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1.
J Photochem Photobiol B ; 203: 111748, 2020 Jan.
Artigo em Inglês | MEDLINE | ID: mdl-31918235

RESUMO

Nanotechnology is an emerged field to develop the plant mediated metal based nanodrugs by green method. In this current study, the zinc oxide metal based nanoparticles were developed using (Clausena lansium (Lour.) Skeels) Peel aqueous extracts and zinc nitrate. The C.L extract zinc nanoparticleswere indicated by the sharp peak seen at 350 nm utilizing the Ultraviolet-Visible spectroscopy (UV-Vis). The high peaks indicate the presence of phytochemicals and its functional groups in ZnONPs were studied by the Fourier Transform Infrared Spectroscopy (FT-IR). The X-Ray Diffraction analysis (XRD) explores the pattern and structure of ZnONPs as spherical and base-centered monoclinic crystalline shapes. The C.L extract with Zn nanoparticles were spherical in nature and the size of the synthesized particles were about 28.42 nm respectively. The autophagy (Beclin-1, LC3-I, LC3-II and ATG4B) and apoptotic (Bax, Bcl-2 and Caspase-3) proteins were regulated by the treatment with ZnONPs in SH-SY5Y neuroblastoma cells. The DNA loss or damage was occurred in the ZnONPs treatment and it was performed using Comet assay. The ZnONPs treatment generates the ROS in the cells and decreased its stability and viability. Addition of NAC prevents ROS in the cultured SH-SY5Y cells and prevents the cells from the apoptosis. We concluded that the ZnONPs potentially kills the neuroblastoma cells by producing the intracellular ROS.


Assuntos
Antineoplásicos/farmacologia , Autofagia/efeitos dos fármacos , Nanopartículas Metálicas/química , Óxido de Zinco/química , Antineoplásicos/química , Apoptose/efeitos dos fármacos , Proteína Beclina-1/metabolismo , Caspase 3/metabolismo , Linhagem Celular Tumoral , Sobrevivência Celular/efeitos dos fármacos , Clausena/química , Clausena/metabolismo , Dano ao DNA/efeitos dos fármacos , Química Verde , Humanos , Nanopartículas Metálicas/toxicidade , Neuroblastoma/metabolismo , Neuroblastoma/patologia , Extratos Vegetais/química , Proteínas Proto-Oncogênicas c-bcl-2/metabolismo , Espécies Reativas de Oxigênio/metabolismo
2.
Molecules ; 24(18)2019 09 18.
Artigo em Inglês | MEDLINE | ID: mdl-31540345

RESUMO

Seven compounds, carbazole alkaloids (heptaphylline, 7-methoxyheptaphylline, 7-methoxymukonal) and coumarins (clausarin, dentatin, nordentatin, and xanthoxyletin), were isolated from the root bark of Clausena harmandiana. Antioxidation, cytotoxicity and apoptosis induction were evaluated in vitro. Results showed that clausarin exerted the highest DPPH radical scavenging and 7-methoxymukonal had the highest ferric reducing antioxidant power. In contrary, dentatin was the least DPPH radical scavenger, and heptaphylline was the least reducing antioxidant power. The isolated compounds showed different cytotoxicity. The hepatocellular carcinoma (HepG2) was generally more sensitive to the isolated compounds than lung cancer (SK-LU-1), colon cancer (HCT-116), and noncancerous (Vero) cell lines, respectively. Clausarin possessed the highest cytotoxicity selectively against cancer cell lines tested. 7-Methoxymukonal and 7-methoxyheptaphylline exhibited less cytotoxicity only in HepG2 cells and were inactive in the SK-LU-1 and HCT116 cells. Despite xantoxyletin possessing low antioxidant and low cytotoxic activity, it induced the highest apoptosis percentage with the lowest necrosis percentage of HepG2 cells after 24 h. In conclusion, xantoxyletin primarily show potential anticancer activity. The root bark of C. harmandiana is a good source of bioactive compounds or the lead for the development of new pharmaceutical agent.


