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1.
Chem Biodivers ; 17(2): e1900656, 2020 Feb.
Artigo em Inglês | MEDLINE | ID: mdl-31910318

RESUMO

The Cunila angustifolia essential oil was obtained from fresh leaves by hydrodistillation and analyzed by GC-FID and GC-MS to determine its chemical composition. The essential oil presented pulegone (29.5 %) and isomenthol (27.0 %) as major components, and other compounds such as menthone (8.6 %), neomenthol (7.2 %), menthyl acetate (2.5 %) and caryophyllene oxide (2.0 %) were identified. The cytotoxic activity of the essential oil was evaluated by MTS assay, with the human cancer cell lines of the lung (A549), breast (MCF-7) and skin melanoma (SK-Mel-28). The assay showed the highest selectivity, to MCF-7 cell lines, with IC50 equal to 34.0 µg mL-1 , low selectivity for SK-Mel-28 cell lines, with IC50 equal to 279.9 µg mL-1 , and no mortality to A549 cell lines.


Assuntos
Lamiaceae/química , Óleos Voláteis/química , Linhagem Celular Tumoral , Sobrevivência Celular/efeitos dos fármacos , Cromatografia Gasosa-Espectrometria de Massas , Humanos , Lamiaceae/metabolismo , Óleos Voláteis/análise , Óleos Voláteis/farmacologia , Folhas de Planta/química , Folhas de Planta/metabolismo
2.
Food Chem Toxicol ; 135: 110940, 2020 Jan.
Artigo em Inglês | MEDLINE | ID: mdl-31693914

RESUMO

Eplingiella fruticosa (Lamiaceae), formally known as Hyptis fruticosa, is an important aromatic medicinal herb used in folk medicine in northeastern Brazil. We aimed to evaluate the anti-hyperalgesic effect of essential oil obtained from E. fruticosa (HypEO) complexed with ßCD (HypEO-ßCD) in a chronic widespread non-inflammatory muscle pain animal model (a mice fibromyalgia-like model, FM). The HypEO was extracted by hydro distillation and its chemical composition was determined by GC-MS/FID. Moreover, Fos protein expression in the spinal cord was assessed by immunofluorescence. (E)-caryophyllene, bicyclogermacrene, 1,8-cineole, α-pinene, ß-pinene and 21 other compounds were identified in the HypEO. The treatment with HypEO-ßCD produced a longer-lasting anti-hyperalgesic effect compared to HypEO, without alterations in motor coordination or myorelaxant effects. Moreover, HypEO and HypEO-ßCD produced a significant anti-hyperalgesic effect over 7 consecutive treatment days. Immunofluorescence assay demonstrated a decrease in Fos protein expression in the spinal cord (p < 0.001). We demonstrated that the anti-hyperalgesic effect produced by HypEO was improved after complexation with ß-CD and this seems to be related to the central pain-inhibitory pathway, suggesting the possible use of E. fruticosa for chronic pain management.


Assuntos
Analgésicos/uso terapêutico , Hiperalgesia/tratamento farmacológico , Lamiaceae/química , Mialgia/tratamento farmacológico , Óleos Voláteis/uso terapêutico , beta-Ciclodextrinas/uso terapêutico , Analgésicos/isolamento & purificação , Animais , Masculino , Camundongos , Óleos Voláteis/isolamento & purificação , Folhas de Planta/química , Proteínas Proto-Oncogênicas c-fos/metabolismo , Medula Espinal/efeitos dos fármacos , Medula Espinal/metabolismo
3.
Phytochemistry ; 170: 112198, 2020 Feb.
Artigo em Inglês | MEDLINE | ID: mdl-31765875

RESUMO

Fungal endophytes from plants are an important source for discovery of novel bioactive natural products. In this study, five undescribed harziane diterpenoids with a 4/7/5/6 tetracyclic scaffold, harzianols F‒J and three known derivatives, were obtained from the liquid fermentation of an endophytic fungus Trichoderma atroviride B7, which was isolated from the healthy flower of a Lamiaceae plant Colquhounia coccinea var. mollis. Their structures were elucidated by comprehensive spectroscopic analyses and X-ray crystallographic diffraction in the case of harzianol F. Harzianol I exhibited significant antibacterial effect against the growth of Staphylococcus aureus (EC50 = 7.7 ± 0.8 µg/mL), Bacillus subtilis (EC50 = 7.7 ± 1.0 µg/mL), and Micrococcus luteus (EC50 = 9.9 ± 1.5 µg/mL). Meanwhile, cytotoxic activity of harzianol I against three cancer cell lines was also observed. A plausible biosynthetic pathway for harziane diterpenoids was proposed.


