stability of Twist1 via elevated ubiquitin mediated proteasomal degradation. AFL induced NSCLC suppression was mediated by Twist1 as Twist1 overexpression could partially reverse the inhibitory effect of AFL on migration and metastasis. Furthermore, AFL could also sensitize NSCLC cells to cisplatin treatment and consistently impair NSCLC proliferation and metastasis. Our current data have identified a tumor suppressive function for AFL in NSCLC by increasing Twist1 degradation. Therefore, the anti-tumor activity of AFL might provide critical insight into pharmaceutic lung cancer intervention to overcome cisplatin resistance.


Assuntos
Antineoplásicos Fitogênicos/farmacologia , Carcinoma Pulmonar de Células não Pequenas/patologia , Flavonas/farmacologia , Proteínas Nucleares/antagonistas & inibidores , Rutaceae/química , Proteína 1 Relacionada a Twist/antagonistas & inibidores , Antineoplásicos Fitogênicos/isolamento & purificação , Apoptose , Carcinoma Pulmonar de Células não Pequenas/tratamento farmacológico , Linhagem Celular Tumoral , Cisplatino , Resistencia a Medicamentos Antineoplásicos , Flavonas/isolamento & purificação , Humanos , Compostos Fitoquímicos/isolamento & purificação , Compostos Fitoquímicos/farmacologia , Folhas de Planta/química , Estabilidade Proteica
17.
Fitoterapia ; 137: 104277, 2019 Sep.
Artigo em Inglês | MEDLINE | ID: mdl-31351127

RESUMO

Five new Lycopodium alkaloids, huperzine Y1 (1), huperzine Y2 (2), huperzine Y3 (3), (+)-huperzine Z (4a) and (-)-huperzine Z (4b) as well as ten known alkaloids (5-14) were isolated from Huperzia serrata. The structures of the new compounds were established using extensive spectroscopic (1D and 2D NMR, IR, and HRESIMS) and calculated electronic circular dichroism (ECD) methods. Compounds 4a and 4b were a pair of enantiomers successfully separated by chiral HPLC resolution. Compounds 2 and 3 indicated inhibitory activities against acetylcholinesterase with IC50 value of 57.1 ±â€¯1.6 and 32.7 ±â€¯1.0 µΜ, respectively. However, no compound showed inhibitory effect on butyrocholinesterase at the concentration of 100 µΜ.


Assuntos
Alcaloides/farmacologia , Huperzia/química , Acetilcolinesterase , Alcaloides/isolamento & purificação , Butirilcolinesterase , China , Inibidores da Colinesterase/isolamento & purificação , Inibidores da Colinesterase/farmacologia , Estrutura Molecular , Compostos Fitoquímicos/isolamento & purificação , Compostos Fitoquímicos/farmacologia
18.
Xi Bao Yu Fen Zi Mian Yi Xue Za Zhi ; 35(6): 526-532, 2019 Jun.
Artigo em Chinês | MEDLINE | ID: mdl-31292057

RESUMO

Objective To investigate the effect and mechanism of Trillium saponins on the invasion and migration of HuH-7 cells regulated by human ß-defensin 2 (HBD-2). Methods HuH-7 cells were treated with 0.5, 1.0, 2.0, 4.0 mg/L Trillium saponins. Cell proliferation was detected by MTT assay. TranswellTM chamber was used to measure cell invasion and migration. The levels of matrix metalloproteinase-2 (MMP2), HBD-2 and matrix metalloproteinase-9 (MMP9) were detected by Western blot analysis. HBD-2 small interfering RNA (siRNA) was transfected into HuH-7 cells. The interference effect of Trillium saponins treatment was verified by real-time quantitative PCR and Western blot analysis, and TranswellTM assay was used to detect cell invasion and migration. Results Except that 0.5 mg/L Trillium saponins had no effect on the proliferation of HuH-7 cells, the proliferation of HuH-7 cells was inhibited by all other doses of Trillium saponins. (0.5, 1.0) mg/L of Trillium saponins down-regulated the levels of MMP2 and MMP9 proteins, increased the level of HBD-2 protein and inhibited cell invasion, migration. HBD-2 siRNA transfection significantly reduced the level of HBD-2 in HuH-7 cells. Down-regulation of HBD-2 increased the invasive, migratory ability and increased the levels of MMP2 and MMP9 proteins in HuH-7 cells treated with Trillium saponins. Conclusion Trillium saponins can inhibit the invasion and migration of HuH-7 cells by promoting the expression of HBD-2.


