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1.
Molecules ; 26(20)2021 Oct 14.
Artigo em Inglês | MEDLINE | ID: mdl-34684794

RESUMO

Luohuazizhu suppository is a Traditional Chinese Medicine used in clinic to treat cervicitis, which is prepared from Callicarpa nudiflora Hook. et Arn (C. nudiflora), an herbal Chinese medicine named Luohuazizhu. This study aimed to figure out the active constituents of C. nudiflora and the potential mechanism for its anti-cervicitis effect. The ethanol extract in C. nudiflora (CNE) and the different fractions of CNE extracted by petroleum ether (CNE-p), dichloromethane (CNE-d), and n-butanol (CNE-b) were tested in vivo for their anti-cervicitis effects. Then the isolated compounds from the CNE-p were tested in vitro for their anti-inflammatory activities. The results displayed that CNE-p, CNE-d, and CNE-b exhibited adequate anti-cervicitis effects, with CNE-p showing the highest efficacy. Further experiment demonstrated that CNE-p could significantly inhibit the expression of NLRP3 in vitro. Six diterpenoids obtained from the CNE-p showed the ability to regulate inflammatory factor levels in vitro. Among these compounds, compounds 1 (callicarpic acid A) and 2 (syn-3,4-seco-12S-hydroxy-15,16-epoxy-4(18),8(17),3(16),14(15)-labdatetraen-3-oic acid) were the most effective agents, and they also inhibited the expression level of NLRP3 in vitro. The results confirmed that C. nudiflora has significant anti-cervicitis effects and the diterpenoids were most likely to be its active components. These data provide scientific support for the clinic usage of Luohuazizhu suppository and the development of new agents in treating cervicitis.


Assuntos
Callicarpa/química , Proteína 3 que Contém Domínio de Pirina da Família NLR/antagonistas & inibidores , Compostos Fitoquímicos/farmacologia , Cervicite Uterina/tratamento farmacológico , Animais , Anti-Inflamatórios/isolamento & purificação , Anti-Inflamatórios/farmacologia , Citocinas/metabolismo , Modelos Animais de Doenças , Diterpenos/isolamento & purificação , Diterpenos/farmacologia , Feminino , Humanos , Medicina Tradicional Chinesa , Camundongos , Simulação de Acoplamento Molecular , Proteína 3 que Contém Domínio de Pirina da Família NLR/química , Compostos Fitoquímicos/isolamento & purificação , Extratos Vegetais/farmacologia , Plantas Medicinais/química , Células RAW 264.7 , Ratos , Ratos Sprague-Dawley , Cervicite Uterina/metabolismo , Cervicite Uterina/patologia
2.
Phytomedicine ; 93: 153486, 2021 Dec.
Artigo em Inglês | MEDLINE | ID: mdl-34649211

RESUMO

BACKGROUND: Callicarpa nudiflora (C. nudiflora), which is a medical herb in genus of Callicarpa, widely grows in the southern part of China. Several investigations had shown that this herb exerts anti-tumor effects. Ezrin is an important membrane-cytoskeleton-binding protein. By organizing membrane proteins and orchestrating their signal transduction, Ezrin contributes to modulation of cytoskeleton rearrangement in cell motility. PURPOSE: To investigate the anti-motile properties of Rhoifolin (RFL), a flavonoid from C. nudiflora, and to determine whether its effects are related to the inhibition on Podocalyxin (PODXL)-Ezrin signal transduction. METHODS: To determine suitable concentration of RFL and exposure time on breast cancer cells, the effects of RFL on viability of breast cancer cells were evaluated by MTT assay. Then, the anti-migratory properties of RFL were determined by AP 48 chamber system and ORISTM cell migration assay. F-actin in MDA-MB-231 cells was visualized by Alexa Fluor™ 488 conjugated Phalloidin. Immunoprecipitation was involved to access the effects of RFL on the interaction between Ezrin and PODXL. In addition, several EMT markers, including E-cadherin, Vimentin, Snail and Slug, were measured by Western Blotting assay and cell immunofluorescent analysis. Finally, the effects of RFL on cell migration, expression of Ezrin and EMT markers were verified by small interfering RNA (siRNA) mediated gene silencing. RESULTS: We showed here that treatments with 10 and 40 µM of RFL induced significant inhibitions on cell migration and alterations on the location and organization of actin cytoskeleton in breast cancer cells. Next, it was found that RFL suppressed Ezrin phosphorylation and consequent interaction with PODXL, significantly. Also, this compound showed an obvious inhibitory effect on TGF-ß1-induced EMT in MDA-MB-231 cells. Furthermore, data from RNA interfering assay confirmed that the inhibitory effects of RFL on Ezrin was enhanced by the deletion of Ezrin. CONCLUSION: RFL shows anti-motile properties on breast cancer cells, which is due to its potential to downregulate Podocalyxin-Ezrin interaction during Epithelial Mesenchymal Transition.


