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1.
BMC Gastroenterol ; 21(1): 295, 2021 Jul 15.
Artigo em Inglês | MEDLINE | ID: mdl-34266417

RESUMO

BACKGROUND: High-resolution anorectal manometry (HRAM) has been developed to improve measurement of anorectal functions. This study aims to identify normal HRAM values in healthy young Vietnamese adults. METHODS: We conducted a cross-sectional study at the National Hospital of Traditional Medicine (Hanoi, Vietnam) from July through December 2014. Healthy young adults were invited to participate in the study. All anorectal measurement values were performed using the ISOLAB high-resolution manometry system. Differences between groups were analyzed using Student's t-tests. RESULTS: Thirty healthy young adults, including 15 males and 15 females aged 19-26 years, were recruited. Mean functional anal canal length was 3.4 ± 0.5 cm (range: 2.4-4.8 mm). Mean maximum resting pressure, mean maximum squeezing pressure, mean maximum coughing pressure, and mean maximum strain pressure were 65.5, 168.0, 125.9, and 84.2 mm Hg, respectively. All anal pressure values were significantly different between males and females. For rectal sensation measurements, only the volume at first sensation was significantly higher in males than in females. CONCLUSIONS: This study provides normal HRAM value for healthy young adults in Vietnam. Sex may influence anal pressure and first rectal sensation values in this cohort. Further studies should be conducted in order to improve the quality of HRAM normal values and to confirm the effects of sex.


Assuntos
Canal Anal , Reto , Estudos Transversais , Feminino , Humanos , Masculino , Manometria , Valores de Referência , Vietnã , Adulto Jovem
2.
Bioorg Med Chem Lett ; 25(5): 1129-34, 2015 Mar 01.
Artigo em Inglês | MEDLINE | ID: mdl-25637363

RESUMO

Six new phenolics, scutellariosides A-F (1-3, 5-6, and 8), together with six known compounds (4, 7, 9-12) were isolated from the whole plant of Scutellaria indica (Labiatae). The chemical structures of these compounds were determined by spectroscopic analyses including 2D NMR. Their anti-inflammatory activities were evaluated against LPS-induced NO production in macrophage RAW 264.7 cells. Among them, compounds 10-12 had inhibitory effects with IC50 values ranging from 7.2 to 27.8µM. Compound 12 reduced LPS-induced iNOS expression in a dose-dependent manner.


Assuntos
Anti-Inflamatórios/química , Anti-Inflamatórios/farmacologia , Macrófagos/efeitos dos fármacos , Fenóis/química , Fenóis/farmacologia , Scutellaria/química , Animais , Anti-Inflamatórios/isolamento & purificação , Linhagem Celular , Flavonoides/química , Flavonoides/isolamento & purificação , Flavonoides/farmacologia , Lipopolissacarídeos/imunologia , Macrófagos/imunologia , Camundongos , Óxido Nítrico/antagonistas & inibidores , Óxido Nítrico/imunologia , Óxido Nítrico Sintase Tipo II/antagonistas & inibidores , Óxido Nítrico Sintase Tipo II/imunologia , Fenóis/isolamento & purificação , Extratos Vegetais/química , Extratos Vegetais/isolamento & purificação , Extratos Vegetais/farmacologia
3.
Molecules ; 20(1): 1059-77, 2015 Jan 09.
Artigo em Inglês | MEDLINE | ID: mdl-25584835