Assuntos
Antibacterianos/farmacologia , Diterpenos/farmacologia , Lamiaceae/química , Compostos Fitoquímicos/farmacologia , Trichoderma/química , Antibacterianos/química , Antibacterianos/isolamento & purificação , Bacillus subtilis/efeitos dos fármacos , Diterpenos/química , Diterpenos/isolamento & purificação , Relação Dose-Resposta a Droga , Testes de Sensibilidade Microbiana , Micrococcus luteus/efeitos dos fármacos , Conformação Molecular , Compostos Fitoquímicos/química , Compostos Fitoquímicos/isolamento & purificação , Staphylococcus aureus/efeitos dos fármacos
4.
Food Chem Toxicol ; 134: 110841, 2019 Dec.
Artigo em Inglês | MEDLINE | ID: mdl-31568851

RESUMO

Clinopodium vulgare L. (Lamiaceae) was used in the traditional Bulgarian medicine for treatment of wounds, diabetes and gastric ulcers. In this study we aimed at safety assessment of C. vulgare lyophilized water extract (CVE) characterized by ultra high-performance liquid chromatography-Orbitrap high resolution mass spectrometry (UHPLC-HRMS). The acute and sub-acute toxicity of CVE was determined in two rodent species (mice and rats), and two routes of administration - intraperitoneal (i.p.) and oral (p.o.). LD50 (i.p.), were found to be 675 mg/kg (mice) and 500 mg/kg (rats). An acute i. p. administration resulted in central nervous system toxic effects. LD50 (p.o.) was higher than 2000 mg/kg for both species. In sub-acute oral administration, CVE did not exert any toxic effect on hematology, blood and urine biochemistry, and histomorphology in pancreas, liver, spleen and kidney. In addition, based on accurate masses, MS/MS and comparison with standards, a variety of flavonoids, caffeic acid oligomers and saponins were tentatively elucidated in CVE. Rosmarinic acid was the major compound. In conclusion, CVE did not cause hematological, biochemical and histopathological changes after oral administration and it is safe for internal use. The obtained UHPLC-HRMS profile revealed CVE as a new rich source of water soluble caffeic acid oligomers.


Assuntos
Cromatografia Líquida de Alta Pressão/métodos , Lamiaceae/química , Extratos Vegetais/toxicidade , Espectrometria de Massas em Tandem/métodos , Administração Oral , Animais , Relação Dose-Resposta a Droga , Feminino , Injeções Intraperitoneais , Camundongos , Camundongos Endogâmicos ICR , Extratos Vegetais/administração & dosagem , Extratos Vegetais/análise , Ratos , Ratos Wistar
5.
Chem Biodivers ; 16(12): e1900434, 2019 Dec.
Artigo em Inglês | MEDLINE | ID: mdl-31587473

RESUMO

Terpenes are a widespread group of secondary metabolites that can be found in various family plants such as the Lamiaceae. In view of their numerous valuable biological activities, the industrial production of concrete terpenes and essential oils rich in the substances is intensively studied. Monoterpenes constitute a significant part of the whole group of the aforementioned secondary metabolites. This is due to their numerous biological activities and their ability to permeate the skin. Despite the fact that these substances have gain popularity, they are not comprehensively characterized. The presented review is based on studies of the biological activities of the most important monoterpenes and the essential oils rich in these compounds. The authors focused attention on antioxidant activity, inhibition towards acetyl- and butyrylcholinesterase, and α-amylase and α-glucosidase, antifungal, hepatoprotective, sedative properties, and their skin permeation enhancement.


Assuntos
Monoterpenos/química , Doença de Alzheimer/tratamento farmacológico , Doença de Alzheimer/patologia , Animais , Antioxidantes/química , Colinesterases/química , Colinesterases/metabolismo , Lamiaceae/química , Lamiaceae/metabolismo , Monoterpenos/farmacologia , Monoterpenos/uso terapêutico , Fator 2 Relacionado a NF-E2/química , Fator 2 Relacionado a NF-E2/metabolismo , Óleos Voláteis/química , Estresse Oxidativo/efeitos dos fármacos
6.
Zhongguo Zhong Yao Za Zhi ; 44(15): 3178-3186, 2019 Aug.
Artigo em Chinês | MEDLINE | ID: mdl-31602870

RESUMO

Ziziphora bungeana is a kind of medicinal plants belongs to Labiatae,and it also a kind of geoherbs in Xinjiang. The main active ingredient linarin has a higher content in inflorescence than in other parts. In this study,high-throughput sequencing technology was used to reveal the transcriptome of the inflorescence of Z. bungeana,77 366 unigenes were acquired,of which 56 375 unigenes were annotated based on search of the database and classification. Through the analysis of metabolic pathways,sixty unigenes were probably encoding some enzymes involved in the flavonoid biosynthesis pathways. The contents of linarin in different parts were determined and the key genes were verified by qRT-PCR. The discovery provides the research basis for further analysis of the enzyme genes involved in the biosynthesis of the major flavonoid components in Z. bungeana.


