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1.
Mol Biol Rep ; 49(4): 2695-2709, 2022 Apr.
Artigo em Inglês | MEDLINE | ID: mdl-35040004

RESUMO

BACKGROUND: Artemisinin (ART) is an anti-malaria natural compound with a moderate anticancer action. As a metabolite of ART, dihydroartemisinin (DHA) may have stronger anti-colorectal cancer (CRC) bioactivities. However, the effects of DHA and ART on CRC chemoprevention, including adaptive immune regulation, have not been systematically evaluated and compared. METHODS: Coupled with a newly-established HPLC analytical method, enteric microbiome biotransformation was conducted to identify if the DHA is a gut microbial metabolite of ART. The anti-CRC potential of these compounds was compared using two different human CRC cell lines for cell cycle arrest, apoptotic induction, and anti-inflammation activities. Naive CD4+ T cells were also obtained for testing the compounds on the differentiation of Treg, Th1 and Th17. RESULTS: Using compound extraction and analytical methods, we observed for the first time that ART completely converted into its metabolites by gut microbiome within 24 h, but no DHA was detected. Although ART did not obviously influence cancer cell growth in the concentration tested, DHA very significantly inhibited the cancer cell growth at relatively low concentrations. DHA included G2/M cell cycle arrest via upregulation of cyclin A and apoptosis. Both ART and DHA downregulated the pro-inflammatory cytokine expression. The DHA significantly promoted Treg cell proliferation, while both ART and DHA inhibited Th1 and Th17 cell differentiation. CONCLUSIONS: As a metabolite of ART, DHA possessed stronger anti-CRC activities. The DHA significantly inhibited cell growth via cell cycle arrest, apoptosis induction and anti-inflammation actions. The adaptive immune regulation is a related mechanism of actions for the observed effects.


Assuntos
Artemisininas , Neoplasias do Colo , Apoptose , Artemisininas/farmacologia , Quimioprevenção , Neoplasias do Colo/tratamento farmacológico , Neoplasias do Colo/prevenção & controle , Humanos
2.
Zhongguo Zhong Yao Za Zhi ; 46(18): 4849-4864, 2021 Sep.
Artigo em Zh | MEDLINE | ID: mdl-34581097

RESUMO

As a unicellular organism, Plasmodium displays a panoply of lipid metabolism pathways that are seldom found together in a unicellular organism. These pathways mostly involve the Plasmodium-encoded enzymatic machinery and meet the requirements of membrane synthesis during the rapid cell growth and division throughout the life cycle. Different lipids have varied synthesis and meta-bolism pathways. For example, the major phospholipids are synthesized via CDP-diacylglycerol-dependent pathway in prokaryotes and de novo pathway in eukaryotes, and fatty acids are synthesized mainly via type Ⅱ fatty acid synthesis pathway. The available studies have demonstrated the impacts of artemisinin and its derivatives, the front-line compounds against malaria, on the lipid metabolism of Plasmodium. Therefore, this article reviewed the known lipid metabolism pathways and the effects of artemisinin and its derivatives on these pathways, aiming to deepen the understanding of lipid synthesis and metabolism in Plasmodium and provide a theoretical basis for the research on the mechanisms and drug resistance of artemisinin and other anti-malarial drugs.


Assuntos
Antimaláricos , Artemisininas , Malária , Plasmodium , Antimaláricos/farmacologia , Artemisininas/farmacologia , Artemisininas/uso terapêutico , Humanos , Metabolismo dos Lipídeos , Malária/tratamento farmacológico
3.
Zhongguo Zhong Yao Za Zhi ; 43(20): 4019-4026, 2018 Oct.
Artigo em Zh | MEDLINE | ID: mdl-30486525

RESUMO

Ferroptosis is a new form of regulated cell death which is different from apoptosis, necrosis and autophagy, and results from iron-dependent lipidperoxide accumulation. Now, it is found that ferroptosis is involved in multiple physiological and pathological processes, such as cancer, arteriosclerosis, neurodegenerative diseases, diabetes, antiviral immune response, acute renal failure, hepatic and heart ischemia/reperfusion injury. On the one hand, it could be found the appropriate drugs to promote ferroptosis to clear cancer cells and virus infected cells, etc. On the other hand, we could inhibit ferroptosis to protect healthy cells. China has a wealth of traditional Chinese medicine resources. Chinese medicine contains a variety of active ingredients that regulate ferroptosis. Here, this paper reported the research of ferroptosis pathway, targets of its inducers and inhibitors that have been discovered, and the regulatory effects of the discovered Chinese herbs and its active ingredients on ferroptosis to help clinical and scientific research.