RESUMO

An HPLC-DAD method for the quality control of wild and cultivated Ganoderma lucidum (Linhzhi) and related species samples was developed and validated. The quantitative determination of G. lucidum and its related species using 14 triterpene constituents, including nine ganoderma acids (compounds 4-12), four alcohols (compounds 13-16), and one sterol (ergosterol, 17) were reported. The standard curves were linear over the concentration range of 7.5-180 µg/mL. The LOD and LOQ values for the analyses varied from 0.34 to 1.41 µg/mL and from 1.01 to 4.23 µg/mL, respectively. The percentage recovery of each reference compound was found to be from 97.09% to 100.79%, and the RSD (%) was less than 2.35%. The precision and accuracy ranged from 0.81%-3.20% and 95.38%-102.19% for intra-day, and from 0.43%-3.67% and 96.63%-103.09% for inter-day, respectively. The study disclosed in detail significant differences between the quantities of analyzed compounds in different samples. The total triterpenes in wild Linhzhi samples were significantly higher than in cultivated ones. The total constituent contents of the five related Linhzhi samples were considerably lower than that in the G. lucidum specimens, except for G. australe as its constituent content outweighed wild Linhzhi's content by 4:1.


Assuntos
Cromatografia Líquida de Alta Pressão/métodos , Ganoderma/química , Triterpenos/análise , Análise de Regressão , Reprodutibilidade dos Testes , Triterpenos/química , Triterpenos/isolamento & purificação , Vietnã
4.
Bioorg Med Chem Lett ; 24(1): 168-72, 2014 Jan 01.
Artigo em Inglês | MEDLINE | ID: mdl-24332631

RESUMO

Angiogenesis plays a critical role in embryonic development and various physiological processes. However, excessive angiogenesis is associated with several pathological conditions including cancer. Angiogenesis is closely related to tumor growth, invasion and metastasis, and is considered a prime target for anticancer therapy. In this study, two new mono cassaine diterpenoid amides (1, 5) and four known compounds (2-4, 6) were isolated from the bark of Erythrophleum fordii (Leguminosae). Their chemical structures were established mainly by 1D and 2D NMR techniques and mass spectrometry. The effects of isolates on endothelial tube formation on Matrigel were investigated. Among them, compound 3 was found to have the most potent inhibitory effect on the capillary-like structure formation of human umbilical vein endothelial cells (HUVECs).


Assuntos
Alcaloides/farmacologia , Inibidores da Angiogênese/farmacologia , Diterpenos/farmacologia , Fabaceae/química , Células Endoteliais da Veia Umbilical Humana/efeitos dos fármacos , Abietanos , Alcaloides/química , Alcaloides/isolamento & purificação , Inibidores da Angiogênese/química , Inibidores da Angiogênese/isolamento & purificação , Proliferação de Células/efeitos dos fármacos , Diterpenos/química , Diterpenos/isolamento & purificação , Relação Dose-Resposta a Droga , Humanos , Conformação Molecular , Casca de Planta/química , Relação Estrutura-Atividade
5.
Bioorg Med Chem Lett ; 24(21): 4989-94, 2014 Nov 01.
Artigo em Inglês | MEDLINE | ID: mdl-25278231

RESUMO

Cytotoxic activity-guided fractionation of Erythrophleum fordii led to the isolation of two new cassaine diterpenoid-diterpenoid amide dimers, erythrophlesins H-I (1, 2). Spectral data indicated that they consist of asymmetrical dimeric structure via an ester bond between two cassaine diterpenoids. MTT assay confirmed that compound 1, erythrophlesin H, had the strongest cytotoxic effect toward the human prostate cancer cell line, PC-3. The molecular mechanism by which this compound induced apoptosis cell in prostate cancer remains unknown. Erythrophlesin H induced apoptosis in a dose-dependent manner. Acridine orange and annexin V-FITC/PI double staining confirmed that erythrophlesin H effectively induces apoptosis in PC-3 cells.