Assuntos
Flavonoides/biossíntese , Lamiaceae/química , Transcriptoma , Perfilação da Expressão Gênica , Sequenciamento de Nucleotídeos em Larga Escala
7.
Biomed Pharmacother ; 117: 109156, 2019 Sep.
Artigo em Inglês | MEDLINE | ID: mdl-31387192

RESUMO

The present study was designed to study the protective effect of Ziziphora clinopodioides flavonoids (ZCF) against H2O2-induced oxidative stress in HUVEC cells. MTT assay was carried out to determine the cell viability of HUVEC cells following pretreatment with ZCF. Fluorescent microscopy measurements were performed to evaluate apoptosis of HUVEC cells. Furthermore, the effects of ZCF on the activities of antioxidants superoxide dismutase (SOD), glutathione peroxidase (GSH-Px), catalase (CAT), malondialdehyde production (MDA) and lactic dehydrogenase (LDH) levels were analyzed. Apoptosis was observed by Hoechst33258 staining and AO staining. Real-time fluorescence quantitative polymerase chain reaction (Real-time PCR) was used to detect the expression of B-cell lymphoma/leukemia-2 (Bcl-2), Bcl-2-associated X protein (Bax) and aspartate proteolytic enzyme-3 (Caspase-3) mRNA. The expression of vascular endothelial growth factor receptor 2 (VEGFR2), protein kinase B (Akt), phosphorylated protein kinase B (p-Akt), Bax, Bcl-2 and Caspase-3 were detected by western blot. ZCF attenuated H2O2-induced cell death, as determined by the MTT assay. ZCF decreased malondialdehyde and lactic dehydrogenase levels, increased superoxide dismutase, glutathione peroxidase, catalase activities and inhibited apoptosis. Moreover, pretreatment with ZCF decreased the expression of Bax and Caspase-3 at mRNA level, increased the expression of Bcl-2 mRNA level, decreased the levels of VEGFR2, Bax and Caspase-3 protein, and increased the level of p-Akt / Akt and Bcl-2 protein in HUVEC cells. These results suggested that ZCF protected against H2O2-induced injury in HUVEC cells. The mechanism for this effect is related to the enhancement of antioxidant capacity, suppression of angiogenesis and apoptosis.


Assuntos
Flavonoides/farmacologia , Células Endoteliais da Veia Umbilical Humana/efeitos dos fármacos , Lamiaceae/química , Estresse Oxidativo/efeitos dos fármacos , Substâncias Protetoras/farmacologia , Antioxidantes/metabolismo , Apoptose/efeitos dos fármacos , Catalase/metabolismo , Morte Celular/efeitos dos fármacos , Linhagem Celular , Sobrevivência Celular/efeitos dos fármacos , Células Endoteliais da Veia Umbilical Humana/metabolismo , Humanos , Peróxido de Hidrogênio/farmacologia , Oxirredução/efeitos dos fármacos , Proteínas Proto-Oncogênicas c-bcl-2/metabolismo , Superóxido Dismutase/metabolismo , Fator A de Crescimento do Endotélio Vascular/metabolismo , Proteína X Associada a bcl-2/metabolismo
8.
Chem Biodivers ; 16(9): e1900254, 2019 Sep.
Artigo em Inglês | MEDLINE | ID: mdl-31381251

RESUMO

The genus Thymus (Lamiaceae) comprises about 214 species throughout the world, mainly found in North Africa, Europe, and temperate Asia zone. They are traditionally used as food additives and folk medicines. This review comprehensively summarizes information about traditional uses, chemical constituents, and biological activities of this genus and provides recommendations for future investigations. All information was gathered from scientific databases including Google Scholar, Sci-Finder, Web of Science, ScienceDirect, and CNKI. Volatile oils are the most concerned constituents of this genus. Flavonoids, phenylpropanoids, tannins, organic acids, terpenoids, and phytosterols were also summarized. This genus plants possessed a variety of activities including antimicrobial, antioxidant, anti-inflammatory, cytotoxic, analgesic, and antidiabetic. In brief, this review will be helpful to provide valuable data for explorations and create more interests towards Thymus genus in the future.