Assuntos
Apoptose , Medicamentos de Ervas Chinesas/farmacologia , Ferro , Materia Medica/farmacologia , China , Humanos
4.
Zhongguo Zhong Yao Za Zhi ; 43(18): 3771-3781, 2018 Sep.
Artigo em Zh | MEDLINE | ID: mdl-30384545

RESUMO

Heme is a key metabolic factor in all life. Malaria parasite has de novo heme-biosynthetic pathway, however the growth and development of parasite depend on the hemoglobin-derived heme metabolism process during the intraerythrocytic stages, such as the ingestion and degradation of hemoglobin in the food vacuole. The hemoglobin metabolism in the food vesicles mainly includes four aspects: hemoglobin transport and intake, hemoglobin enzymolysis to produce heme, heme polymerization into malarial pigment, and heme transport via the food vacuole. The potential mechanisms of antimalarial drugs,such as chloroquine, artemisinin and atovaquone may be related to this process. The main four aspects of this metabolic process, key metabolic enzymes, effects of antimalarial drugs on the process and their potential mechanism of action would be summarized in this paper, providing ideas for rational use and mechanism exploration of similar drugs.


Assuntos
Heme/metabolismo , Plasmodium/metabolismo , Antimaláricos/farmacologia , Artemisininas/farmacologia , Atovaquona/farmacologia , Cloroquina/farmacologia , Eritrócitos/parasitologia , Hemoglobinas/metabolismo , Humanos , Plasmodium/efeitos dos fármacos
5.
Zhongguo Zhong Yao Za Zhi ; 41(12): 2315-2320, 2016 Jun.
Artigo em Zh | MEDLINE | ID: mdl-28901079

RESUMO

The main objective of this research is to observe protective effects of three phenylallyl compounds(cinnamyl alcohol,cinnamaldehyde and cinnamic acid)from Guizhi decoction against ox-LDL-induced oxidative stress injury on human brain microvascular endothelial cells(HBMEC).In this study,the toxicity and optimal protective concentration of three phenylallyl compounds from Guizhi decoction were determined by MTT assay.The HBMEC were divided into control group(DMSO),model group(ox-LDL),tert-butylhydroquinone (t-BHQ) group,cinnamyl alcohol group, cinnamaldehyde group and cinnamic acid group.The model group were treated with ox-LDL (50 mg•L⁻¹)for 24 h,other groups were separately treated with t-BHQ, cinnamyl alcohol, cinnamaldehyde and cinnamic acid of 20 µmol•L⁻¹, and exposed to ox-LDL (50 mg•L⁻¹) for 24 h at the same time.The survival rate of HBMEC was detected by MTT assay,reactive oxygen species(ROS) production of injured cells were detected using laser scanning confocal microscope (LSCM),the content of SOD, MDA, eNOS and NO in HBMEC was determined by ELISA, and the expressions of Nrf2 mRNA were detected by quantitative Real-time PCR(qRT-PCR).The results shows that oxidative stress injury of HBMEC could be induced by ox-LDL, the three phenylallyl compounds from Guizhi decoction did not affect morphology and viability of normal HBMEC.Compared with model group, the three phenylallyl compounds from Guizhi decoction could improve the above oxidative stress status and up-regulate Nrf2 mRNA expressions in injured HBMEC(P<0.05, P<0.01) .These findings suggested that the three phenylallyl compounds from Guizhi decoction have certain protective effects against ox-LDL-induced oxidative stress injury on HBMEC(cinnamaldehyde> t-BHQ> cinnamic acid>cinnamyl alcohol),the protective mechanism maybe related to regulation of antioxidant enzymes gene expression in HBMEC by Nrf2.


Assuntos
Medicamentos de Ervas Chinesas/farmacologia , Células Endoteliais/efeitos dos fármacos , Lipoproteínas LDL/efeitos adversos , Estresse Oxidativo/efeitos dos fármacos , Encéfalo/citologia , Células Cultivadas , Humanos
6.
Yao Xue Xue Bao ; 50(7): 836-41, 2015 Jul.
Artigo em Zh | MEDLINE | ID: mdl-26552144

RESUMO

To further uncover the scientific significance and molecular mechanism of the Chinese herbs with pungent hot or warm natures, endogenous and exogenous expression systems were established by isolation of dorsal root ganglion (DRG) neurons and transfection of HEK293 cells with TRPV1 channel gene separately. On this basis, the regulation action of capsaicin, one main ingredient from chili pepper, on TRPV1 channel was further explored by using confocal microscope. Besides, the three-sites one-unit technique and method were constructed based on the brown adipose tissue (BAT), anal and tail skin temperatures. Then the effect of capsaicin on mouse energy metabolism was evaluated. Both endogenous and exogenous TRPV1 channel could be activated and this action could be specifically blocked by the TRPV1 channel inhibitor capsazepine. Simultaneously, the mice's core body temperature and BAT temperature fall down and then go up, accompanied by the increase of temperature of the mice's tail skin. Promotion of the energy metabolism by activation of TRPV1 channel might be the common way for the pungent-hot (warm) herbs to demonstrate their natures.