Assuntos
Neoplasias da Mama , Callicarpa , Neoplasias da Mama/tratamento farmacológico , Linhagem Celular Tumoral , Movimento Celular , Proteínas do Citoesqueleto , Dissacarídeos , Transição Epitelial-Mesenquimal , Feminino , Flavonoides/farmacologia , Glicosídeos , Humanos , Sialoglicoproteínas
3.
Zhongguo Zhong Yao Za Zhi ; 46(16): 4139-4144, 2021 Aug.
Artigo em Chinês | MEDLINE | ID: mdl-34467725

RESUMO

The purpose of the research is to study the bioactive constituents of Callicarpa nudiflora. From the 65% ethanol extract of C. nudiflora leaves, ten compounds were isolated by macroporous adsorption resin, Sephadex LH-20, ODS, silica gel, and preparative HPLC. These compounds were identified as callicapene M6(1), sterebin A(2), isomartynoside(3), crenatoside(4), luteolin-7-O-neohesperidoside(5), apigenin-7-O-ß-D-neohesperidoside(6), isoacteoside(7), acteoside(8),(7R)-campneoside I(9), and(7S)-campneoside I(10) on the basis of NMR, HR-ESI-MS, and optical rotation data. Compound 1 was obtained as a new compound. Compounds 2 and 4 were isolated from the genus Callicarpa for the first time. Compounds 9 and 10 were isolated from C. nudiflora for the first time.


Assuntos
Callicarpa , Diterpenos , Cromatografia Líquida de Alta Pressão , Estrutura Molecular , Folhas de Planta
4.
Chin J Nat Med ; 19(8): 632-640, 2021 Aug.
Artigo em Inglês | MEDLINE | ID: mdl-34419263

RESUMO

A phytochemical investigation was carried out on the extract of a medicinal plant Callicarpa nudiflora, resulting in the characterization of five new 3, 4-seco-isopimarane (1-5) and one new 3, 4-seco-pimarane diterpenoid (6), together with four known compounds. The structures of the new compounds were fully elucidated by extensive analysis of MS, 1D and 2D NMR spectroscopic data, and time-dependent density functional theory (TDDFT) calculation of electronic circular dichroism (ECD) spectra, and DFT calculations for NMR chemical shifts and optical rotations.


Assuntos
Abietanos , Callicarpa , Diterpenos , Abietanos/química , Abietanos/isolamento & purificação , Callicarpa/química , Diterpenos/química , Diterpenos/isolamento & purificação , Estrutura Molecular , Compostos Fitoquímicos/química , Compostos Fitoquímicos/isolamento & purificação , Folhas de Planta
5.
Zootaxa ; 4926(3): zootaxa.4926.3.1, 2021 Feb 09.
Artigo em Inglês | MEDLINE | ID: mdl-33756737

RESUMO

Among the thecate hydroids brought back by the Proteus-Guyane 2017 expedition of the Muséum national d'histoire naturelle of Paris, France, from French Guiana, two interesting species are reported upon. The plumulariid Callicarpa gracilis Fewkes, 1881, known so far from the type specimen only, is comprehensively redescribed 140 years after its original description. It adopts two different morphotypes with respect to both its tropho- and gonosome, forming either simple or ramified colonies, with either structurally-complex or rudimentary phylactocarps, respectively. Taxonomic notes on the genera Callicarpa Fewkes, 1881 and Hippurella Allman, 1877 are provided in light of their intricate history of origin and fate, together with the provisional resurrection of Antomma Stechow, 1919, as an allied genus of the former. The aglaopheniid Aglaophenia trifida L. Agassiz, 1862, whose gonosome was only partly documented to date, is redescribed thoroughly based on specimens bearing male and female corbulae. Scanning electron microscopy and molecular data were also used to document both species. A checklist of the thecate hydroids from French Guiana gathered during Proteus-Guyane 2017 and Guyane 2014 expeditions is provided as an appendix, together with brief notes on some species. Not dealing with the present study, but taking advantage of it, a new name, Antennella billardi Galea, nom. nov., is proposed as a replacement name for Plumularia balei Billard, 1911, which is a permanently invalid junior primary homonym of P. balei Bartlett, 1907.