Assuntos
Anti-Infecciosos/farmacologia , Anti-Inflamatórios/farmacologia , Antineoplásicos Fitogênicos/farmacologia , Antioxidantes/farmacologia , Hipoglicemiantes/farmacologia , Lamiaceae/química , Animais , Anti-Infecciosos/química , Anti-Infecciosos/isolamento & purificação , Anti-Inflamatórios/química , Anti-Inflamatórios/isolamento & purificação , Antineoplásicos Fitogênicos/química , Antineoplásicos Fitogênicos/isolamento & purificação , Antioxidantes/química , Antioxidantes/isolamento & purificação , Humanos , Hipoglicemiantes/química , Hipoglicemiantes/isolamento & purificação
9.
Comp Immunol Microbiol Infect Dis ; 66: 101335, 2019 Oct.
Artigo em Inglês | MEDLINE | ID: mdl-31437681

RESUMO

Hydatidosis caused by Echinococcus granulosus is a major zoonotic diseases. In addition to imposing heavy economic losses, the disease is a public health problem worldwide. The larval stage of the parasite (hydatid cyst) is formed in a wide range of domestic, wild and human beings as intermediate hosts. On the other, its recurrence has been reported anywhere as a reemerging disease. Although the cysts have some evading mechanisms, both human TH1 and TH2 cells subsets are stimulated. Because of increasing resistance and adverse effects of medications such as abnormalities of liver and other organs functions and abdominal pain, seeking alternative therapeutic approaches to be inexpensive, easy available, with low side effects and toxicity seems essential. However, the lack of information on the social and economic welfares of herbal medicines for the industrial scale application is a limitation. Zataria Multiflora bois (ZMB) has exhibited huge advantages and tremendous protoscolicidal effects as demonstrated by numerous studies and its combination therapies with anti-parasitic drugs have exerted desirable outcomes in vitro and in vivo. Noticeably, the compound confers negligible side effects or toxicity even at high concentrations. ZMB has exhibited promising inhibitory effects against hydatid cyst, particularly when combined with chemical drugs and in formulations of nanoemulsions. Its immunomodulatory effects include increase of nitric oxide production (NO) and protection of hepatic cells (Kupffer cells, fat-storing cells, and endothelial cells), enhancement of macrophages and T cells and increase of cytokines production. This study aimed at assessment of ZMB traits for application against hydatid cyst protoscolices.


Assuntos
Equinococose/tratamento farmacológico , Echinococcus granulosus/efeitos dos fármacos , Células Endoteliais/parasitologia , Lamiaceae/química , Animais , Equinococose/imunologia , Echinococcus granulosus/imunologia , Humanos , Imunomodulação , Larva/efeitos dos fármacos , Fígado/efeitos dos fármacos , Fígado/parasitologia , Extratos Vegetais , Linfócitos T/imunologia
10.
Fitoterapia ; 138: 104345, 2019 Oct.
Artigo em Inglês | MEDLINE | ID: mdl-31470063

RESUMO

The present study reports the phytochemical investigation of n-butanol-soluble extracts of Glechoma longituba. Five new oleanane-type triterpenoid saponins with an 11α, 12α-epoxy unit, named glechomanosides A - E, were isolated from the n-butanol soluble fraction of G. longituba. Their chemical structures were established using HRESIMS, IR, 1D NMR, and 2D NMR techniques. The compounds were all evaluated for their antithrombus activities by monitoring thrombin time (TT), prothrombin time (PT), activated partial thromboplastin time (APTT), and antiplatelet aggregation assays. These results suggest that G. longituba might be a candidate plant source of an interesting antithrombotic activity.


Assuntos
Plaquetas/efeitos dos fármacos , Lamiaceae/química , Ácido Oleanólico/análogos & derivados , Saponinas/farmacologia , Animais , China , Feminino , Masculino , Camundongos , Estrutura Molecular , Ácido Oleanólico/isolamento & purificação , Ácido Oleanólico/farmacologia , Tempo de Tromboplastina Parcial , Compostos Fitoquímicos/isolamento & purificação , Compostos Fitoquímicos/farmacologia , Agregação Plaquetária , Tempo de Protrombina , Coelhos , Saponinas/isolamento & purificação , Tempo de Trombina
11.
BMC Complement Altern Med ; 19(1): 173, 2019 Jul 12.
Artigo em Inglês | MEDLINE | ID: mdl-31299960