Assuntos
Capsaicina/análogos & derivados , Plantas Medicinais/química , Canais de Cátion TRPV/fisiologia , Termogênese , Tecido Adiposo Marrom/efeitos dos fármacos , Tecido Adiposo Marrom/fisiologia , Animais , Capsaicina/farmacologia , Metabolismo Energético , Gânglios Espinais/citologia , Células HEK293 , Humanos , Camundongos , Neurônios/efeitos dos fármacos , Neurônios/fisiologia , Temperatura
7.
Cancer Chemother Pharmacol ; 93(5): 411-425, 2024 May.
Artigo em Inglês | MEDLINE | ID: mdl-38191768

RESUMO

BACKGROUND: Artemisinin (ART) and its derivatives are important antimalaria agents and have received increased attention due to their broad biomedical effects, such as anticancer and anti-inflammation activities. Recently, ruthenium-derived complexes have attracted considerable attention as their anticancer potentials were observed in preclinical and clinical studies. METHODS: To explore an innovative approach in colorectal cancer (CRC) management, we synthesized ruthenium-dihydroartemisinin complex (D-Ru), a novel metal-based artemisinin derivative molecule, and investigated its anticancer, anti-inflammation, and adaptive immune regulatory properties. RESULTS: Compared with its parent compound, ART, D-Ru showed stronger antiproliferative effects on the human CRC cell lines HCT-116 and HT-29. The cancer cell inhibition of D-Ru comprised G1 cell cycle arrest via the downregulation of cyclin A and the induction of apoptosis. ART and D-Ru downregulated the expressions of pro-inflammatory cytokines IL-1ß, IL-6, and IL-8. Although ART and D-Ru did not suppress Treg cell differentiation, they significantly inhibited Th1 and Th17 cell differentiation. CONCLUSIONS: Our results demonstrated that D-Ru, a novel ruthenium complexation of ART, remarkably enhanced its parent compound's anticancer action, while the anti-inflammatory potential was not compromised. The molecular mechanisms of action of D-Ru include inhibition of cancer cell growth via cell cycle arrest, induction of apoptosis, and anti-inflammation via regulation of adaptive immunity.


Assuntos
Apoptose , Artemisininas , Neoplasias do Colo , Pontos de Checagem da Fase G1 do Ciclo Celular , Humanos , Artemisininas/farmacologia , Artemisininas/química , Apoptose/efeitos dos fármacos , Neoplasias do Colo/patologia , Neoplasias do Colo/tratamento farmacológico , Neoplasias do Colo/imunologia , Pontos de Checagem da Fase G1 do Ciclo Celular/efeitos dos fármacos , Proliferação de Células/efeitos dos fármacos , Imunidade Adaptativa/efeitos dos fármacos , Rutênio/química , Rutênio/farmacologia , Antineoplásicos/farmacologia , Antineoplásicos/química , Células HCT116 , Células HT29 , Animais , Citocinas/metabolismo , Complexos de Coordenação/farmacologia , Complexos de Coordenação/química , Camundongos
8.
J Asian Nat Prod Res ; 12(1): 76-87, 2010 Jan.
Artigo em Inglês | MEDLINE | ID: mdl-20390747

RESUMO

Cinnamaldehyde (1) is a pharmacologically active ingredient isolated from cassia twig (Ramulus Cinnamomi), which is commonly used in herbal remedies to treat fever-related diseases. Both TRPV1 and TRPM8 ion channel proteins are abundantly expressed in sensory neurons, and are assumed to act as a thermosensor, with the former mediating the feeling of warmth and the latter the feeling of cold in the body. Both of them have recently been reported to be involved in thermoregulation. The purpose of this paper is to further uncover the antipyretic mechanisms of 1 by investigating its effects on the mRNA expression levels and functions of both TRPV1 and TRPM8. The results showed that 1 could up-regulate the mRNA expression levels of TRPV1 at both 37 and 39 degrees C, and its calcium-mediating function was significantly increased at 39 degrees C, all of which could not be blocked by pretreatment of the neuronal cells with ruthenium red, a general transient receptor potential (TRP) blocker, indicating that the action of 1 was achieved through a non-TRPA1 channel pathway. In conclusion, the findings in our in vitro studies might account for part of the peripheral molecular mechanisms for the antipyretic action of 1.


Assuntos
Acroleína/análogos & derivados , Cassia/química , Canais Iônicos/metabolismo , Neurônios/metabolismo , Canais de Cátion TRPV/genética , Acroleína/química , Acroleína/isolamento & purificação , Acroleína/farmacologia , Animais , Animais Recém-Nascidos , Capsaicina/farmacologia , Caules de Planta/química , RNA Mensageiro/genética , RNA Mensageiro/metabolismo , Ratos , Ratos Sprague-Dawley , Canais de Cátion TRPM/metabolismo , Canais de Cátion TRPV/metabolismo
9.
Am J Chin Med ; 36(1): 159-69, 2008.
Artigo em Inglês | MEDLINE | ID: mdl-18306459