Assuntos
Callicarpa , Expedições , Hidrozoários , Animais , Feminino , Guiana Francesa , Masculino
6.
J Ethnopharmacol ; 267: 113523, 2021 Mar 01.
Artigo em Inglês | MEDLINE | ID: mdl-33129947

RESUMO

ETHNOPHARMACOLOGICAL RELEVANCE: Callicarpa japonica Thunb., as an herbal medicine has been used for the treatment of inflammatory diseases in China and Korea. MATERIALS AND METHODS: Ultra performance liquid chromatography-photodiode array-quadrupole time-of-flight mass spectrometer (UPLC-PDA-QTof MS) was used to detect the major phenylethanoid glycosides in the C. japonica extract. BALB/c mice were intraperitoneally sensitized by ovalbumin (OVA) (on days 0 and 7) and challenged by OVA aerosol (on days 11-13) to induce airway inflammatory response. The mice were also administered with C. japonica Thunb. (CJT) (20 and 40 mg/kg Per oral) on days 9-13. CJT pretreatment was conducted in lipopolysaccharide (LPS)-stimulated RAW264.7 or phorbol 12-myristate 13-acetate (PMA)-stimulated A549 cells. RESULTS: CJT administration significantly reduced the secretion of Th2 cytokines, TNF-α, IL-6, immunoglobulin E (IgE) and histamine, and the recruitment of eosinophils in an OVA-exposed mice. In histological analyses, the amelioration of inflammatory cell influx and mucus secretion were observed with CJT. The OVA-induced airway hyperresponsiveness (AHR), iNOS expression and NF-κB activation were effectively suppressed by CJT administration. In addition, CJT led to the upregulation of HO-1 expression. In an in vitro study, CJT pretreatment suppressed the LPS-induced TNF-α secretion in RAW264.7 cells and attenuated the PMA-induced IL-6, IL-8 and MCP-1 secretion in A549 cells. These effects were accompanied by downregulated NF-κB phosphorylation and by upregulated HO-1 expression. CONCLUSION: These results suggested that CJT has protective activity against OVA-induced airway inflammation via downregulation of NF-κB activation and upregulation of HO-1, suggesting that CJT has preventive potential for the development of allergic asthma.


Assuntos
Antiasmáticos/farmacologia , Anti-Inflamatórios/farmacologia , Asma/prevenção & controle , Hiper-Reatividade Brônquica/prevenção & controle , Callicarpa , Heme Oxigenase-1/metabolismo , Pulmão/efeitos dos fármacos , Proteínas de Membrana/metabolismo , NF-kappa B/metabolismo , Extratos Vegetais/farmacologia , Células A549 , Animais , Antiasmáticos/isolamento & purificação , Anti-Inflamatórios/isolamento & purificação , Asma/induzido quimicamente , Asma/enzimologia , Asma/fisiopatologia , Hiper-Reatividade Brônquica/induzido quimicamente , Hiper-Reatividade Brônquica/enzimologia , Hiper-Reatividade Brônquica/fisiopatologia , Broncoconstrição/efeitos dos fármacos , Callicarpa/química , Citocinas/metabolismo , Modelos Animais de Doenças , Feminino , Humanos , Pulmão/enzimologia , Pulmão/fisiopatologia , Camundongos , Camundongos Endogâmicos BALB C , Ovalbumina , Extratos Vegetais/isolamento & purificação , Células RAW 264.7 , Transdução de Sinais , Regulação para Cima
7.
Nat Prod Res ; 35(7): 1107-1114, 2021 Apr.
Artigo em Inglês | MEDLINE | ID: mdl-31303054

RESUMO

Two new terpenoids (1-2) and seven known compounds (3-9) were isolated from methanol extract of Callicarpa macrophylla leaves. Their structures were determined to be ent-7α,16ß,17,18-tetrahydroxykaur-15-one (1), 3ß-acetoxy-urs-12-ene-11-one-12-ol (2), ent-1ß-acetoxy-7α,14ß-dihydroxykaur-16-en-15-one (3), 3ß-acetoxy-11α,13ß-dihydroxyolean-12-one (4), ß-amyrin (5), spinasterol (6), ursolic acid (7), ß-sitosterol (8), and daucosterol (9) by analyses of their MS, NMR spectroscopic data and by comparison with those reported in the literature. Compounds 1 - 4, and 7 displayed potential cytotoxic activity towards HepG-2, LU-1, and MCF-7 human cancer cell lines with IC50 values ranging from 0.46 ± 0.21 to 18.14 ± 0.33 µM. Compound 6 showed IC50 values of 14.17 ± 0.21 and 5.72 ± 0.42 µM against Hep-G2 and MCF-7 cell lines, respectively.


Assuntos
Callicarpa/química , Terpenos/isolamento & purificação , Espectroscopia de Ressonância Magnética Nuclear de Carbono-13 , Linhagem Celular Tumoral , Humanos , Concentração Inibidora 50 , Ácido Oleanólico/análogos & derivados , Ácido Oleanólico/química , Ácido Oleanólico/farmacologia , Extratos Vegetais/análise , Extratos Vegetais/química , Extratos Vegetais/farmacologia , Folhas de Planta/química , Espectroscopia de Prótons por Ressonância Magnética , Terpenos/análise , Terpenos/química , Terpenos/farmacologia , Triterpenos/química , Triterpenos/farmacologia
8.
Phytochemistry ; 181: 112577, 2021 Jan.
Artigo em Inglês | MEDLINE | ID: mdl-33190100