RESUMO

BACKGROUND: This study was aimed to determination the tumor inhibitory effect and explore the potential mechanisms of Lagopsis supine ethanol extract (Ls) on colorectal cancer. METHODS: The cell growth inhibition experiment of Ls in colorectal cancer cell lines was determined by MTT method in the time course of 24, 48 and 72 h in four gradient drug concentrations. The protein expression levels of pSTAT3, pJAK2, STAT3, JAK2, Bcl-2 and caspase 3 were measured by Western blot method. The mRNA levels of the downstream genes of STAT3 were detected through semi-quantitative RT PCR. Sixty Balb/c-nude mice were xenograft with HCT116 colorectal cancer cells through subcutaneously. The xenografts were divided into five groups: model group, positive group (capecitabine 300 mg/kg) and three dosages of Ls treated groups (75, 150 and 300 mg/kg). Tumor size and tumor weight were calculated for evaluation the anti-tumor effects. H & E staining and immunohistochemical analysis were used to determine the histopathological changes and the levels of pSTAT3 and pJAK2 in the tumor tissues. RESULTS: Ls exhibited a significant anti-proliferation effect in HCT116 and SW480 cells in vitro. The protein levels of pSTAT3, pJAK2 and Bcl-2, and the mRNA levels of Bcl-2 and Bak notably reduced with a dose-dependent manner. While the protein levels of caspase 3, and mRNA levels of Bax and caspase-3 remarkably increased in the gradient dosage of Ls in HCT116 cells. HCT116 in vivo xenografts experiment showed that the growth of the tumors significantly inhibited by Ls administration, which with no any significant body weight changes in each experiment group. The histopathology analysis displayed that Ls significantly reduced the inflammatory cells in tumor tissue. Furthermore, Ls also significantly down-regulate the protein levels of pSTAT3 and pJAK2 in the tumor tissues, compared with the model group. CONCLUSIONS: This work shows that Ls inhibited the cell proliferation of colorectal cancer in vitro and significantly reduced the tumor growth in HCT116 xenografts in vivo, which is probably related with the JAK/STAT signal pathway.


Assuntos
Antineoplásicos Fitogênicos/uso terapêutico , Neoplasias Colorretais/tratamento farmacológico , Medicamentos de Ervas Chinesas/uso terapêutico , Lamiaceae/química , Animais , Antineoplásicos Fitogênicos/isolamento & purificação , Linhagem Celular Tumoral , Neoplasias Colorretais/metabolismo , Neoplasias Colorretais/patologia , Humanos , Masculino , Camundongos Endogâmicos BALB C , Camundongos Nus , Proteínas de Neoplasias/biossíntese , Ensaios Antitumorais Modelo de Xenoenxerto
12.
Curr Pharm Biotechnol ; 20(12): 1064-1071, 2019.
Artigo em Inglês | MEDLINE | ID: mdl-31333125

RESUMO

BACKGROUND: Biodegradable films are appropriate alternatives to synthetic polymers due to their potential to enhance food safety and their function as a carrier for wide a range of food additives especially natural antioxidants. OBJECTIVE: The aim of this study was to compare the potential antioxidant activities of sodium alginate films containing resveratrol (RES) alone and in combination with Zataria multiflora essential oil (ZEO) using an in vitro model. METHODS: At first, the major chemical compositions of ZEO were evaluated by GC/MS. Then, the amount of phenolic compounds of sodium alginate films were evaluated by total phenolic contents assay and antioxidant activities of films were evaluated by 2,2-Diphenyl-1-picrylhydrazyl (DPPH) and 2,2'-azino-bis (3-ethylbenzothiazoline-6-sulfonic acid) (ABTS) assays. Finally, the concentrations of ZEO and RES which showed better antioxidant activities in sodium alginate films were incorporated to films in combination forms to evaluate their synergistic effects. RESULTS: According to gas chromatography-mass spectrometry (GC/MS) analysis, 35 compounds of ZEO were identified and Thymol (37.94%), p-Cymene (9.50%) and 3-Carene (4.98%) were the most important compounds of essential oil, respectively. The results of the radical scavenging evaluations, showed better antioxidant activities of the films containing RES than the films containing ZEO and Butylated hydroxytoluene (BHT). Also, the combined uses of ZEO and RES into alginate films had the synergistic effects (P<0.05). CONCLUSION: Therefore, it can be concluded that alginate films incorporated with the combination of ZEO and RES is the appropriate option to postpone the oxidative reactions and can be used as natural antioxidant in the food packaging industry.


Assuntos
Alginatos/química , Antioxidantes/química , Embalagem de Alimentos/métodos , Lamiaceae/química , Óleos Voláteis/química , Resveratrol/química , Sinergismo Farmacológico , Embalagem de Alimentos/normas , Inocuidade dos Alimentos , Cromatografia Gasosa-Espectrometria de Massas
13.
Res Vet Sci ; 125: 333-344, 2019 Aug.
Artigo em Inglês | MEDLINE | ID: mdl-31352282