RESUMO

3-phenyl-propenal is one of the principle compounds isolated from Guizhi (Ramulus Cinnamomi), the principal drug in Guizhi-Tang (GZT), a famous traditional Chinese medical formula. The aim of the present study was to investigate the effects of 3-phenyl-propenal on the expression of toll-like receptor 3 (TLR3), TLR4 and the downstream signaling components on Raw264.7 murine microphages. Raw264.7 cells were cultured in RPMI-1640 medium containing LPS (lipopolysaccharide) or poly (I:C) in the presence or absence of 3-phenyl-propenal. After 24-hour incubation, the medium was collected and the amount of TNF-alpha and IFN-beta was measured by ELISA. mRNA expression of TLR3, TLR4, myeloid differentiation factor (MyD88), TRAF-6 (tumor necrosis factor receptor-associated), TRAM (toll-like receptor-associated molecule) and TRIF (TIR domain-containing adaptor inducing IFN-beta) were analyzed by real-time PCR with SYBR green dye. Protein expression of TLR3 and TLR4 was analyzed by Western blotting and that of MyD88 and TRAF-6 was analyzed by immunofluorescence assay. The results indicate that LPS increased the expression of TLR4, MyD88, TRAF-6, TRAM and TRIF, but had no influence on TLR3, while poly (I:C) up-regulated the expression of TLR3, MyD88, TRAM and TRIF. 3-phenyl-propenal significantly decreased the expression of LPS-induced TLR4, MyD88, TRAF-6, while possessing no effect on LPS-induced TRAM and TRIF expression in Raw264.7 cells. When cells were stimulated by poly (I:C), 3-phenyl-propenal significantly decreased TLR3 and MyD88 expression. In conclusion, 3-phenyl-propenal blocked the over-expression of TLR3, TLR4, their downstream signaling components MyD88 and TRAF-6, which indicate that it had an antagonistic effect on TLR3 and TLR4.


Assuntos
Acroleína/análogos & derivados , Macrófagos/fisiologia , Receptores Toll-Like/genética , Acroleína/farmacologia , Animais , Técnicas de Cultura de Células , Linhagem Celular , Interferon beta/metabolismo , Macrófagos/efeitos dos fármacos , Camundongos , Reação em Cadeia da Polimerase , Transdução de Sinais/efeitos dos fármacos , Transdução de Sinais/fisiologia , Receptor 3 Toll-Like/efeitos dos fármacos , Receptor 3 Toll-Like/genética , Receptor 4 Toll-Like/efeitos dos fármacos , Receptor 4 Toll-Like/genética , Fator de Necrose Tumoral alfa/metabolismo
10.
Yao Xue Xue Bao ; 42(7): 798-802, 2007 Jul.
Artigo em Zh | MEDLINE | ID: mdl-17882968

RESUMO

To observe the effects of phenylallyl compounds on prostaglandin E2 (PGE2) release in mouse cerebral microvascular endothelial cells (bEnd. 3) stimulated by IL-1beta, and to analyze their structure-activity relationship. Different concentrations of phenylallyl compounds were added separately, and the content of PGE2 induced by IL-1beta in the culture media was measured by ELISA assay. The 50% inhibitory concentration (IC50) of PGE2 was calculated. Studies showed that phenylallyl compounds could affect the PGE2 release differently in bEnd. 3 cells induced by IL-1beta. Close relationships were shown between the inhibitory activities and the location and number of the substituent groups. In conclusion, phenylallyl compounds exhibited inhibitory activities at different extent on PGE2 release in bEnd. 3 cells stimulated by IL-1beta and presented certain structure-activity relationship.


Assuntos
Encéfalo/irrigação sanguínea , Cinamatos/farmacologia , Dinoprostona/antagonistas & inibidores , Células Endoteliais/metabolismo , Interleucina-1beta/farmacologia , Acroleína/análogos & derivados , Acroleína/isolamento & purificação , Acroleína/farmacologia , Animais , Células Cultivadas , Cinamatos/isolamento & purificação , Dinoprostona/metabolismo , Medicamentos de Ervas Chinesas/química , Células Endoteliais/citologia , Concentração Inibidora 50 , Camundongos , Microvasos/citologia , Propanóis/isolamento & purificação , Propanóis/farmacologia , Relação Estrutura-Atividade
11.
Zhongguo Zhong Yao Za Zhi ; 32(4): 327-32, 2007 Feb.
Artigo em Zh | MEDLINE | ID: mdl-17455470

RESUMO

OBJECTIVE: To investigate the influences of Shensu Yin to RAW 264.7 on the expression of TLR3, TLR4 and the factors of the downstream in RAW 264. 7 cells. METHOD: RAW 264.7 cell line was stimulated with Lipopolysaccharide and POLY I: C, respectively, and treated with the drug serum of Shensuyin simultaneously. 24 hours later, collected the supernatant and measured the inflammatory factors TNF-alpha and IFN-beta, extracted mRNA and measured the expression of TLR3, TLR4 and other correlated indexes of the downstream, analyzed and evaluated Shensu Yin's substance basis of pharmacodynamic actions. RESULT: Shensu Yin drug serum depressed the expression of TLR4, MyD88, TRAF-6, TRAM and TRIF mRNA, as a result, it decreased the amount of TNF-alpha and IFN-beta. CONCLUSION: Depressing the expression of TLR3, MyD88, TRAM and TRIF mRNA may be the elementary basis of Shensu Yin to play heat-clearing and detoxicating effect.