Assuntos
Alcaloides/química , Amidas/farmacologia , Antineoplásicos Fitogênicos/farmacologia , Apoptose/efeitos dos fármacos , Diterpenos/farmacologia , Fabaceae/química , Neoplasias da Próstata/tratamento farmacológico , Abietanos , Amidas/química , Antineoplásicos Fitogênicos/química , Proliferação de Células/efeitos dos fármacos , Diterpenos/química , Humanos , Técnicas In Vitro , Masculino , Estrutura Molecular , Neoplasias da Próstata/patologia , Espectrometria de Massas por Ionização por Electrospray , Células Tumorais Cultivadas
6.
Biol Res ; 47: 20, 2014 May 27.
Artigo em Inglês | MEDLINE | ID: mdl-25028057

RESUMO

BACKGROUND: This study evaluated the cytotoxic activity of extracts from Caesalpinia sappan heartwood against multiple cancer cell lines using an MTT cell viability assay. The cell death though induction of apoptosis was as indicated by DNA fragmentation and caspase-3 enzyme activation. RESULTS: A methanol extract from C. sappan (MECS) showed cytotoxic activity against several of the cancer cell lines. The most potent activity exhibited by the MECS was against HeLa cells with an IC50 value of 26.5 ± 3.2 µg/mL. Treatment of HeLa cells with various MECS concentrations resulted in growth inhibition and induction of apoptosis, as indicated by DNA fragmentation and caspase-3 enzyme activation. CONCLUSION: This study is the first report of the anticancer properties of the heartwood of C. sappan native to Vietnam. Our findings demonstrate that C. sappan heartwood may have beneficial applications in the field of anticancer drug discovery.


Assuntos
Antineoplásicos Fitogênicos/farmacologia , Apoptose , Caesalpinia/química , Extratos Vegetais/farmacologia , Feixe Vascular de Plantas/metabolismo , Animais , Antineoplásicos Fitogênicos/isolamento & purificação , Caspase 3/metabolismo , Linhagem Celular Tumoral , Proliferação de Células/efeitos dos fármacos , Sobrevivência Celular , Citotoxinas/farmacologia , Fragmentação do DNA , Ensaios de Seleção de Medicamentos Antitumorais/métodos , Ativação Enzimática/efeitos dos fármacos , Feminino , Formazans , Inibidores do Crescimento/farmacologia , Células HeLa , Humanos , Indicadores e Reagentes , Concentração Inibidora 50 , Metanol , Camundongos Endogâmicos C57BL , Sais de Tetrazólio , Vietnã
7.
Chem Pharm Bull (Tokyo) ; 62(2): 185-90, 2014.
Artigo em Inglês | MEDLINE | ID: mdl-24492589

RESUMO

A new megastigmane glycoside, galloyl linarionoside A (1), together with 13 known compounds (2-14) were isolated from the aerial parts of Aceriphyllum rossii ENGLER. (Saxifragaceae). The chemical structures of the isolated compounds were established mainly by using nuclear magnetic resonance spectra, mass spectrometry, and modified Mosher's method. Among the isolates, compounds 4, 5, 6 and 7 showed potent inhibitory activity against the lipopolysaccharide-induced nitric oxide production in RAW264.7 macrophage cells with IC50 values of 12.5, 9.5, 10.5 and 9.3 µM, respectively. The anti-inflammatory effect of compound 7 was accompanied by dose-dependent decreases in the production of inducible nitric oxide synthase and cyclooxygenase-2 proteins not in the inhibitor kappa B (IκB)-dependent nuclear factor-kappa B activation.


Assuntos
Anti-Inflamatórios/química , Anti-Inflamatórios/farmacologia , Macrófagos/efeitos dos fármacos , Macrófagos/imunologia , Óxido Nítrico/imunologia , Componentes Aéreos da Planta/química , Saxifragaceae/química , Animais , Anti-Inflamatórios/isolamento & purificação , Linhagem Celular , Proteínas I-kappa B/imunologia , Lipopolissacarídeos/imunologia , Camundongos , NF-kappa B/imunologia , Extratos Vegetais/química , Extratos Vegetais/isolamento & purificação , Extratos Vegetais/farmacologia
8.
Molecules ; 19(11): 19172-9, 2014 Nov 19.
Artigo em Inglês | MEDLINE | ID: mdl-25415478