Assuntos
Alcaloides , Antineoplásicos Fitogênicos , Apoptose/efeitos dos fármacos , Clausena/química , Cumarínicos , Citotoxinas , Neoplasias/tratamento farmacológico , Alcaloides/química , Alcaloides/farmacologia , Antineoplásicos Fitogênicos/química , Antineoplásicos Fitogênicos/farmacologia , Cumarínicos/química , Cumarínicos/farmacologia , Citotoxinas/química , Citotoxinas/farmacologia , Células HCT116 , Células Hep G2 , Humanos , Neoplasias/metabolismo , Neoplasias/patologia , Casca de Planta/química , Raízes de Plantas/química
3.
Molecules ; 24(17)2019 Aug 28.
Artigo em Inglês | MEDLINE | ID: mdl-31466274

RESUMO

Clausena lansium Lour. Skeels (Rutaceae) is widely distributed in South China and has historically been used as a traditional medicine in local healthcare systems. Although the characteristic components (carbazole alkaloids and coumarins) of C. lansium have been found to possess a wide variety of biological activities, little attention has been paid toward the other components of this plant. In the current study, phytochemical analysis of isolates from a water-soluble stem and leaf extract of C. lansium led to the identification of 12 compounds, including five aromatic glycosides, four sesquiterpene glycosides, two dihydrofuranocoumarin glycosides, and one adenosine. All compounds were isolated for the first time from the genus Clausena, including a new aromatic glycoside (1), a new dihydrofuranocoumarin glycoside (6), and two new sesquiterpene glycosides (8 and 9). The phytochemical structures of the isolates were elucidated using spectroscopic analyses including NMR and MS. The existence of these compounds demonstrates the taxonomic significance of C. lansium in the genus Clausena and suggests that some glycosides from this plant probably play a role in the anticancer activity of C. lansium to some extent.


Assuntos
Clausena/química , Compostos Fitoquímicos/análise , Estrutura Molecular , Especificidade de Órgãos , Compostos Fitoquímicos/química , Folhas de Planta/química , Caules de Planta/química
4.
Zhongguo Zhong Yao Za Zhi ; 44(10): 2096-2101, 2019 May.
Artigo em Chinês | MEDLINE | ID: mdl-31355567

RESUMO

The chemical constituents from the stems and leaves of Clausena emarginata were separated and purified by column chromatographies on silica gel,ODS,Sephadex LH-20,and PR-HPLC. The structures of the isolated compounds were identified on the basis of physicochemical properties and spectroscopic analysis,as well as comparisons with the data reported in the literature. Sixteen compounds were isolated from the 90% ethanol extract of the stems and leaves of C. emarginata,which were identified as siamenol( 1),murrastanine A( 2),3-formyl-1,6-dimethoxycarbazole( 3),3-methoxymethylcarbazole( 4),3-methylcarbazole( 5),murrayafoline A( 6),3-formylcarbazole( 7),3-formyl-1-hydroxycarbazole( 8),3-formyl-6-methoxycarbazole( 9),murrayanine( 10),murrayacine( 11),girinimbine( 12),nordentatin( 13),chalepin( 14),8-hydroxy-6-methoxy-3-pentylisocoumarin( 15) and ethyl orsellinate( 16). Compounds 1-4,14-16 were isolated from C. emarginata for the first time. Among them,compounds 1,2,15 and 16 were isolated from the genus Clausena for the first time. All isolated compounds were evaluated for their cytotoxic activities against five human cancer cell lines: HL-60,SMMC-7721,A-549,MCF-7 and SW480 in vitro. Compounds 12 and 14 showed significant inhibitory effects against various human cancer cell lines with IC_(50) values comparable to those of doxorubicin.


Assuntos
Antineoplásicos Fitogênicos/farmacologia , Clausena/química , Compostos Fitoquímicos/farmacologia , Antineoplásicos Fitogênicos/isolamento & purificação , Linhagem Celular Tumoral , Doxorrubicina , Humanos , Compostos Fitoquímicos/isolamento & purificação , Folhas de Planta/química , Caules de Planta/química
5.
J Agric Food Chem ; 67(20): 5764-5771, 2019 May 22.
Artigo em Inglês | MEDLINE | ID: mdl-31083994