RESUMO

The new concept that Na/K-ATPase acts as a receptor prompted us to look for new ligands from Callicarpa kwangtungensis Chun. Using column chromatography, an undescribed phenethyl alcohol glycoside, callicarpanoside A, and an undescribed benzyl alcohol glycoside, callicarpanoside B, along with twelve known polyphenols were isolated from Callicarpa kwangtungensis Chun. All the isolated compounds were evaluated for their Na/K-ATPase (NKA) inhibitory activities. Using our NKA technology platform-based screening assay protocols, callicarpanoside B was identified as an undescribed Na/K-ATPase agonist. In particular, the newly identified benzyl alcohol glycoside was found to bind NKA and activate the receptor NKA/Src complex, resulting in the activation of protein kinase cascades. These cascades included extracellular signal-regulated kinases and protein kinase C epsilon, as well as NKA α1 endocytosis at nanomolar concentrations. Unlike the class of cardiotonic steroids, callicarpanoside B showed less inhibition of NKA activity and caused less cellular toxicity. Moreover, callicarpanoside B was found to bind NKA at a different site other than the cardiotonic steroids binding site. Thus, we have identified an undescribed NKA α1 agonist that may be used to enhance the physiological processes of NKA α1 signaling.


Assuntos
Callicarpa , Glicosídeos Cardíacos , Glicosídeos Cardíacos/farmacologia , Glicosídeos/farmacologia , Transdução de Sinais , ATPase Trocadora de Sódio-Potássio/metabolismo
9.
J Ethnopharmacol ; 264: 113123, 2021 Jan 10.
Artigo em Inglês | MEDLINE | ID: mdl-32783986

RESUMO

ETHNOPHARMALOGICAL RELEVANCE: Callicarpa nudiflora Hook. & Arn. is a perennial evergreen shrub or low arbor in the Genus Callicarpa. Its dried aerial parts are used as traditional Chinese herbal medicine, Luo-hua-zi-zhu (Callicarpa nudiflora), which has been widely used in anti-bacteria and anti-ulcer in China (Commission, 2015; Development, 1994; Ming-Sheng, 2008). AIM OF THE STUDY: The present paper reviewed findings in phytochemistry and pharmacology of Callicarpa nudiflora. METHODS: Chinese and English studies on Callicarpa nudiflora were collected from databases including Web of Science, SciFinder, PubMed, Elsevier, and CNKI (Chinese), and the phytochemical and pharmacological studies of Callicarpa nudiflora were reviewed. RESULTS: A total of 300 small molecules, 173 of which are volatile oils, have been isolated from Callicarpa nudiflora. These small molecules could be divided into seven structural types - phenylpropanoids, flavonoids, triterpenes, diterpenes, iridoid glycosides, volatile oils, and other small molecules. Different types of compounds in Callicarpa nudiflora were summarized as follow: a) diterpenoid compounds can inhibit the generation of nitric oxide (NO) for exerting the function of anti-inflammation; b) triterpene compounds can play a role of anti-thrombus via inhibiting platelet aggregation and oleanane type and arbutane type pentacyclic triterpenes have the hepatoprotective activities; c) iridoid glycosides have cytotoxicity to tumor cells, and phenylpropanoids compounds have an antioxidant effect and could improve the function of memory. Our group further studied the antiviral activities of Callicarpa nudiflora finding that it has significant effects on RSV, EV71, COXB5, and HSV-1.


Assuntos
Callicarpa , Etnofarmacologia/métodos , Compostos Fitoquímicos/farmacologia , Compostos Fitoquímicos/uso terapêutico , Extratos Vegetais/farmacologia , Extratos Vegetais/uso terapêutico , Animais , Anti-Inflamatórios/isolamento & purificação , Anti-Inflamatórios/farmacologia , Anti-Inflamatórios/uso terapêutico , Humanos , Compostos Fitoquímicos/isolamento & purificação , Extratos Vegetais/isolamento & purificação , Inibidores da Agregação Plaquetária/isolamento & purificação , Inibidores da Agregação Plaquetária/farmacologia , Inibidores da Agregação Plaquetária/uso terapêutico
10.
Fitoterapia ; 147: 104774, 2020 Nov.
Artigo em Inglês | MEDLINE | ID: mdl-33152461

RESUMO

Nine new diterpenoids, Rubellacrns A - I (1-9), including five isopimaranes (1-4, 9), four pimaranes (5-8), together with five known isopimarane analogues (10-14), were isolated from Callicarpa rubella. The structures of these compounds were unambiguously established by HR-ESIMS and NMR spectroscopic data, the absolute configurations of compounds 5 and 9 were determined by ECD. All the isolated compounds were tested for their anti-inflammatory effects and compounds 2 and 11-14 showed NLRP3-inflammasome inhibitory activity with IC50 values ranging from 7.02 to 14.38 µM.