Assuntos
Medicamentos de Ervas Chinesas/farmacologia , Macrófagos/efeitos dos fármacos , Transdução de Sinais/efeitos dos fármacos , Receptor 3 Toll-Like/genética , Proteínas Adaptadoras de Transporte Vesicular/genética , Animais , Linhagem Celular , Combinação de Medicamentos , Medicamentos de Ervas Chinesas/isolamento & purificação , Interferon beta/metabolismo , Lipopolissacarídeos/farmacologia , Macrófagos/citologia , Macrófagos/metabolismo , Masculino , Camundongos , Fator 88 de Diferenciação Mieloide/genética , Plantas Medicinais/química , Poli I-C/farmacologia , RNA Mensageiro/biossíntese , RNA Mensageiro/genética , Distribuição Aleatória , Ratos , Ratos Sprague-Dawley , Receptores de Interleucina/genética , Receptor 4 Toll-Like/genética , Fator de Necrose Tumoral alfa/metabolismo
12.
Eur J Pharmacol ; 537(1-3): 174-80, 2006 May 10.
Artigo em Inglês | MEDLINE | ID: mdl-16624280

RESUMO

Cinnamaldehyde is a principle compound isolated from Guizhi-Tang, which is a famous traditional Chinese medical formula used to treat influenza, common cold and other pyretic conditions. The aim of the present study was to investigate the effects of cinnamaldehyde on expression and activity of cyclooxygenase (COX) and prostaglandin E(2) (PGE(2)) in rat cerebral microvascular endothelial cells (RCMEC). RCMEC were cultured, and identified by immunohistochemistry for von Willebrand factor in cytoplasm of the cells. Then cells were incubated in M199 medium containing interleukin (IL)-1beta in the presence or absence of cinnamaldehyde. After incubation, the medium was collected and the amount of PGE(2) was measured by enzyme-linked immunosorbent assay (ELISA). The cells were harvested, mRNA expression and activity of COX were analyzed by real-time reverse transcription-polymerase chain reaction (RT-PCR) with SYBR Green dye and ELISA respectively. Positive immunostaining for von Willebrand factor was present diffusely in the cytoplasm of >95% RCMEC. IL-1beta increased the mRNA expression and activity of COX-2, and production of PGE(2) in a dose- and time-dependent manner in RCMEC, while mRNA and activity of COX-1 were not significantly altered. Cinnamaldehyde significantly decreased IL-1beta-induced COX-2 activity and PGE(2) production in a dose-dependent manner, while it showed no inhibitory effect on IL-1beta-induced COX-2 mRNA expression in cultured RCMEC. In conclusion, cinnamaldehyde reduces IL-1beta-induced COX-2 activity, but not IL-1beta-induced COX-2 mRNA expression, and consequently inhibits production of PGE(2) in cultured RCMEC.


Assuntos
Acroleína/análogos & derivados , Inibidores de Ciclo-Oxigenase 2/farmacologia , Dinoprostona/antagonistas & inibidores , Células Endoteliais/efeitos dos fármacos , Acroleína/farmacologia , Animais , Células Cultivadas , Córtex Cerebral/citologia , Córtex Cerebral/metabolismo , Ciclo-Oxigenase 1/genética , Ciclo-Oxigenase 1/metabolismo , Ciclo-Oxigenase 2/genética , Ciclo-Oxigenase 2/metabolismo , Dinoprostona/metabolismo , Medicamentos de Ervas Chinesas , Células Endoteliais/metabolismo , Febre/tratamento farmacológico , Regulação Enzimológica da Expressão Gênica/efeitos dos fármacos , Interleucina-1/farmacologia , RNA Mensageiro/metabolismo , Ratos
13.
Am J Chin Med ; 34(4): 685-93, 2006.
Artigo em Inglês | MEDLINE | ID: mdl-16883638

RESUMO

Fever, an elevation in body temperature, is thought to be terminally mediated by prostaglandin E(2) (PGE(2)). Both Guizhi Tang (GZT) and its active fraction A (Fr.A) showed an antipyretic effect in rats. 3-Phenyl-2-propene-1-ol was one of the active compounds isolated from Fr.A. In the present study, we examined the influence of interleukin-1beta (IL-1beta) on prostaglandin E(2) (PGE(2)) release, and the effect of 3-phenyl-2-propene-1-ol on IL-1beta-induced PGE(2) release from rat cerebral endothelial cells (rCMEC). Cultured rCMEC were used in the study. In vitro, cells express typical phenotypic markers of brain endothelium. Using a monoclonal antibody against von Willebrand factor, immunocytochemical analysis revealed positive immunoreactivity in the cytoplasm of cultured cells. rCMEC were incubated in M199 medium containing IL-1beta in the presence or absence of 3-phenyl-2-propene-1-ol. After incubation, the conditioned media were collected and the amount of PGE(2) was measured by enzyme-linked immunosorbent assay (ELISA). IL-1beta increased the production of PGE(2) in a dose- and time-dependent manner. 3-Phenyl-2-propene-1-ol significantly decreased IL-1beta-induced PGE(2) release in a dose-dependent manner. Our results indicate that 3-phenyl-2-propene-1-ol inhibits the PGE(2) release from rCMEC stimulated by IL-1beta, and may have an antipyretic effect.