RESUMO

Clausena lansium, also known as wampee, is a species of strongly scented evergreen trees belonging to the genus Clausena (Rutaceae), which is native to southern China. Its ripe fruits have been consumed as a very popular fruit and reported to possess a range of biological activities. To study the potential health-promoting constituents from the fruits of C. lansium, a chemical investigation on its fruits was thus carried out. In this study, 16 carbazole alkaloids (1-16), including six new carbazole alkaloids, clausenalansines A-F (1-6), were separated from the fruits of C. lansium. The molecular structures of these isolated new carbazole alkaloids (1-6) were ambiguously established on the basis of comprehensive spectroscopic methods. The known analogues (7-16) were determined via comparing their experimental data with those described in the literature, which were separated from C. lansium for the first time. All these isolated alkaloids were tested in vitro for their neuroprotective effects against 6-hydroxydopamine induced cell death in human neuroblastoma SH-SY5Y cells. Carbazole alkaloids 1-16 displayed remarkable neuroprotective effects possessing the EC50 values ranging from 0.36 ± 0.02 to 10.69 ± 0.15 µM. These findings indicate that regular consumption of the fruits of C. lansium may help people prevent the occurrence of Parkinson's disease. In addition, the separation and identification of these carbazole alkaloids possessing remarkable neuroprotective effects from the fruits of C. lansium could be extremely important to the discovery of new agents for the prevention and treatment of Parkinson's disease.


Assuntos
Alcaloides/química , Carbazóis/química , Clausena/química , Medicamentos de Ervas Chinesas/química , Fármacos Neuroprotetores/química , Alcaloides/isolamento & purificação , Alcaloides/farmacologia , Carbazóis/isolamento & purificação , Carbazóis/farmacologia , Sobrevivência Celular/efeitos dos fármacos , Medicamentos de Ervas Chinesas/isolamento & purificação , Medicamentos de Ervas Chinesas/farmacologia , Frutas/química , Humanos , Estrutura Molecular , Fármacos Neuroprotetores/isolamento & purificação , Fármacos Neuroprotetores/farmacologia
6.
Molecules ; 24(7)2019 04 09.
Artigo em Inglês | MEDLINE | ID: mdl-30970599

RESUMO

Essential oils (EOs) have been shown to have a diversity of beneficial human health effects. Clausena is a large and highly diverse genus of plants with medicinal and cosmetic significance. The aim of this study was to analyze the composition of Clausena lansium EOs and to investigate their potential antifungal effects. The chemical compositions of Clausena lansium EOs obtained by hydrodistillation were analyzed by gas chromatography-mass spectrometry (GC-MS). A total of 101 compounds were identified among the diverse extracts of C. lansium. EOs of leaves and pericarps from different cultivars (Hainan local wampee and chicken heart wampee) collected in Hainan (China) were classified into four clusters based on their compositions. These clusters showed different antifungal activities against five Candida species (C. albicans, C. tropicalis, C. glabrata, C. krusei and C. parapsilosis) using the disc diffusion method. Clausena lansium EOs of pericarps displayed noteworthy antifungal activitives against all the tested Candida strains with inhibition zone diameters in the range of 11.1­23.1 mm. EOs of leaves showed relatively low antifungal activities with inhibition zone diameters in the range of 6.5­22.2 mm. The rank order of antifungal activities among the four EO clusters was as follows: Cluster IV> Cluster III > Cluster I ≥ Cluster II. These results represent the first report about the correlation between chemical composition of C. lansium EOs and antifungal activity. Higher contents of ß-phellandrene, ß-sesquiphellandrene and ß-bisabolene in EOs of pericarps were likely responsible for the high antifungal activity of Cluster IV EOs. Taken together, our results demonstrate the chemical diversity of Clausena lansium EOs and their potential as novel antifungal agents for candidiasis caused by Candida spp. Furthermore, the obtained results showing a wide spectrum of antifungal activities provide scientific evidence for the traditional use of these plants.


Assuntos
Antifúngicos , Candida/crescimento & desenvolvimento , Clausena/química , Óleos Voláteis , Antifúngicos/química , Antifúngicos/farmacologia , Candidíase/tratamento farmacológico , Cicloexenos/química , Cicloexenos/farmacologia , Cromatografia Gasosa-Espectrometria de Massas , Monoterpenos/química , Monoterpenos/farmacologia , Óleos Voláteis/química , Óleos Voláteis/farmacologia , Sesquiterpenos/química , Sesquiterpenos/farmacologia , Relação Estrutura-Atividade
8.
Phytomedicine ; 55: 31-39, 2019 Mar 01.
Artigo em Inglês | MEDLINE | ID: mdl-30668441