RESUMO

A series of Lycopodium alkaloids, namely lycosquarosine A (1), acetylaposerratinine (2), huperzine A (3), huperzine B (4), 8α-hydrophlemariurine B (5), and huperzinine (6), has been isolated from Vietnamese Huperzia squarrosa. Among them, lycosquarosine A (1) is the new metabolite of the natural source. Lycosquarosine A completely inhibited AChE activity in a dose dependent manner with an IC50 value of 54.3 µg/mL, while acetylaposerratinine (2) showed stronger inhibitory activity than 1 with an IC50 value of 15.2 µg/mL. This result indicates that these alkaloids may be a potent source of AChE inhibitors.


Assuntos
Alcaloides/química , Alcaloides/farmacologia , Inibidores da Colinesterase/química , Inibidores da Colinesterase/farmacologia , Huperzia/química , Lycopodium/química , Concentração Inibidora 50 , Extratos Vegetais/química , Extratos Vegetais/farmacologia , Sesquiterpenos/química , Sesquiterpenos/farmacologia
9.
Bioorg Med Chem Lett ; 23(5): 1428-32, 2013 Mar 01.
Artigo em Inglês | MEDLINE | ID: mdl-23357630

RESUMO

Four new lanostane triterpenes, butyl lucidenate P (1), butyl lucidenate D(2) (2), butyl lucidenate E(2) (3) and butyl lucidenate Q (4) along with 11 known compounds (5-15) were isolated from the fruiting bodies of Ganoderma lucidum. Their chemical structures were established mainly by 1D and 2D NMR techniques and mass spectrometry. Their anti-inflammatory activity was evaluated against LPS-induced NO production in macrophage RAW 264.7 cells. Compounds 1, 3, 4, 9, 10 and 15 showed inhibitory potency with IC(50) values of 7.4, 6.4, 4.3, 9.4, 9.2 and 4.5 µM, respectively. Compounds 1, 3 and 15 dose-dependently reduced the LPS-induced iNOS expressions. Preincubation of cell with 1, 3 and 15 significantly suppressed LPS-induced expression of COX-2 protein.


Assuntos
Anti-Inflamatórios/química , Anti-Inflamatórios/farmacologia , Óxido Nítrico/antagonistas & inibidores , Reishi/química , Triterpenos/química , Triterpenos/farmacologia , Linhagem Celular Tumoral , Ciclo-Oxigenase 2/biossíntese , Ciclo-Oxigenase 2/metabolismo , Indução Enzimática/efeitos dos fármacos , Carpóforos/química , Humanos , Lipopolissacarídeos/farmacologia , Macrófagos/efeitos dos fármacos , Macrófagos/metabolismo , Óxido Nítrico/biossíntese , Óxido Nítrico/metabolismo , Óxido Nítrico Sintase Tipo II/antagonistas & inibidores , Óxido Nítrico Sintase Tipo II/biossíntese , Óxido Nítrico Sintase Tipo II/metabolismo , Ressonância Magnética Nuclear Biomolecular
10.
Biosci Biotechnol Biochem ; 77(12): 2378-82, 2013.
Artigo em Inglês | MEDLINE | ID: mdl-24317049

RESUMO

Two new phenolic compounds, caesalpiniaphenols G-H (1 and 2), were isolated from Vietnamese Caesalpinia sappan heartwood. The chemical structures were established mainly by extensive spectroscopic studies and chemical evidence. Compounds 1 and 2 showed potent inhibitory activity against HL-60 cancer cell lines with respective IC50 values of 16.7 and 22.5 µg/mL. Treating HL-60 cells with various concentrations of 1 resulted in growth inhibition and the induction of apoptosis.