Assuntos
Callicarpa/química , Diterpenos/farmacologia , Inflamassomos/antagonistas & inibidores , Proteína 3 que Contém Domínio de Pirina da Família NLR/antagonistas & inibidores , Abietanos , Animais , Linhagem Celular , China , Diterpenos/isolamento & purificação , Macrófagos/efeitos dos fármacos , Camundongos , Estrutura Molecular , Compostos Fitoquímicos/isolamento & purificação , Compostos Fitoquímicos/farmacologia , Folhas de Planta/química
11.
Chem Biodivers ; 17(12): e2000798, 2020 Dec.
Artigo em Inglês | MEDLINE | ID: mdl-33135326

RESUMO

Four new diterpenoids, rubellawus A-D (1-4), along with three known compounds, were isolated and identified from the flowers of Callicarpa rubella. Their structures were elucidated by various spectroscopic analysis. All the compounds were screened for their anti-inflammatory activity and 14α-hydroxyisopimaric acid and isopimaric acid showed significant NLRP3 inflammasome inhibitory activity with IC50 values of 7.02 and 3.99 µM.


Assuntos
Callicarpa/química , Diterpenos/isolamento & purificação , Diterpenos/farmacologia , Inflamassomos/antagonistas & inibidores , Proteína 3 que Contém Domínio de Pirina da Família NLR/antagonistas & inibidores , Animais , Linhagem Celular , Diterpenos/química , Análise Espectral/métodos , Relação Estrutura-Atividade
12.
Zhongguo Zhong Yao Za Zhi ; 45(15): 3642-3650, 2020 Aug.
Artigo em Chinês | MEDLINE | ID: mdl-32893553

RESUMO

This article is based on basic data such as field surveys and literature surveys, contrasting and analyzing the distribution of Callicarpa nudiflora by different zoning methods, different data sources, and different spatial scales. The results showed that there were certain differences in the distribution results obtained by using different methods, such as qualitative description, similar ecological environment, and niche model, to divide the distribution of the C. nudiflora, but all of them could reflect the distribution of C. nudiflora to different degrees. Among them, the qualitative description division method has certain advantages in macro guidance in a large scale. The distribution range obtained by the ecological environment similar division method is wider than that obtained by applying the qualitative description method and the niche model method. The results of the zoning of the distribution of the C. nudiflora obtained from different data sources were different. The number and representativeness of the survey data have an impact on the zoning results. Through the analysis of the distribution of different spatial scales, the ecological factors and contribution rates that affect the distribution of C. nudiflora are different in China and in the world. The comprehensive multi-source data analysis showed that C. nudiflora mainly distributed in southern coastal provinces such as Hainan, Guangdong, Guangxi and Fujian in China, and also in Jiangxi, Guizhou, Yunnan, Sichuan, Chongqing, Hunan, Gansu, Taiwan and other provinces. Globally, C. nudiflora are suitable for distribution in Southeast Asia, such as China, Vietnam, Laos, Myanmar, India, etc. There are also potential distribution areas in the southern United States and Mexico.


Assuntos
Callicarpa , China , Coleta de Dados , Armazenamento e Recuperação da Informação , Vietnã
13.
J Nat Prod ; 83(7): 2191-2199, 2020 07 24.
Artigo em Inglês | MEDLINE | ID: mdl-32628479

RESUMO

Callicarpins A-D (1-4), possessing an unprecedented A-homoent-clerodane scaffold with a bicyclo[5.4.0]undecane ring system, and callicarpins E-G (5-7), with 5/6-fused ent-clerodane diterpenoid skeletons, were isolated from Callicarpaarborea and C. integerrim. Their structures were elucidated by comprehensive spectroscopic data, X-ray crystal diffraction, chemical derivatization, and electronic circular dichroism (ECD) data. Putative biosynthetic pathways for these callicarpins are proposed. Compounds 2, 3b, and 6-8 showed potent inhibitory effects against the NLRP3 inflammasome with IC50 values from 1.4 to 5.3 µM, and 2 significantly blocked NLRP3 inflammasome-induced pyroptosis by inhibiting Casp-1 activation and IL-1ß secretion in J774A.1 cells.