RESUMO

BACKGROUND: Clausena excavata Burm.f. (Rutaceae) has been used for the treatment of stomach disorders including peptic ulcer. PURPOSE: In this study, we aimed to investigate dentatin isolated from C. excavata Burm.f., for anti-ulcer activity against ethanol ulcer model in rats. METHODS: Gastric acid output, ulcer index, serum profile, histological evaluation using Hematoxylin and eosin (HE), periodic acid Schiff base stainings and immunohistochemical localization for heat shock proteins 70 (HSP70) were all investigated. Possible involvement of reduced glutathione (GSH), lipid peroxidation, prostaglandin E2 (PGE2), superoxide dismutase (SOD) enzymes, radical scavenging, and anti-Helicobacter pylori activity were investigated. RESULTS: Dentatin showed anti-secretory activity against the pylorus ligature model and protected the gastric mucosa from ethanol ulceration, as revealed by the improved macroscopic and histological appearance. Dentatin significantly increased the gastric homogenate content of PGE2 GSH and SOD. Dentatin inhibited the lipid peroxidation as revealed by the reduced gastric content of malondialdehyde (MDA). Moreover, dentatin up-regulated HSP70 expression. However, dentatin showed insignificant anti-H. pylori activity. CONCLUSION: Dentatin possesses gastro-protective activity, which could be attributed to the anti-secretory, mucus production, anti-oxidant, and HSP70 activities.


Assuntos
Antiulcerosos/farmacologia , Antioxidantes/farmacologia , Compostos Heterocíclicos com 3 Anéis/farmacologia , Úlcera Gástrica/tratamento farmacológico , Animais , Clausena/química , Etanol/efeitos adversos , Feminino , Mucosa Gástrica/efeitos dos fármacos , Mucosa Gástrica/metabolismo , Glutationa/metabolismo , Proteínas de Choque Térmico HSP70/metabolismo , Helicobacter pylori/efeitos dos fármacos , Peroxidação de Lipídeos/efeitos dos fármacos , Masculino , Malondialdeído/metabolismo , Muco/efeitos dos fármacos , Ratos Sprague-Dawley , Úlcera Gástrica/induzido quimicamente , Úlcera Gástrica/patologia , Superóxido Dismutase/metabolismo
9.
Nat Prod Res ; 33(23): 3337-3342, 2019 Dec.
Artigo em Inglês | MEDLINE | ID: mdl-29772923

RESUMO

A phytochemical investigation on the stems and leaves of Clausena emarginata led to the isolation of a previously undescribed carbazole alkaloid, clausemargine A (1), together with 11 known analogues (2-12). The structure of 1 was elucidated by extensive spectroscopic methods and the known compounds were identified by comparisons with data reported in the literature. All known compounds (2-12) were isolated from C. emarginata for the first time. All isolated compounds were evaluated for their their antiproliferative activities against five human cancer cell lines: HL-60, SMMC-7721, A-549, MCF-7 and SW480 in vitro. Compounds 1-12 showed significant antiproliferative effects with IC50 values ranging from 0.28 to 15.18 µM.


Assuntos
Alcaloides/química , Alcaloides/farmacologia , Antineoplásicos Fitogênicos/química , Antineoplásicos Fitogênicos/farmacologia , Clausena/química , Carbazóis/química , Linhagem Celular Tumoral , Ensaios de Seleção de Medicamentos Antitumorais , Humanos , Espectroscopia de Ressonância Magnética , Estrutura Molecular , Folhas de Planta/química
10.
Nat Prod Res ; 33(18): 2631-2637, 2019 Sep.
Artigo em Inglês | MEDLINE | ID: mdl-29667419

RESUMO

A phytochemical investigation on the stems and leaves of Clausena lenis led to the isolation of a new furanocoumarin, clauselenisin A (1), together with five known analogues (2-6). The structure of 1 was elucidated by extensive spectroscopic methods and the known compounds were identified by comparisons with data reported in the literature. All known compounds (2-6) were isolated from C. lenis for the first time. All isolated compounds were evaluated for their their antiproliferative activities against five human cancer cell lines: HL-60, SMMC-7721, A-549, MCF-7 and SW480 in vitro. Compounds 1-6 showed significant antiproliferative effects with IC50 values ranging from 0.36 to 16.48 µM.