Assuntos
Caesalpinia/química , Citotoxinas/farmacologia , Fenóis/farmacologia , Extratos Vegetais/farmacologia , Antineoplásicos/farmacologia , Apoptose/efeitos dos fármacos , Linhagem Celular Tumoral , Humanos , Concentração Inibidora 50 , Vietnã
11.
Phytother Res ; 27(9): 1419-22, 2013 Sep.
Artigo em Inglês | MEDLINE | ID: mdl-23192855

RESUMO

Two neolignans, 4'-methoxymagndialdehyde (1) and magnaldehyde B (2), were isolated from the stem bark of Magnolia officinalis (Magnoliaceae), evaluated for apoptosis-inducing effects in human cervical epitheloid carcinoma HeLa cells. The apoptosis-inducing activity of compounds 1 and 2 were assessed by DNA content using flow cytometric analysis. In the immunoblotting analysis, the treatment with 1 and 2 resulted in the cleavage of procaspase-8 and -3 and poly(ADP-ribose)polymerase into active forms. In addition, in vivo, the administration of 2 to Lewis lung carcinoma-inoculated mice evidenced a significant inhibition of tumor growth (volume) with reduction of 28.7% at concentration of 20 mg/kg, as compared with the control mice. These findings suggest that 2 can inhibit the proliferation of tumor cells, and might be an anti-tumoric agent.


Assuntos
Antineoplásicos Fitogênicos/farmacologia , Apoptose/efeitos dos fármacos , Lignanas/farmacologia , Magnolia/química , Animais , Carcinoma Pulmonar de Lewis , Caspase 3/metabolismo , Caspase 8/metabolismo , Proliferação de Células/efeitos dos fármacos , Células HeLa , Humanos , Masculino , Camundongos , Casca de Planta/química , Poli(ADP-Ribose) Polimerases/metabolismo
12.
Bioorg Med Chem Lett ; 22(24): 7436-9, 2012 Dec 15.
Artigo em Inglês | MEDLINE | ID: mdl-23127886

RESUMO

Two new phenolics, (3S,4R)-3,7,2',3'-tetrahydroxy-3,4-dihydro-9H-indeno[6,5-c]chromene (caesalpiniaphenol E, 1), and (3R,4S)-3,7-dihydroxy-3-(3'-methoxy-4'-hydroxyphenyl)-4-methoxychroman (caesalpiniaphenol F, 2), together with eleven known compounds (3-13), were isolated from the heartwood of Caesalpinia sappan. Their chemical structures were established mainly by 1D and 2D NMR techniques and mass spectrometry. Their anti-inflammatory activity was evaluated against LPS-induced NO production in macrophage RAW264.7 cells. Among them, compounds 10 and 13 showed strong inhibitory activities toward the LPS-induced NO production in macrophage RAW264.7 cells, with IC(50) values of 12.5 and 8.1 µm, respectively. In addition, compounds 10 and 13 inhibited the inductions of iNOS mRNA in dose-dependent manners, indicating that these compounds attenuated the synthesis of these transcripts at the transcriptional level.


Assuntos
Anti-Inflamatórios/farmacologia , Benzopiranos/farmacologia , Caesalpinia/química , Cromanos/farmacologia , Inibidores Enzimáticos/farmacologia , Macrófagos/efeitos dos fármacos , Animais , Anti-Inflamatórios/química , Anti-Inflamatórios/isolamento & purificação , Benzopiranos/química , Benzopiranos/isolamento & purificação , Linhagem Celular , Cromanos/química , Cromanos/isolamento & purificação , Relação Dose-Resposta a Droga , Inibidores Enzimáticos/química , Inibidores Enzimáticos/isolamento & purificação , Lipopolissacarídeos/antagonistas & inibidores , Lipopolissacarídeos/farmacologia , Macrófagos/metabolismo , Camundongos , Conformação Molecular , Óxido Nítrico/antagonistas & inibidores , Óxido Nítrico/biossíntese , Óxido Nítrico Sintase Tipo II/antagonistas & inibidores , Óxido Nítrico Sintase Tipo II/biossíntese , Óxido Nítrico Sintase Tipo II/metabolismo , RNA Mensageiro/antagonistas & inibidores , RNA Mensageiro/biossíntese , RNA Mensageiro/metabolismo , Relação Estrutura-Atividade
13.
J Nat Prod ; 75(12): 2069-75, 2012 Dec 28.
Artigo em Inglês | MEDLINE | ID: mdl-23234407