Assuntos
Callicarpa/química , Diterpenos Clerodânicos/química , Inflamassomos/metabolismo , Proteína 3 que Contém Domínio de Pirina da Família NLR/antagonistas & inibidores , Piroptose/efeitos dos fármacos , Diterpenos Clerodânicos/administração & dosagem , Diterpenos Clerodânicos/farmacologia , Relação Dose-Resposta a Droga , Proteína 3 que Contém Domínio de Pirina da Família NLR/metabolismo , Análise Espectral/métodos
14.
ACS Infect Dis ; 6(7): 1667-1673, 2020 07 10.
Artigo em Inglês | MEDLINE | ID: mdl-32579326

RESUMO

The rise of antibiotic resistance presents a significant healthcare challenge and precludes the use of many otherwise valuable antibiotics. One potential solution to this problem is the use of antibiotics in combination with resistance-modifying agents, compounds that act synergistically with existing antibiotics to resensitize previously resistant bacteria. In this study, 12(S),16ξ-dihydroxycleroda-3,13-dien-15,16-olide, a clerodane diterpene isolated from the medicinal plant Callicarpa americana, was found to synergize with oxacillin against methicillin-resistant Staphylococcus aureus. This synergy was confirmed by checkerboard (fractional inhibitory concentration index (FICI) = 0.125) and time-kill assays, with a subinhibitory dose of 12(S),16ξ-dihydroxycleroda-3,13-dien-15,16-olide causing the effective concentration of oxacillin to fall below the susceptibility breakpoint for S. aureus, a >32-fold decrease in both cases.


Assuntos
Callicarpa , Diterpenos Clerodânicos , Staphylococcus aureus Resistente à Meticilina , Antibacterianos/farmacologia , Diterpenos Clerodânicos/farmacologia , Sinergismo Farmacológico , Testes de Sensibilidade Microbiana , Oxacilina , Staphylococcus aureus
15.
Molecules ; 25(10)2020 May 13.
Artigo em Inglês | MEDLINE | ID: mdl-32414033

RESUMO

Plants of the genus Callicarpa are known to possess several medicinal effects. The constituents of the Taiwan endemic plant Callicarpa hypoleucophylla have never been studied. Therefore, C. hypoleucophylla was selected for our phytochemical investigation. Two new clerodane-type diterpenoids, named callihypolins A (1) and B (2), along with seven known compounds were isolated from the leaves and twigs of the Lamiaceae plant C. hypoleucophylla and then characterized. The structures of compounds 1 and 2 were elucidated by spectroscopic data analysis, specifically, two-dimension nuclear magnetic resonance (NMR). The anti-inflammatory activity of compounds 1-9 based on the suppression of superoxide anion generation and elastase release was evaluated. Among the isolates, compounds 2-4 showed anti-inflammatory activity (9.52-32.48% inhibition at the concentration 10 µm) by suppressing superoxide anion generation and elastase release. Our findings not only expand the description of the structural diversity of the compounds present in plants of the genus Callicarpa but also highlight the possibility of developing anti-inflammatory agents from Callicarpa endemic species.


Assuntos
Anti-Inflamatórios , Callicarpa/química , Diterpenos Clerodânicos , Neutrófilos/metabolismo , Adulto , Anti-Inflamatórios/química , Anti-Inflamatórios/farmacologia , Diterpenos Clerodânicos/química , Diterpenos Clerodânicos/farmacologia , Feminino , Humanos , Masculino , Neutrófilos/patologia , Superóxidos/metabolismo
16.
J Ethnopharmacol ; 258: 112881, 2020 Aug 10.
Artigo em Inglês | MEDLINE | ID: mdl-32311484

RESUMO

ETHNOPHARMACOLOGICAL RELEVANCE: Callicarpa kwangtungensis Chun (C. kwangtungensis) is a very famous herbal medicine with the function of promoting blood circulation and removing blood stasis which is beneficial for cardiovascular disease (CVD). Phenylethanoid glycosides (PGs) are the major class of active ingredients in C. kwangtungensis and present significant anti-oxidative and anti-inflammatory property related to apoptosis. Therefore, this study aimed to investigate the effects of total phenylethanoid glycosides of C. kwangtungensis (CK-PGs) on isoproterenol (ISO) induced myocardial ischemic injury (MI) and the mechanisms related to the apoptosis mediated by oxidative damage and inflammation. METHODS: The myocardial ischemia animal model was established as subcutaneous injecting ISO. Echocardiography and biomarkers were employed to determine the degree of myocardial damage. Histopathological changes were observed by hematoxylin and eosin test. The TUNEL staining and activity of caspase-3 were measured to detect the level of apoptosis which is medicated by the oxidative damage detected by the level of MDA, GSH and ROS tested with the kit and the inflammation reflected by TNF-α. The activity of Na+-K+-ATPase (NKA) was detected by the commercial kits, whose expression was measured by immunohistochemistry analysis. At last, Western blot analysis was used to measure Na+-K+-ATPase/Src/ERK1/2 and Bax/Bcl-2 pathway. RESULTS: CK-PGs showed cardioprotective effect against ISO-induced myocardial ischemic injury evidenced by improving heart function and lowering myocardial injury markers. CK-PGs could inhibit the level of apoptosis as shown by the decrease of the TUNEL-positive cells, the activity of caspase-3 and increase of the expression of Bax. CK-PGs also reduced oxidative stress and inflammation to suppress apoptosis by decreasing the level of ROS, MDA, and increasing GSH activity and lowering the level of TNF-α. In addition, CK-PGs exerted the protection by increasing the activity and the expression of NKA. Meanwhile, Na+-K+-ATPase/Src/ERK1/2pathway was weakened for the inhibition of apoptosis. CONCLUSIONS: CK-PGs could protect cardiomyocytes from myocardial injury through suppressing Na+-K+-ATPase/Src/ERK1/2 pathway and inhibiting apoptosis mediated by oxidative stress and inflammation.