RESUMO

Minthostachys verticillata essential oil (EO) is a natural product that reports immunomodulatory effects on human T cells as well as anti-inflammatory activity. Bovine mastitis is a worldwide disease, mainly caused by bacteria, affecting milk quality and yield, leading to high economic losses. Environmental pathogens, as Enterococcus faecium, are implicated in the disease. Antibiotic therapy is adequate, although it can leave residues in milk, causing problems in human health. The search of immunomodulatory substances for bovine mastitis treatment is a promising alternative strategy. The aim of this study was to characterize the effect of M. verticillata EO on macrophage phagocytosis and evaluate its immunomodulatory and protective effects in mice challenged with E. faecium. The results showed that EO activated macrophage phagocytosis mechanisms inducing reactive oxygen species production. Moreover, EO modulated the innate immune response in mammary glands of female Balb/c mice challenged with E. faecium decreasing the infiltration of polymorphonuclear neutrophils and IL-1ß and TNF-α mRNA expression. In addition, EO increased the expression of IL-10 in the last hours of infection. Treatment with EO did not increase the number of activated CD4+ or CD8+ T cells or the production of specific antibodies. These results suggest that EO play an important role in helping to resolve the infection in the first hours without activating adaptive immunity. In addition, a marked decrease of the bacterial count in the glands of mice treated with EO was observed. A natural product such as M. verticillata EO could have a potential use to control bovine mastitis.


Assuntos
Enterococcus faecium/fisiologia , Imunidade Inata/efeitos dos fármacos , Lamiaceae/química , Macrófagos/efeitos dos fármacos , Mastite Bovina/tratamento farmacológico , Óleos Voláteis/farmacologia , Fagocitose/efeitos dos fármacos , Animais , Bovinos , Feminino , Fatores Imunológicos/farmacologia , Macrófagos/imunologia , Mastite Bovina/microbiologia , Camundongos , Camundongos Endogâmicos BALB C , Óleos Voláteis/química , Substâncias Protetoras/farmacologia
14.
Phytomedicine ; 63: 153037, 2019 Oct.
Artigo em Inglês | MEDLINE | ID: mdl-31357075

RESUMO

BACKGROUND: Non-Small-Cell Lung Cancer (NSCLC) is the most-frequent cause of cancer death, and novel chemotherapeutic drugs for treating NSCLC are urgently needed. 2α, 3α, 23-trihydroxy-13α, 27-cyclours-11-en-28-oic acid (euscaphic acid G) is a new hexacyclic triterpene acid isolated by our group from Glechoma longituba (Nakai) Kupr. However, the underlying mechanisms responsible for the anticancer effects of hexacyclic triterpene acid have not been elucidated. PURPOSE: In the present work, we evaluated growth inhibitory effect of the new isolated hexacyclic triterpene acid and explored the underlying molecular mechanisms. METHODS/STUDY DESIGNS: Herbs were extracted and constituents were purified by chromatographic separation, including silica gel, ODS, MCI, Sephadex LH-20 and preparative HPLC. The compound structures were elucidated by the use of UV, NMR and MS spectral data. The anticancer activity of euscaphic acid G was evaluated by MTT assay. Cell cycle, apoptosis, reactive oxygen species and mitochondrial membrane potential were determined by flow cytometry. To display the possible mechanism of euscaphic acid G on NCI-H460 cells, RT-PCR, immunofluorescence and Western blot analysis were carried out. RESULTS: A new hexacyclic triterpene acid, euscaphic acid G, together with fifteen known triterpenoids, was isolated from the aerial parts of G. longituba. Our results showed that euscaphic acid G exerted strong anti-proliferative activity against NCI-H460 cells in a concentration- and time-dependent manner. Flow cytometry demonstrated euscaphic acid G arrested the cell cycle at G1 phase, induced cellular apoptosis, accompanied by ROS generation and mitochondrial membrane potential reduction. Mechanistic studies revealed that euscaphic acid G treatment inhibited IKKα/ß phosphorylation and IκBα phosphorylation, which subsequently caused the blockage of NF-κB p65 phosphorylation and nuclear translocation. CONCLUSION: In conclusion, these results suggested that euscaphic acid G from G. longituba showed potential anticancer effects against lung cancer cells via inducing cell cycle arrest and apoptosis, at least partly, through NF-κB signaling pathways.


Assuntos
Antineoplásicos Fitogênicos/farmacologia , Lamiaceae/química , NF-kappa B/antagonistas & inibidores , Triterpenos/farmacologia , Apoptose/efeitos dos fármacos , Carcinoma Pulmonar de Células não Pequenas/tratamento farmacológico , Pontos de Checagem do Ciclo Celular/efeitos dos fármacos , Linhagem Celular Tumoral , Ensaios de Seleção de Medicamentos Antitumorais , Humanos , Neoplasias Pulmonares/tratamento farmacológico , Potencial da Membrana Mitocondrial/efeitos dos fármacos , NF-kappa B/metabolismo , Espécies Reativas de Oxigênio/metabolismo , Transdução de Sinais/efeitos dos fármacos , Triterpenos/química
15.
Acta Pharm ; 69(3): 443-449, 2019 Sep 01.
Artigo em Inglês | MEDLINE | ID: mdl-31259737