RESUMO

Four new phenolic compounds, caesalpiniaphenols A-D (1-4), together with eight known compounds were isolated from Caesalpinia sappan heartwood. The chemical structures were established mainly by NMR, MS, ECD, and Mosher's method. Compounds 4, 5, and 7 showed weak inhibitory activity against the LPS-induced NO production in macrophage RAW264.7 cells with IC(50) values of 12.2, 3.5, and 5.7 µM, respectively.


Assuntos
Anti-Inflamatórios não Esteroides/isolamento & purificação , Anti-Inflamatórios não Esteroides/farmacologia , Caesalpinia/química , Fenóis/isolamento & purificação , Fenóis/farmacologia , Animais , Anti-Inflamatórios não Esteroides/química , Concentração Inibidora 50 , Lipopolissacarídeos/farmacologia , Macrófagos/efeitos dos fármacos , Camundongos , Estrutura Molecular , Óxido Nítrico/análise , Óxido Nítrico/biossíntese , Ressonância Magnética Nuclear Biomolecular , Fenóis/química , República da Coreia , Madeira/química
14.
Bioorg Med Chem Lett ; 21(23): 6960-3, 2011 Dec 01.
Artigo em Inglês | MEDLINE | ID: mdl-22024033

RESUMO

A new alkaloid, methyl 2'-(7,8-dihydrosanguinarine-8-yl)acetate (1), together with six known alkaloids, stylopine (2), protopine (3), norchelidonine (4), chelidonine (5), berberine (6), and 8-hydroxydihydrosanguinarine (7), were isolated from Chelidonium majus. Their chemical structures were primarily established using 1D and 2D NMR techniques and mass spectrometry. The anti-inflammatory activity of the isolates was examined for their inhibitory effects on LPS-induced NO production in macrophage RAW264.7 cells. Among them, compounds 5 and 7 showed strong inhibitory activities toward the LPS-induced NO production in macrophage RAW264.7 cells with IC(50) values of 7.3 and 4.5 µM, respectively. In addition, compounds 5 and 7 inhibited the inductions of COX-2 and iNOS mRNA in dose-dependent manners, indicating that these compounds attenuated the syntheses of these transcripts at the transcriptional level.


Assuntos
Alcaloides/química , Alcaloides/farmacologia , Benzofenantridinas/síntese química , Chelidonium/química , Isoquinolinas/síntese química , Lipopolissacarídeos , Macrófagos/efeitos dos fármacos , Óxido Nítrico/metabolismo , Animais , Benzofenantridinas/química , Benzofenantridinas/farmacologia , Linhagem Celular , Ciclo-Oxigenase 2/metabolismo , Concentração Inibidora 50 , Isoquinolinas/química , Isoquinolinas/farmacologia , Lipopolissacarídeos/farmacologia , Macrófagos/metabolismo , Camundongos , Estrutura Molecular , Óxido Nítrico/antagonistas & inibidores , Extratos Vegetais/farmacologia
15.
Bioorg Med Chem Lett ; 21(22): 6884-7, 2011 Nov 15.
Artigo em Inglês | MEDLINE | ID: mdl-21978676

RESUMO

Three new phenolics: ((7S)-8'-(benzo[3',4']dioxol-1'-yl)-7-hydroxypropyl)benzene-2,4-diol (1), ((7S)-8'-(4'-hydroxy-3'-methoxyphenyl)-7-hydroxypropyl)benzene-2,4-diol (2) and ((8R,8'S)-7-(4-hydroxy-3-methoxyphenyl)-8'-methylbutan-8-yl)-3'-methoxybenzene-4',5'-diol (3), along with four known compounds (4-7) were isolated from the seeds of Myristica fragrans. Their chemical structures were established mainly by 1D and 2D NMR techniques and mass spectrometry. Their anti-inflammatory activity was evaluated against LPS-induced NO production in macrophage RAW264.7 cells.