Assuntos
Dinoprostona/metabolismo , Células Endoteliais/efeitos dos fármacos , Interleucina-1/farmacologia , Propanóis/farmacologia , Animais , Sobrevivência Celular/efeitos dos fármacos , Células Cultivadas , Córtex Cerebral/irrigação sanguínea , Cinnamomum/química , Dinoprostona/biossíntese , Relação Dose-Resposta a Droga , Células Endoteliais/citologia , Células Endoteliais/metabolismo , Propanóis/química , Ratos , Fatores de Tempo
14.
Zhongguo Zhong Yao Za Zhi ; 31(13): 1087-90, 2006 Jul.
Artigo em Zh | MEDLINE | ID: mdl-17048610

RESUMO

OBJECTIVE: To observe the effect of 2-methoxycinnamaldehyde (isolated from fraction A of Guizhi Tang) on activity of COX and PGE2 release in rat cerebral microvascular endothelial cells (rCMEC) stimulated by IL-1. METHOD: rCMEC were cultured, and identified by immunohistochemistry for von Willebrand factor (VIII factor, a marker for all endothelial cells) in cytoplasm of the cells. Different concentrations of 2-methoxycinnamaldehyde were added respectively and incubated for 3 hours, then stimulated for another 12 hours by IL-1. Activities of COX-1 and COX-2 in rCMEC, and production of PGE2 in the conditioned media were measured by ELISA. RESULT: Positive immunostaining for VIII factor was present diffusely in the cytoplasm of > 90% rCMEC. After being exposed to 30 ng x mL(-1) IL, the activity of COX-2 in rCMEC and the production of PGE2 in conditioned media were higher than those of control group, while there was no difference on activity of COX-1 in the two groups. 2-methoxycinnamaldehyde could down-regulate them in concentration-dependently, and significant differences on the activity of COX-2 and amount of PGE2 were showed in 200 microg x mL(-1) concentration. CONCLUSION: 2-methoxycinnamaldehyde can affect the PGE2 release in rCMEC induced by IL-1, which might be related with its inhibition on the activity of COX-2.


Assuntos
Acroleína/análogos & derivados , Encéfalo/irrigação sanguínea , Ciclo-Oxigenase 2/metabolismo , Dinoprostona/metabolismo , Células Endoteliais/metabolismo , Acroleína/administração & dosagem , Acroleína/isolamento & purificação , Acroleína/farmacologia , Animais , Células Cultivadas , Ciclo-Oxigenase 1/metabolismo , Relação Dose-Resposta a Droga , Combinação de Medicamentos , Medicamentos de Ervas Chinesas/química , Medicamentos de Ervas Chinesas/isolamento & purificação , Células Endoteliais/citologia , Interleucina-1/antagonistas & inibidores , Masculino , Microcirculação/citologia , Plantas Medicinais/química , Ratos , Ratos Sprague-Dawley
15.
J Ethnopharmacol ; 189: 361-85, 2016 Aug 02.
Artigo em Inglês | MEDLINE | ID: mdl-27377337

RESUMO

ETHNOPHARMACOLOGICAL RELEVANCE: Gastrodia elata Blume (Orchidaceae) is commonly called Tian ma in Chinese and mainly distributed in the mountainous areas of eastern Asia, such as China, Korea, Japan and India. It is an extensively used traditional Chinese herbal medicine in the clinical practice of traditional Chinese medicine, to treat headache, migraine, dizziness, epilepsy, infantile convulsion, tetany and so on. The present paper reviews the advancements in investigation of botany and ethnopharmacology, phytochemistry, pharmacology, toxicology and quality control of Gastrodia elata Blume. Finally, the possible tendency and perspective for future investigation of this plant are also put forward. MATERIALS AND METHODS: The information on Gastrodia elata Blume was collected via piles of resources including classic books about Chinese herbal medicine, and scientific databases including Pubmed, Google Scholar, ACS, Web of science, ScienceDirect databases, CNKI and others. Plant taxonomy was validated by the databases "The Plant List", and "Mansfeld's Encyclopedia". RESULTS: Over 81 compounds from this plant have been isolated and identified, phenolics and polysaccharides are generally considered as the characteristic and active constituents of Gastrodia elata Blume. Its active compounds possess wide-reaching biological activities, including sedative, hypnotic, antiepileptic, anticonvulsive, antianxietic, antidepressant, neuroprotective, antipsychotic, anti-vertigo, circulatory system modulating, anti-inflammationary, analgesic, antioxidative, memory-improving and antiaging, antivirus and antitumor effects. CONCLUSION: Despite the publication of various papers on Gastrodia elata Blume, there is still, however, the need for definitive research and clarification of other bioactive compounds using bioactivity-guided isolation strategies, and the possible mechanism of action as well as potential synergistic or antagonistic effects of multi-component mixtures derived from Gastrodia elata Blume need to be evaluated. It is also necessary and important to do more quality control and toxicological study on human subjects in order to maintain its efficacy stable in the body and validate its safety in clinical uses. In addition, more investigations on other parts of this plant beyond the tubers are needed. Further studies on Gastrodia elata Blume will lead to the development of new drugs and therapeutics for various diseases, and how to utilize it better should be paid more attention to.