Assuntos
Antineoplásicos Fitogênicos/química , Antineoplásicos Fitogênicos/farmacologia , Clausena/química , Furocumarinas/química , Furocumarinas/farmacologia , Células A549 , Linhagem Celular Tumoral , Ensaios de Seleção de Medicamentos Antitumorais , Células HL-60 , Humanos , Espectroscopia de Ressonância Magnética , Estrutura Molecular , Folhas de Planta/química , Caules de Planta/química
11.
Molecules ; 24(1)2018 Dec 27.
Artigo em Inglês | MEDLINE | ID: mdl-30591670

RESUMO

A rapid and sensitive ionic liquid (IL) based headspace gas chromatography-mass spectrometry (HS-GC-MS) method was developed for analyzing volatile components in leaf, pericarp, and seed of Clausena lansium from different areas in Hainan Province, China. HS efficiencies were carefully investigated by using three ILs and water as matrix media. Extraction parameters, including equilibrium temperature, equilibrium time, and stirring rate had been evaluated and optimized by using an orthogonal design with OA9(3³) table. Under the optimized condition of IL-based HS-GC-MS, only 100 mg of sample and 2 mL of [Bmim][BF4] were needed to comprehensively and accurately analyze the volatile components in Clausena lansium. By utilizing a cluster analysis, six clusters were obtained for ninety components. This method was simpler, more rapid, and more sensitive when compared with previously reported methods for analyzing and identifying volatile components in Clausena lansium. The results may provide a theoretical basis for further exploitation of Clausena lansium.


Assuntos
Clausena/química , Cromatografia Gasosa-Espectrometria de Massas/métodos , Líquidos Iônicos/química , Compostos Orgânicos Voláteis/análise , Análise de Variância , Filogenia , Folhas de Planta/química , Sementes/química
12.
Chin J Nat Med ; 16(7): 509-512, 2018 Jul.
Artigo em Inglês | MEDLINE | ID: mdl-30080650

RESUMO

The present study carried out a phytochemical investigation of the methanol extract of the branches and leaves of Clausena lansium and afforded nine carbazole alkaloids (compounds 1-9) including two new carbazole alkaloids, claulansiums A and B (compounds 1 and 2). The new compounds were elucidated on the basis of extensive spectroscopic data (MS, NMR, IR, and UV) and the known compounds were identified by comparing spectroscopic data with those reported in literature. All the isolated compounds were tested for their cytotoxic activity against A549 and Hela cancer cell lines. Our results showed that compounds 2-6 exhibited varying degrees of cytotoxicity to cancer cells, with IC50 values ranging from 8.67 to 98.89 µmol·L-1.


Assuntos
Alcaloides/química , Alcaloides/toxicidade , Clausena/química , Extratos Vegetais/química , Folhas de Planta/química , Caules de Planta/química , Células A549 , Alcaloides/isolamento & purificação , Antineoplásicos/química , Antineoplásicos/isolamento & purificação , Antineoplásicos/toxicidade , Carbazóis/química , Carbazóis/isolamento & purificação , Carbazóis/toxicidade , Linhagem Celular Tumoral , Sobrevivência Celular/efeitos dos fármacos , Células HeLa , Humanos , Estrutura Molecular , Extratos Vegetais/toxicidade , Plantas Medicinais/química
13.
Biomed Res Int ; 2018: 7093691, 2018.
Artigo em Inglês | MEDLINE | ID: mdl-29977915

RESUMO

Clausena lansium (Lour.) Skeels, commonly known as "wampee," is an excellent food ingredient of medicinal value. Effects of leaf developmental stages on the composition of phenolics, flavonoids, and antioxidant activity were investigated. Phenolics composition was studied using HPLC-PAD, whereas antioxidant activity was estimated by oxygen radical absorbance capacity (ORAC) and cellular antioxidant activity (CAA) assays. Increase in bound flavonoids, quercetin, and cellular antioxidant activity was observed in bound and free fractions at different stages of leaf development. Predominantly, quercetin and ferulic acid contents were high in free and bound fractions of old leaves. In addition, phenolic components depicted highly significant positive association (p < 0.05) with antioxidant activity. Overall, old leaves of wampee have utility value similar to leaf buds, so they could be a more sustainable and economical source of bioactive compounds for commercial application in nutraceutical and pharmaceutical industries.