RESUMO

Lamium album and Lamium purpureum are species belonging to the genus Lamium. Aerial parts of the two species and roots of Lamium album have applications in human and veterinary traditional medicine. Haemostatic properties of butanolic extracts of Lamium species were investigated by two experimental models in Wistar rats: haemostatic test by tail bleeding time determination and acenocoumarolcarrageenan test. Results of the haemostatic test by tail bleeding determination demonstrated haemostatic activity of both extracts. In the acenocoumarol-carrageenan test, only the Lamium album extract showed haemostatic activity, comparable to that of vitamin K. Based on the qualitative chemical data on iridoid glycosides (HPTLC), 8-acetylshanzhiside methyl ester might be assumed to be responsible for haemostatic activity. Based on the acute toxicity test, none of the extracts showed toxicity.


Assuntos
Hemostáticos/farmacologia , Lamiaceae/química , Componentes Aéreos da Planta/química , Extratos Vegetais/farmacologia , Animais , Feminino , Hemostáticos/química , Masculino , Camundongos , Extratos Vegetais/química , Ratos , Ratos Wistar
16.
Cell Mol Biol (Noisy-le-grand) ; 65(5): 3-8, 2019 Jun 30.
Artigo em Inglês | MEDLINE | ID: mdl-31304900

RESUMO

Cyclotrichium niveum is an endemic plant for Turkey and it appears to have in vitro antioxidant and acetylcholinesterase inhibition properties. To the best of our knowledge, there has been no study on the in vivo effects of this plant. Therefore, the purpose of this study was to evaluate the effects of C. niveum on lead (Pb)-acetate-induced potential alterations in brain acetylcholinesterase activity, as well as oxidative stress in male rats. The rats were randomly assigned to control, Pb-acetate, C. niveum and Pb-acetate+ C. niveum groups. Pb-acetate was provided in drinking water (500 ppm), and C. niveum was administered via orogastric gavage (4 ml/kg) for 30 days. The acetylcholinesterase activity in the brain significantly decreased only in the Pb-acetate group. The malondialdehyde level significantly increased, and the reduced glutathione activity decreased in the Pb-acetate group. The reduced glutathione and glutathione-S-transferase activities of the C. niveum group were higher than the control group. No Pb was detected on a ppb level in the brain tissue of the control and C. niveum groups, while it was detected in the brains of the rats in the Pb-acetate and Pb-acetate+ C. niveum groups (185+8.98 ppb and 206+56.65 ppb, respectively). The data collected in this study suggested that C. niveum may reduce inhibition of brain AChE activity and oxidative stress against Pb-acetate-induced alterations in the brain of male rats.


Assuntos
Acetilcolinesterase/metabolismo , Antioxidantes/farmacologia , Encéfalo/metabolismo , Inibidores da Colinesterase/farmacologia , Lamiaceae/química , Fármacos Neuroprotetores/farmacologia , Compostos Organometálicos/administração & dosagem , Estresse Oxidativo/efeitos dos fármacos , Extratos Vegetais/farmacologia , Administração Oral , Animais , Glutationa/metabolismo , Glutationa Redutase/metabolismo , Glutationa Transferase/metabolismo , Masculino , Malondialdeído/metabolismo , Compostos Organometálicos/efeitos adversos , Ratos , Ratos Wistar , Turquia
17.
Appl Biochem Biotechnol ; 189(4): 1291-1303, 2019 Dec.
Artigo em Inglês | MEDLINE | ID: mdl-31254228

RESUMO

With growing concern about the possible risks and side effects of antibiotic drugs, more and more natural products with antibacterial activity are studied as the substitutes. In this paper, the antibacterial activity of hydroquinone and arbutin in Ainsliaea bonatii was investigated, which both displayed relatively strong antibacterial activity against Staphylococcus aureus (SA), methicillin-resistant S. aureus (MRSA), and extended spectrum ß-lactamase S. aureus (ESBL-SA). The antibacterial mechanism of hydroquinone had been explored by scanning electron microscopy (SEM), alkaline phosphatase (AKP), and bacterial extracellular protein leakage. Results showed that hydroquinone could destroy the bacterial cell wall and membrane, increase permeability, lead leakage of intracellular substance affect synthesis of protein, and influence expression of genes.