Assuntos
Etnofarmacologia , Gastrodia/química , Compostos Fitoquímicos/farmacologia , Extratos Vegetais/farmacologia , Rizoma/química , Animais , Modelos Animais de Doenças , Etnobotânica , Humanos , Medicina Tradicional , Compostos Fitoquímicos/isolamento & purificação , Compostos Fitoquímicos/uso terapêutico , Compostos Fitoquímicos/toxicidade , Fitoterapia , Extratos Vegetais/isolamento & purificação , Extratos Vegetais/uso terapêutico , Extratos Vegetais/toxicidade , Plantas Medicinais , Medição de Risco , Testes de Toxicidade
16.
Am J Chin Med ; 44(7): 1363-1378, 2016.
Artigo em Inglês | MEDLINE | ID: mdl-27785943

RESUMO

Shaoyao-Gancao Tang (SGT) is one of the most frequently used compound formulas in the treatment of pain-related diseases in the medical practice of traditional Chinese medicine (TCM). To investigate the anti-inflammatory and antinociceptive effects, as well as to uncover the molecular mechanism of SGT, the rat pain model of arthritis was experimentally induced by single unilateral injection of rats' left hind paw with Freund's complete adjuvant (FCA). SGT was orally administered to the rats daily at three doses individually for a period of 16 days post-model induction. Swollen degrees and pain thresholds of the rats in different groups were measured for evaluation of the anti-inflammatory and anti-nociceptive effects of SGT. Furthermore, the mRNA and protein expression levels of transient receptor potential ion channel protein vanilloid receptor 1 (TRPV1) channel as well as its calcium-mediating function in the isolated DRG neurons were further detected to provide indexes for exploration of the molecular mechanisms mediating anti-arthritic activities of SGT. As a result, FCA injection induced significant allodynia, inflammation and edema, accompanied by a significant increase in both expression and calcium-mediating function of the TRPV1 channel. Pharmacologically, oral administration of SGT at a high or middle dose demonstrated a significant relief from the above-mentioned pathological conditions in a dose-dependent manner. Simultaneously the mRNA and protein expressional levels of TRPV1 channel, as well as its calcium-mediating function, were down-regulated greatly. These findings suggest that SGT possesses a significant analgesic and anti-inflammatory effect on arthritis rats; its therapeutic activities might be achieved through reversing the elevated expression and function of TRPV1 channel evoked by FCA.


Assuntos
Artrite Experimental/complicações , Regulação para Baixo/efeitos dos fármacos , Medicamentos de Ervas Chinesas/farmacologia , Dor/tratamento farmacológico , Dor/etiologia , Canais de Cátion TRPV/genética , Canais de Cátion TRPV/metabolismo , Administração Oral , Analgésicos/administração & dosagem , Analgésicos/farmacologia , Animais , Anti-Inflamatórios/administração & dosagem , Anti-Inflamatórios/farmacologia , Artrite Experimental/imunologia , Cálcio/metabolismo , Modelos Animais de Doenças , Relação Dose-Resposta a Droga , Medicamentos de Ervas Chinesas/administração & dosagem , Adjuvante de Freund/imunologia , Expressão Gênica/efeitos dos fármacos , Masculino , Fitoterapia , RNA Mensageiro/metabolismo , Ratos Sprague-Dawley
17.
Zhongguo Zhong Yao Za Zhi ; 28(11): 1056-60, 2003 Nov.
Artigo em Zh | MEDLINE | ID: mdl-15615417

RESUMO

OBJECTIVE: To investigate the effect of Guizhi Tang and its active components on the fever induced by EP3 receptor agonist sulprostone in rats. METHOD: The rise in body temperature evoked by a LCV(lateral cerebroventricle)-injection of sulprostone was compared with that of sulprostone induced-fever rats pretreated with Guizgi Tang and its active compounds, cinnamaldehyde, cinnamic acid and total glucosides of paeony. RESULT: Pretreatments with Guizhi Tang and cinnamaldehyde inhibited the rise in body temperature induced by sulprostone, while cinnamic acid tended to augment the fever. The sulprostone-induced fever was blocked by an ip pretreatment of total glucosides of paeony even below the basement. CONCLUSION: Present data suggest that interruption with the down-stream events of EP3 receptor may contribute to the antipyretic action of Guizhi Tang, cinnamaldehyde and the total glucosides of paeony, while cinnamic acid may have no such effect.