Assuntos
Anti-Inflamatórios/química , Anti-Inflamatórios/farmacologia , Myristica/química , Óxido Nítrico/antagonistas & inibidores , Fenóis/química , Fenóis/farmacologia , Animais , Anti-Inflamatórios/isolamento & purificação , Linhagem Celular , Macrófagos/efeitos dos fármacos , Macrófagos/imunologia , Espectroscopia de Ressonância Magnética , Camundongos , Óxido Nítrico/imunologia , Fenóis/isolamento & purificação , Sementes/química
16.
Planta Med ; 77(1): 66-9, 2011 Jan.
Artigo em Inglês | MEDLINE | ID: mdl-20645248

RESUMO

Two new lignans, (2 R,3 R)-2 ß-(4''-hydroxy-3''-methoxybenzyl)-3 α-(4'-hydroxy-3'-methoxybenzyl)-γ-butyrolactone 2-O-( ß-D-glucopyranoside) (1) and (1 S,2 R,3 S)-dimethyl-1,2,3,4-tetrahydro-3,6,7-trihydroxy-1-(3',4'-dihydroxyphenyl)naphthalene-2,3-dicarboxylate (2) together with nine known compounds (3-11) were isolated from the ethyl acetate fraction of the roots of Pulsatilla koreana. Their chemical structures were established based on physicochemical and spectroscopic data analyses. All isolates were investigated for their inhibition effects against the classical pathway of the complement system. Among them, compound 6 showed significant inhibitory activity with an IC (50) value of 75.9 µM, compounds 8 and 9 had moderate effects with IC (50) values of 182.2 and 166.5 µM, respectively.


Assuntos
Lignanas/farmacologia , Pulsatilla/química , Fracionamento Químico , Proteínas do Sistema Complemento/química , Lignanas/química , Lignanas/isolamento & purificação , Extratos Vegetais/química , Raízes de Plantas/química
17.
Phytother Res ; 25(4): 611-4, 2011 Apr.
Artigo em Inglês | MEDLINE | ID: mdl-20981867

RESUMO

In the course of screening plants used in natural medicines as memory enhancers, a 70% ethanol extract of the aerial parts of Leonurus heterophyllus showed significant AChE inhibitory activity. Bioassay-guided fractionation and repeated column chromatography led to the isolation of a new labdane-type diterpenoids (1), named leoheteronin F, and six known compounds (2-7). The chemical structures of isolated compounds were elucidated based on extensive 1D and 2D NMR spectroscopic data. The isolates 1-7 were investigated in vitro for their anticholinesterase activity using mouse cortex AChE enzyme. Leoheteronin A (5) and leopersin G (7), which possess a 15,16-epoxy group at the side chain, were found to be potent in the inhibition of AChE.


Assuntos
Inibidores da Colinesterase/farmacologia , Diterpenos/farmacologia , Leonurus/química , Animais , Espectroscopia de Ressonância Magnética , Masculino , Ratos , Ratos Sprague-Dawley
18.
Phytother Res ; 25(11): 1579-85, 2011 Nov.
Artigo em Inglês | MEDLINE | ID: mdl-21394807

RESUMO

Ganoderma lucidum is known as a medicinal mushroom used in traditional medicine. In our study, the cytotoxic activities of 17 compounds (1-17) isolated from the fruiting bodies of G. lucidum were investigated. Among them, ergosta-7,22-diene-2ß,3α,9α-triol (EGDT) induced apoptosis in HL-60 human premyelocytic leukemia cells. EGDT activated the apoptotic process, including DNA fragmentation and caspase-3 activity. In immunoblotting analysis, treatment with EGDT resulted in the cleavage of procaspase-3 and poly(ADP-ribose) polymerase (PARP) into active forms. In the in vivo study, the administration (i.p.) of EGDT to Lewis lung carcinoma (LLC)-inoculated mice evidenced a significant inhibition of tumor growth. These results indicate that EGDT was one of the apoptotic constituents of G. lucidum, and might be an antitumor agent.