Assuntos
Antioxidantes/farmacologia , Clausena/química , Extratos Vegetais/farmacologia , China , Flavonoides , Fenóis , Folhas de Planta/crescimento & desenvolvimento
14.
Fitoterapia ; 128: 20-25, 2018 Jul.
Artigo em Inglês | MEDLINE | ID: mdl-29723562

RESUMO

Five new amide alkaloids (1-3, 5-6) were isolated from the seeds of Clausena lansium together with one new natural product (4) and four known analogues (7-10). The structures of the new amide alkaloids were elucidated based on a comprehensive spectroscopic data analysis including 1D and 2D NMR as well as HRESIMS, and by comparison with the literature. The bioactivity results showed that compound 8 expressed potent nematicidal activity against Panagrellus redivevus, with IC50 value of 0.12 mM, while compounds 3 and 5 presented moderate nematicidal activity with IC50 values of 2.75 and 3.93 mM, respectively (abamectin as the positive control with IC50 value of 1.05 mM).


Assuntos
Alcaloides/isolamento & purificação , Amidas/isolamento & purificação , Anti-Helmínticos/isolamento & purificação , Clausena/química , Sementes/química , Alcaloides/farmacologia , Amidas/farmacologia , Animais , Anti-Helmínticos/farmacologia , Estrutura Molecular , Tylenchida/efeitos dos fármacos
15.
Asian Pac J Cancer Prev ; 19(4): 917-922, 2018 Apr 25.
Artigo em Inglês | MEDLINE | ID: mdl-29693341

RESUMO

Clausena excavata Burm f. is used by traditional healers to treat cancer patients in South East Asia. The use of the plant and its compounds is based on Asian folklore with little or no scientific evidence supporting the therapeutic efficacy The current study aimed to determine the effect of pure clausenidin isolated from C. excavata on caspase-8-induced cell death as well as angiogenesis in the HepG2 hepatocellular carcinoma cell line. Caspase-8 and extrinsic death receptor protein expression was determined using spectrophotometry and protein profile arrays, respectively. Ultrastructural analysis of clausenidin-treated cells was conducted using transmission electron microscopy. In addition, anti-angiogenic effects of clausenidin were investigated by Western blot analysis. Clausenidin significantly (p<0.05) increased the activity of caspase-8 and expression of protein components of the death inducing signaling complex (DISC) in HepG2 cells. Ultrastructural analysis of the clausenidin-treated HepG2 cells revealed morphological abnormalities typical of apoptosis. Furthermore, clausenidin significantly (p<0.05) decreased the expression of vascular endothelial growth factor (VEGF). Therefore, clausenidin is a potential anti-angiogenic agent which may induce apoptosis of hepatocellular carcinoma cells.


Assuntos
Apoptose/efeitos dos fármacos , Carbazóis/farmacologia , Carcinoma Hepatocelular/patologia , Caspase 3/metabolismo , Clausena/química , Extratos Vegetais/farmacologia , Fator A de Crescimento do Endotélio Vascular/metabolismo , Carcinoma Hepatocelular/tratamento farmacológico , Carcinoma Hepatocelular/metabolismo , Proliferação de Células/efeitos dos fármacos , Humanos , Neoplasias Hepáticas/tratamento farmacológico , Neoplasias Hepáticas/metabolismo , Neoplasias Hepáticas/patologia , Espécies Reativas de Oxigênio/metabolismo , Células Tumorais Cultivadas
16.
Phytochemistry ; 151: 1-8, 2018 Jul.
Artigo em Inglês | MEDLINE | ID: mdl-29625192

RESUMO

Nine undescribed carbazole and quinoline alkaloids, named dunnines A-E, and 14 known analogues were isolated from the leaves and stems of Clausena dunniana. Their structures were elucidated on the basis of comprehensive analysis of NMR and HRMS spectroscopic data, and the absolute configurations were assigned via comparison of their specific rotations and calculated and experimental ECD data. (±)-Dunnines A-C and (±)-clausenawalline A are four pairs of biscarbazole atropisomers and (±)-dunnine D is a pair of dihydropyranocarbazole enantiomers. They were separated by chiral HPLC to obtain the optically pure compounds. Three compounds showed weak inhibitory effects on nitric oxide production stimulated by lipopolysaccharide in BV-2 microglial cells (IC50 > 50 µM); five compounds could significantly promote insulin secretion in HIT-T15 cell line (1.9-3.1-fold of the control, p < 0.01) at 40 µM, and nine compounds could inhibit the apoptosis of PC12 cell induced by 6-hydroxydopamine with IC50 values in the range of 10.9-47.2 µM.