Assuntos
Callicarpa/química , Cardiotônicos/farmacologia , Glicosídeos/farmacologia , Inflamação/tratamento farmacológico , Animais , Apoptose/efeitos dos fármacos , Cardiotônicos/isolamento & purificação , Modelos Animais de Doenças , Glicosídeos/isolamento & purificação , Inflamação/patologia , Sistema de Sinalização das MAP Quinases/efeitos dos fármacos , Miócitos Cardíacos/efeitos dos fármacos , Miócitos Cardíacos/patologia , Estresse Oxidativo/efeitos dos fármacos , Ratos , Ratos Sprague-Dawley , ATPase Trocadora de Sódio-Potássio/metabolismo , Quinases da Família src/metabolismo
17.
J Ethnopharmacol ; 258: 112857, 2020 Aug 10.
Artigo em Inglês | MEDLINE | ID: mdl-32298752

RESUMO

ETHNOPHARMACOLOGICAL RELEVANCE: Callicarpa kwangtungensis, as a characteristic traditional herb in China, has been widely used as indigenous medicine for thousands of years in the treatment of upper respiratory tract infection, tonsillitis, pneumonia and traumatic bleeding in China. Phenylethanoid glycosides (PhGs), as natural polyphenols, are especially abundant in this herb and can be regarded as the representative active ingredients in C. kwangtungensis. AIM OF THIS STUDY: This study was performed to investigate the anti-inflammatory pharmacodynamic basis of six PhGs (acteoside, forsythoside B, poliumoside, alyssonoside, parvifloroside A, and syringalide A 3'-α-L-rhanmnopyranoside) isolated from C. kwangtungensis from the perspective of antioxidation. MATERIALS AND METHODS: Six PhGs were isolated from the anti-inflammatory extracts of C. kwangtungensis by various chromatographic techniques and their anti-inflammatory activity on RAW 264.7 murine macrophages induced by LPS was investigated by measuring the release of tumor necrosis factor (TNF-α), the colonic interleukin-6 (IL-6), nitric oxide (NO) and reactive oxygen species (ROS). Further, the underlying anti-inflammatory mechanism of two PhGs (forsythoside B and alyssonoside) was explored by determining the expression of Kelch-like ECH-association protein 1 (Keap1), nuclear factor erythroid 2-related factor 2 (Nrf2), heme oxygenase-1 (OH-1) and quinone oxidoreductase 1 (NQO1). Besides, molecular simulation was also employed to evaluate the binding capacity of two PhGs with Keap1. RESULTS: Compared with the model group, six PhGs revealed obviously inhibitory effects on TNF-α, IL-6, NO and the generation of ROS in RAW 264.7 macrophages. Moreover, forsythoside B and alyssonoside could act as the inhibitors of Keap1-Nrf2 interaction, then activated the nuclear translocation of Nrf2 and promoted the upregulated protein expression of HO-1 and NQO1, finally suppressed LPS-induced inflammatory response in RAW 264.7 macrophages. Molecular modeling exhibited hydrogen bonds played a crucial role for the binding of PhGs with the Nrf2 binding site in Keap1 protein. CONCLUSIONS: Natural PhGs-induced protection against LPS-induced inflammatory response via activating Keap1/Nrf2/HO-1 signaling pathway in RAW 264.7 macrophages were confirmed, which provided experimental and theoretical basis for the deeper use of C. Kwangtungensis in the treatment and prevention of diseases related to inflammation and oxidative stress.


Assuntos
Callicarpa/química , Glicosídeos/farmacologia , Inflamação/tratamento farmacológico , Macrófagos/efeitos dos fármacos , Animais , Anti-Inflamatórios/isolamento & purificação , Anti-Inflamatórios/farmacologia , Glicosídeos/química , Glicosídeos/isolamento & purificação , Heme Oxigenase-1/metabolismo , Inflamação/patologia , Proteína 1 Associada a ECH Semelhante a Kelch/metabolismo , Lipopolissacarídeos , Macrófagos/patologia , Proteínas de Membrana/metabolismo , Camundongos , Modelos Moleculares , Fator 2 Relacionado a NF-E2/metabolismo , Polifenóis/química , Polifenóis/isolamento & purificação , Polifenóis/farmacologia , Células RAW 264.7 , Espécies Reativas de Oxigênio/metabolismo , Transdução de Sinais/efeitos dos fármacos
18.
J Sep Sci ; 43(12): 2487-2494, 2020 Jun.
Artigo em Inglês | MEDLINE | ID: mdl-32294314