Assuntos
Antineoplásicos Fitogênicos/farmacologia , Apoptose/efeitos dos fármacos , Fitosteróis/farmacologia , Reishi/química , Animais , Carcinoma Pulmonar de Lewis/tratamento farmacológico , Caspase 3/metabolismo , Fragmentação do DNA , Feminino , Células HL-60/efeitos dos fármacos , Humanos , Camundongos
19.
Chem Pharm Bull (Tokyo) ; 59(1): 129-31, 2011.
Artigo em Inglês | MEDLINE | ID: mdl-21212562

RESUMO

Two new flavonoid glycosides, (1, 2), and eleven known compounds, (3-13), were isolated from from a 70% EtOH extract of the leaves of Chromolaena odorata (Asteraceae). Their structures were elucidated by 1D and 2D NMR spectroscopic interpretation as well as by chemical studies. The newly isolated compounds were tested in vitro for their cytotoxic activities against the LLC and HL-60 cancer cell lines. Compound 1 showed cytotoxicity against LLC and HL-60 cancer cell lines with IC(50) values of 28.2 and 11.6 µM, respectively. Compound 2 exhibited significant cytotoxic activity in the inhibition of HL-60 cancer cell lines with IC(50) value of 10.8 µM.


Assuntos
Antineoplásicos Fitogênicos/química , Chromolaena/química , Flavonoides/química , Glicosídeos/química , Antineoplásicos Fitogênicos/isolamento & purificação , Antineoplásicos Fitogênicos/toxicidade , Linhagem Celular Tumoral , Glicosídeos/isolamento & purificação , Glicosídeos/toxicidade , Humanos , Espectroscopia de Ressonância Magnética , Conformação Molecular , Folhas de Planta/química
20.
Ann Med Surg (Lond) ; 70: 102846, 2021 Oct.
Artigo em Inglês | MEDLINE | ID: mdl-34540223

RESUMO

INTRODUCTION AND IMPORTANCE: No case has been reported regarding esophago-gastrectomy due to caustic chemicals in the literature. CASE PRESENTATION: The first case was a 43-year-old woman with BMI 28.5. After one month of taking a weight loss drug called HERBAL, the patient experienced vomiting, and signs of progressive dysphagia, while being unable to eat any solid food. Endoscopy results revealed many scars causing the narrowing of the esophagus, starting from the upper third of the esophagus, 25cm from the dental arch. After 2 months, she lost 26kg (BMI 18.3). Endoscopic reexamination showed the esophagus's stricture, 25cm from the dental arch. X-ray also showed that the esophagus and stomach were completely narrow and atrophied. The second case was a 37-year-old woman who suffered from domestic violence and drunk about 50 ml of toilet detergents to commit suicide. After one month, the patient went through dysphagia and was unable to eat. Esophageal endoscopy showed that the esophagus was narrowed in the upper third part, 20cm from the dental arch, which led to the inaccessibility of the conventional insertion tube that required nasoscope instead. CLINICAL DISCUSSION: The results demonstrated many ulcer scars, retraction inside the esophagus and stomach, abnormally small volume of stomach, narrowing cardia, and pyloric stenosis. In both cases, thoracoscopic surgery was performed for esophago-gastrectomy, and the upper gastrointestinal tract was subsequently reconstructed using the ileum-right colon. CONCLUSIONS: The ileum-right colon segment is a part that can be used to reconstruct the upper gastrointestinal tract following esophago-gastrectomy.

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