Assuntos
Apoptose/efeitos dos fármacos , Carbazóis/farmacologia , Clausena/química , Insulina/metabolismo , Óxido Nítrico/antagonistas & inibidores , Quinolinas/farmacologia , Animais , Carbazóis/química , Carbazóis/isolamento & purificação , Linhagem Celular , Relação Dose-Resposta a Droga , Humanos , Lipopolissacarídeos/antagonistas & inibidores , Lipopolissacarídeos/farmacologia , Camundongos , Estrutura Molecular , Óxido Nítrico/biossíntese , Oxidopamina , Células PC12 , Quinolinas/química , Quinolinas/isolamento & purificação , Ratos , Relação Estrutura-Atividade
17.
Bioorg Chem ; 77: 387-392, 2018 04.
Artigo em Inglês | MEDLINE | ID: mdl-29421715

RESUMO

Two new carbazole alkaloids 1 and 2, and eleven known congeners 3-13 were isolated and identified from Clausena sanki for the first time. Their structures were elucidated on the basis of extensive UV, IR, MS, NMR spectroscopic data and comparison with literatures. The compounds 1-13 were evaluated by MTT assay to determine whether they decreased VEGF-mediated cell proliferation in HUVECs with Axitinib as positive control. Among them, compounds 1, 2, 6, 8, and 13 (µM) exhibited moderate antiangiogenic activities, which inhibited VEGF-induced HUVEC proliferation in vitro with IC50 values of 12.1 (C.I. 8.2-15.2), 58.1 (C.I. 56.3-63.4), 13.7 (C.I. 9.2-15.4), 16.0 (C.I. 9.5-16.4), and 63.2 (C.I. 57.8-65.7) µM, respectively. Moreover, the antiangiogenic activities of compounds 1-13 were evidenced in vivo in the zebrafish embryo model. As a result, compounds 1, 2, 6, 8, and 13 showed effectively suppress angiogenesis. These research results may guide the search for new natural products with antiangiogenic attributes.


Assuntos
Alcaloides/farmacologia , Inibidores da Angiogênese/farmacologia , Carbazóis/farmacologia , Clausena/química , Fatores de Crescimento do Endotélio Vascular/antagonistas & inibidores , Alcaloides/química , Alcaloides/isolamento & purificação , Inibidores da Angiogênese/química , Inibidores da Angiogênese/isolamento & purificação , Animais , Carbazóis/química , Carbazóis/isolamento & purificação , Proliferação de Células/efeitos dos fármacos , Relação Dose-Resposta a Droga , Células Endoteliais da Veia Umbilical Humana/efeitos dos fármacos , Células Endoteliais da Veia Umbilical Humana/metabolismo , Humanos , Estrutura Molecular , Relação Estrutura-Atividade , Fatores de Crescimento do Endotélio Vascular/metabolismo , Peixe-Zebra/embriologia
18.
Biomed Pharmacother ; 99: 253-260, 2018 Mar.
Artigo em Inglês | MEDLINE | ID: mdl-29334669

RESUMO

Clausena excavata (C. excavata) has been used as a traditional medicine for the treatment of abdominal pain, enteritis, dysentery, and malaria. The present study was designed to evaluate the effect of a 50% ethanol extract of C. excavata (ECE) on weight loss, adipocyte size, and obesity-related biochemical parameters in high-fat diet (HFD)-induced obese mice. After 6 weeks of HFD + ECE administration, HFD-induced total fat, subcutaneous fat, and visceral fat were evaluated by micro-computed tomography. The serum levels of triglyceride (TG), total cholesterol (TCH), high-density lipoprotein (HDL) cholesterol, and low-density lipoprotein (LDL) cholesterol were evaluated with a biochemical analyzer, and leptin and adiponectin levels in the serum were assessed via enzyme-linked immunoassay (ELISA). Moreover, adipocyte size and lipid formation in the liver were examined. We found that weight gain, epididymal fat pad weight, adipocyte size, and lipid formation were markedly attenuated in the livers of HFD-induced obese mice treated with ECE. Furthermore, TG, TCH, and leptin decreased in the serum, whereas adiponectin increased. In conclusion, our data show that ECE has potent anti-obesity activity in vivo and support the development of ECE as a potential therapeutic agent for the treatment of obesity.