RESUMO

Callicarpa kwangtungensis Chun is a traditional Chinese medicine that has various therapeutic effects. Despite its wide use in Chinese medicine, the study is still quite limited, especially its chemical compositions. In this research, an ultra-high-pressure liquid chromatography coupled with Q Exactive hybrid quadrupole-orbitrap high-resolution accurate mass spectrometry tandem mass spectrometry method was utilized to analyze its chemical compositions for the first time. As a result, a total of 124 compounds, including 20 phenylethanoid glycosides, 31 flavonoids, 36 organic acids, 26 terpenoids and 11 phenols, were identified or tentatively characterized in 30 min. Among them, 49 compounds, including 5 phenylethanoid glycosides, 12 flavonoids, 16 organic acids, 12 terpenoids, and 4 phenols, were identified in Callicarpa kwangtungensis Chun for the first time. Besides, the fragmentation pathways were also discussed. This research established a rapid and reliable method to analyze the chemical compositions of complicated herb without the process of isolation, and provide abundant information on the chemical material basis for further bioactivity and quality control studies.


Assuntos
Callicarpa/química , Medicamentos de Ervas Chinesas/análise , Cromatografia Líquida de Alta Pressão , Espectrometria de Massas , Medicina Tradicional Chinesa , Estrutura Molecular
19.
J Pharm Biomed Anal ; 182: 113110, 2020 Apr 15.
Artigo em Inglês | MEDLINE | ID: mdl-32004768

RESUMO

Callicarpa nudiflora, belonging to the family Verbenaceae, is widely used to treat inflammation caused by bacterial infection.However, the underlying active substances of C. nudiflora against inflammation remains obscure. In this work, an ultra high-performance liquid chromatography (UHPLC) coupled with quadrupole time-of-flight mass spectrometry method was developed to characterize the ingredients in C. nudiflora, and a validated UHPLC coupled with triple quadrupole tandem mass spectrometry method was applied to quantify major components. As a result, a total of 96 chemical compounds were identified in C. nudiflora, and 26 compounds of them were further quantified in 34 batches of C. nudiflora. Based on the identified components from C. nudiflora, a compound-target network for the anti-inflammation effect was constructed by reverse docking target prediction, disease associated genes screening in DisGeNET and the protein-protein interaction from STRING. The compound-target network showed that C. nudiflora might exert anti-inflammation effect on the target of complement 3 and 5 in the pathway of cells and molecules involved in local acute inflammatory response, and 16 effective candidate compounds were found such as catalpol, acteoside, rutin, etc. This study provided an opportunity to deepen the understanding of the chemical composition and the potential anti-inflammatory mechanism of C. nudiflora.


Assuntos
Anti-Inflamatórios/isolamento & purificação , Callicarpa/química , Cromatografia Líquida de Alta Pressão/métodos , Extratos Vegetais/química , Animais , Anti-Inflamatórios/análise , Anti-Inflamatórios/farmacologia , Inflamação/tratamento farmacológico , Espectrometria de Massas/métodos , Camundongos , Simulação de Acoplamento Molecular , Extratos Vegetais/análise , Extratos Vegetais/farmacologia , Células RAW 264.7
20.
Nat Prod Res ; 34(2): 197-203, 2020 Jan.
Artigo em Inglês | MEDLINE | ID: mdl-30856343

RESUMO

Two new norneolignans, (7S,8R)-3-methoxy-3',4,9-trihydroxy-4',7-epoxy-8,3'-neolignane-1'-carboxylic acid (1) and (7R,8R)-3-methoxyl-4,9-dihydroxy-3':7,4':8-diepoxyneolignan-1'-carboxylic acid methyl ester (2) were isolated from Callicarpa kwangtungensis, together with ten known compounds, genistin (3), daidzin (4), silybin A (5), isosilybin A (6), isosilybin B (7), p-hydroxybenzaldehyde (8), syringic acid (9), lanceolatin A (10), icariside C5 (11), and (3S,6E,10R)-10-ß-D-glucopyranosyloxy-3,11-dihydroxy-3,7,11-trimethyldodeca-1,6-diene (12). Compounds 1 and 2 were evaluated for their effects on the inhibition of nitric oxide (NO) production in lipopolysaccharide induced RAW264.7 cells. Compounds 1 and 2 exhibited inhibitory activity with IC50 values of 31.45 ± 0.38 and 40.72 ± 0.54 µM, respectively.


Assuntos
Callicarpa/química , Lignanas/isolamento & purificação , Óxido Nítrico/antagonistas & inibidores , Animais , Concentração Inibidora 50 , Lignanas/análise , Lignanas/química , Lignanas/farmacologia , Lipopolissacarídeos , Macrófagos/metabolismo , Camundongos , Estrutura Molecular , Óxido Nítrico/biossíntese , Células RAW 264.7
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