Assuntos
Antibacterianos/farmacologia , Arbutina/farmacologia , Hidroquinonas/farmacologia , Lamiaceae/química , Staphylococcus aureus Resistente à Meticilina/metabolismo , Antibacterianos/química , Arbutina/química , Hidroquinonas/química , Staphylococcus aureus Resistente à Meticilina/ultraestrutura
18.
Int J Biol Macromol ; 136: 1000-1006, 2019 Sep 01.
Artigo em Inglês | MEDLINE | ID: mdl-31254574

RESUMO

The effect of sulfated modification on the physicochemical properties and antioxidant activities of polysaccharide (MP) from Mesona chinensis Benth were investigated by chemical methods, Fourier transform infrared spectroscopy, high performance anion exchange chromatography, and establishing oxidative stress model and free radical model. Results showed that sulfated modification caused a significant change in chemical composition and the apparent structure of MP, but the degradation of the main chain of MP was inconspicuous. Sulfated Mesona chinensis Benth polysaccharide (SMP) exhibited excellent free radical scavenging activities and improved the protective effect of MP on cellular oxidative stress by increasing superoxide dismutase (SOD) activity and decreasing malondialdehyde (MDA) content. This study suggested that sulfated modification is an effective method to improve the antioxidant activities of MP, so as to expand the development and application of MP.


Assuntos
Antioxidantes/química , Antioxidantes/farmacologia , Lamiaceae/química , Estresse Oxidativo/efeitos dos fármacos , Polissacarídeos/química , Polissacarídeos/farmacologia , Sulfatos/química , Animais , Compostos de Bifenilo/química , Proliferação de Células/efeitos dos fármacos , Peróxido de Hidrogênio/farmacologia , Malondialdeído/metabolismo , Camundongos , Peso Molecular , Monossacarídeos/análise , Picratos/química , Células RAW 264.7 , Superóxido Dismutase/metabolismo
19.
Life Sci ; 231: 116519, 2019 Aug 15.
Artigo em Inglês | MEDLINE | ID: mdl-31152813

RESUMO

Glechoma hederacea belongs to the Labiatae family and has many biological activities. The objective of this study was to evaluate the chemical composition, antioxidant and anti-inflammatory activities of a hot water extract of G. hederacea (HWG). Our results indicated that rosmarinic acid, chlorogenic acid, caffeic acid, rutin, genistin, and ferulic acid were the most abundant phytochemicals in HWG. The free radical scavenging capacity of HWG in cell-free systems was evaluated by using the α,α-diphenyl-ß-picrylhydrazyl (DPPH) and ß-carotene bleaching assays. The antioxidant and anti-inflammatory activities of HWG were determined in vitro in lipopolysaccharide (LPS)-activated RAW 264.7 macrophages. The results demonstrated that DAPI staining, the comet assay, and DNA fragmentation showed that HWG prevented LPS-induced DNA damage in RAW264.7 macrophages, reduced the content of LPS-induced nitric oxide (NO) and malondialdehyde (MDA), increased GSH levels, and regulated antioxidant enzyme activities. We also demonstrated that HWG significantly decreased the LPS-induced mRNA expression of iNOS, COX-2, TNF-α, IL-6, and IL-1ß in RAW264.7 macrophages, and reduced the LPS-induced protein expression of iNOS and COX-2 in RAW264.7 macrophages. These results show that HWG and its main components possess potent antioxidant and anti-inflammatory properties.


Assuntos
Medicamentos de Ervas Chinesas/farmacologia , Lamiaceae/química , Animais , Anti-Inflamatórios/farmacologia , Antioxidantes/farmacologia , Ciclo-Oxigenase 2/metabolismo , Medicamentos de Ervas Chinesas/isolamento & purificação , Lamiaceae/metabolismo , Lipopolissacarídeos/farmacologia , Macrófagos/metabolismo , Camundongos , NF-kappa B/metabolismo , Óxido Nítrico/metabolismo , Compostos Fitoquímicos/química , Células RAW 264.7/efeitos dos fármacos , Espécies Reativas de Oxigênio/metabolismo , Fator de Necrose Tumoral alfa/metabolismo
20.
Planta Med ; 85(11-12): 869-910, 2019 Aug.
Artigo em Inglês | MEDLINE | ID: mdl-31216581

RESUMO

The 2 genera Ballota and Otostegia, belonging to the Lamiaceae family, are closely related taxonomically and found mainly in the Mediterranean area, Middle East, and North Africa. Since ancient times, they have been largely employed in traditional medicine for their biological properties such as antimicrobial, anti-inflammatory, antispasmodic, insecticidal, anti-malaria, etc. Phytochemical investigations of Ballota and Otostegia species have revealed that diterpenoids are the main constituents of the genera. A large number of flavonoids and other metabolites were also identified. This review, covering literature from 1911 up to 2018, includes traditional uses, chemical profiles (both of volatile and nonvolatile metabolites), and biological properties of all the taxa of these 2 genera studied to date.


Assuntos
Ballota , Lamiaceae , Fitoterapia/métodos , Extratos Vegetais/uso terapêutico , Animais , Ballota/química , Ballota/metabolismo , Humanos , Lamiaceae/química , Lamiaceae/metabolismo , Medicina Tradicional , Extratos Vegetais/química
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