Assuntos
Fármacos Antiobesidade/uso terapêutico , Clausena/química , Obesidade/tratamento farmacológico , Extratos Vegetais/uso terapêutico , Adipócitos/efeitos dos fármacos , Adipócitos/metabolismo , Adipócitos/patologia , Adiponectina/sangue , Animais , Fármacos Antiobesidade/farmacologia , Cromatografia Líquida de Alta Pressão , Dieta Hiperlipídica , Leptina/sangue , Lipídeos/sangue , Masculino , Camundongos Endogâmicos C57BL , Camundongos Obesos , Obesidade/sangue , Obesidade/patologia , Extratos Vegetais/administração & dosagem , Extratos Vegetais/farmacologia
19.
J Food Sci ; 83(1): 212-220, 2018 Jan.
Artigo em Inglês | MEDLINE | ID: mdl-29227535

RESUMO

Clausena lansium (Lour.) Skeels (Wampee) is widely grown in China and considered as a healthy fruit. Its leaves are also considered as traditional herbs. This study analyzed polyphenol compounds in polyphenol extracts of the leaves C. lansium (lour.) Skeels (PEL) and investigated the protective effect of PEL against hyperglycemia and hyperlipidemia in T2DM rats. The result showed that PEL is composed mainly of gallic acid, chlorogenic acid, coffee acid, ferulic acid, and rutin. PEL could obviously relieve some symptoms of T2DM rats, including emaciation, hyperhidrosis, polyphagia, diuresis, liver swelling, kidney, and pancreas hypertrophy, as well as reduce fasting blood glucose. Moreover, the supplementation of PEL significantly ameliorated lipids disorder and protected liver in T2DM rats, including fat accumulation, improvement of lipid distribution and hepatocyte protection. These results indicate that the Oral of PEL have potential effects of against hyperglycemia and hyperlipidemia in diabetic disorders. PRACTICAL APPLICATION: The leaves Clausena lansium (lour.) Skeels is rich in polyphenol and other ingredients. In this research, the preliminary study shows that PEL can reduce fasting blood glucose and improve lipids disorder in rats, which will bring to diabetic patients a way to improve the disease and enhance the quality of life. The PEL therefore can be used for the production of pharmaceutical raw materials and the design of novel functional foods by simple conversion.


Assuntos
Clausena/química , Diabetes Mellitus Experimental/tratamento farmacológico , Hipoglicemiantes/farmacologia , Extratos Vegetais/farmacologia , Folhas de Planta/química , Polifenóis/farmacologia , Animais , China , Colesterol/sangue , Frutas/química , Hipolipemiantes/farmacologia , Fígado/efeitos dos fármacos , Fígado/metabolismo , Masculino , Ratos , Ratos Wistar , Triglicerídeos/sangue
20.
Bioorg Chem ; 76: 359-364, 2018 02.
Artigo em Inglês | MEDLINE | ID: mdl-29232633

RESUMO

Five new carbazole alkaloids, clausehainanines A-E (1-5), together with seven known analogues (6-12) were isolated from the stems and leaves of C. hainanensis. Their structures were elucidated by extensive spectroscopic methods. Among them, compounds 1-5 were an unusual type of carbazole alkaloids, possessing diverse isopentenyl derivatives as substituents at C-2. All isolated compounds were evaluated for their antiproliferative activities against five human cancer cell lines: HL-60, SMMC-7721, A-549, MCF-7 and SW480 in vitro. Alkaloids 1-12 showed significant antiproliferative effects against various human cancer cell lines with IC50 values ranging from 0.12 to 15.56 µM. These findings suggest that the discoveries of these carbazole alkaloids with significant cytotoxic activities isolated from C. hainanensis could be of great importance to the development of new anticancer agents.


Assuntos
Alcaloides/farmacologia , Antineoplásicos Fitogênicos/farmacologia , Carbazóis/farmacologia , Clausena/química , Alcaloides/química , Alcaloides/isolamento & purificação , Antineoplásicos Fitogênicos/química , Antineoplásicos Fitogênicos/isolamento & purificação , Carbazóis/química , Carbazóis/isolamento & purificação , Linhagem Celular Tumoral , Cisplatino/farmacologia , Doxorrubicina/farmacologia , Ensaios de Seleção de Medicamentos Antitumorais , Humanos , Estrutura Molecular , Folhas de Planta/química , Caules de Planta/química
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