Assuntos
Invasividade Neoplásica , Saponinas/farmacologia , Trillium/química , beta-Defensinas/metabolismo , Linhagem Celular Tumoral , Movimento Celular , Humanos , Metaloproteinase 2 da Matriz/metabolismo , Metaloproteinase 9 da Matriz/metabolismo , Compostos Fitoquímicos/farmacologia
19.
Fitoterapia ; 137: 104254, 2019 Sep.
Artigo em Inglês | MEDLINE | ID: mdl-31271782

RESUMO

Five new polyphenolic derivatives, sepiumols A-E (1-5), were isolated from the root barks of Periploca sepium. Their structures were elucidated by interpretation of NMR spectroscopic and mass spectrometric data. Compounds 1, 3 and 5 were found to exhibit significant antifungal activity, particularly for 3 with the remarkable activity against Gibberella saubinetii and Alternaria longipes with MIC values of 1.56 and 3.13 µg/mL (ketoconazole: 0.78 µg/mL), respectively. In addition, compounds 1, 3 and 5 also displayed significant antibacterial activity against methicillin-resistant Staphylococcus aureu with MIC values of 12.50-25 µg/mL (ciprofloxacin: 0.78 µg/mL).


Assuntos
Antibacterianos/farmacologia , Antifúngicos/farmacologia , Periploca/química , Polifenóis/farmacologia , Alternaria/efeitos dos fármacos , Antibacterianos/isolamento & purificação , Antifúngicos/isolamento & purificação , Gibberella/efeitos dos fármacos , Staphylococcus aureus Resistente à Meticilina/efeitos dos fármacos , Estrutura Molecular , Compostos Fitoquímicos/isolamento & purificação , Compostos Fitoquímicos/farmacologia , Casca de Planta/química , Raízes de Plantas/química , Polifenóis/isolamento & purificação
20.
Fitoterapia ; 137: 104251, 2019 Sep.
Artigo em Inglês | MEDLINE | ID: mdl-31271783

RESUMO

The MeOH extract from leaves of Saururus cernuus L. (Saururaceae) displayed in vitro activity against trypomastigote forms of T. cruzi (100% of parasite death at 200 µg/mL), suggesting the presence of bioactive compounds. Thus, the bioactivity-guided fractionation was carried out, leading to the isolation of three related neolignan derivatives, identified as threo-austrobailignan-5 (1), threo-austrobailignan-6 (2), and threo-dihydroguaiaretic acid (3). Anti-T. cruzi activity of compounds 1-3 was performed against cell-derived trypomastigotes and intracellular amastigotes. Additionally, the mammalian cytotoxicity was investigated using NCTC cells. Compound 2 was the most effective against extracellular trypomastigotes with IC50 of 3.7 µM, while compound 3 showed activity in both clinically relevant forms of the parasite, trypomastigotes and amastigotes, with IC50 values of 7.0 and 16.2 µM, respectively. However, the structurally related compound 1 was inactive. Based on these results, compounds 2 and 3 were selected to evaluate the mechanism of cellular death. Compound 2 induced alteration in the plasma membrane permeability and consequently in the ROS levels after 120 min of incubation. By using flow cytometry and fluorescence microscopy, compound 3 showed alterations in the mitochondrial membrane potential (ΔΨm) of trypomastigotes. Considering the promising chemical and biological properties of neolignans 2 and 3, these compounds could be used as starting points to develop new lead compounds for Chagas disease.


Assuntos
Lignanas/farmacologia , Potencial da Membrana Mitocondrial/efeitos dos fármacos , Saururaceae/química , Tripanossomicidas/farmacologia , Trypanosoma cruzi/efeitos dos fármacos , Animais , Brasil , Células Cultivadas , Guaiacol/análogos & derivados , Lignanas/isolamento & purificação , Macrófagos Peritoneais/parasitologia , Camundongos Endogâmicos BALB C , Estrutura Molecular , Compostos Fitoquímicos/isolamento & purificação , Compostos Fitoquímicos/farmacologia , Folhas de Planta/química , Espécies Reativas de Oxigênio/metabolismo , Tripanossomicidas/isolamento & purificação
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