Assuntos
Acroleína/análogos & derivados , Analgésicos não Narcóticos/farmacologia , Medicamentos de Ervas Chinesas/farmacologia , Febre/fisiopatologia , Glucosídeos/farmacologia , Acroleína/isolamento & purificação , Acroleína/farmacologia , Analgésicos não Narcóticos/isolamento & purificação , Animais , Temperatura Corporal/efeitos dos fármacos , Cinamatos/isolamento & purificação , Cinamatos/farmacologia , Dinoprostona/análogos & derivados , Combinação de Medicamentos , Medicamentos de Ervas Chinesas/isolamento & purificação , Febre/induzido quimicamente , Glucosídeos/isolamento & purificação , Masculino , Paeonia/química , Plantas Medicinais/química , Ratos , Ratos Wistar , Receptores de Prostaglandina E/agonistas , Receptores de Prostaglandina E Subtipo EP3
18.
Chin J Nat Med ; 12(2): 89-102, 2014 Feb.
Artigo em Inglês | MEDLINE | ID: mdl-24636058

RESUMO

Siraitia grosvenorii is a perennial herb endemic to Guangxi province of China. Its fruit, commonly known as Luo hanguo, and has been used for hundreds of years as a natural sweetener and as a traditional medicine for the treatment of pharyngitis, pharyngeal pain, as well as an anti-tussive remedy in China. Based on ninety-three literary sources, this review summarized the advances in chemistry, biological effects, and toxicity research of S. grosvenorii during the past 30 years. Several different classes of compounds have been isolated or detected from various parts of S. grosvenorii, mainly triterpenoids, flavonoids, polysaccharides, amino acids, and essential oils. Various types of extracts or individual compounds derived from this species exhibited a wide array of biological effects e.g. anti-tussive, phlegm-relieving, anti-oxidant, immunomodulatory, liver-protecting, glucose-lowering, and anti-microbial. The existing research has shown that extracts and individual compounds from S. grosvenorii are basically non-toxic. Finally, some suggestions for further research on specific chemical and pharmacological properties of S. grosvenorii are proposed in this review.


Assuntos
Cucurbitaceae/química , Extratos Vegetais/farmacologia , Aminoácidos , Animais , Flavonoides , Humanos , Polissacarídeos , Triterpenos
19.
Chin J Integr Med ; 19(11): 826-35, 2013 Nov.
Artigo em Inglês | MEDLINE | ID: mdl-23754163

RESUMO

OBJECTIVE: To explore the pathological mechanisms of Guizhi Decoction () syndrome and the therapeutic molecular mechanisms of the Guizhi Decoction, Mahuang Decoction (), Sangju Decoction ( ) and Yinqiao Powder (), as well as the potentially biological basis that Guizhi Decoction is most effective only for the patients with Guizhi Decoction syndrome in clinical practice. METHODS: We first got serum samples from the patients suffering from both upper respiratory tract infection and Guizhi Decoction syndrome identified by the doctors of Chinese medicine (CM) in the clinic. Four formulas with therapeutic actions of pungent warmth or pungent coolness for superficial syndromes were chosen and four kinds of rat serum samples each containing one of the above-mentioned herbal formulas were collected, then the effects of Guizhi Decoction syndromes' patient serum as well as the effects of sera containing the formulas after being stimulated by the patient serum samples on both the mRNA expression of certain toll-like receptor (TLR) subtypes and the release of some inflammatory cytokines in RAW264.7 cells were tested and analyzed in vitro. RESULTS: The expression of TLR-3, TLR-4 and TLR-9 mRNA among the 9 tested TLR subforms were up-regulated in the macrophages stimulated by the sera from untreated upper respiratory infection patients with the Guizhi Decoction syndrome (symptomcomplex). The products such as interleukin (IL)-1ß, IL-6, tumor necrosis factor (TNF)-α and interferon (IFN)-ß from stimulated macrophages through TLR signaling pathways were also increased correspondingly. Interestingly, the changes induced by the Guizhi Decoction syndrome patients' sera were masked significantly after the macrophages were incubated with the sera from donors treated with Guizhi Decoction. Similarly, the three other exterior-releasing formulas were all effective in reversing the up-regulated changes of certain TLR subforms to different degrees, but both the number of targeted TLRs and efficacy of them seemed to be inferior to that of Guizhi Decoction. CONCLUSION: Evidence from these experiments might contribute to the scientific explanation of both the pharmacological mechanisms of Guizhi Decoction and also the CM theory that Guizhi Decoction is specifically prescribed for the treatment of Guizhi Decoction syndrome (The gearing formula to the symptom-complex).


Assuntos
Citocinas/metabolismo , Medicamentos de Ervas Chinesas/farmacologia , Regulação da Expressão Gênica/efeitos dos fármacos , Receptores Toll-Like/genética , Animais , Sobrevivência Celular/efeitos dos fármacos , Sobrevivência Celular/genética , Feminino , Voluntários Saudáveis , Humanos , Mediadores da Inflamação/metabolismo , Concentração Inibidora 50 , Macrófagos/efeitos dos fármacos , Macrófagos/metabolismo , Masculino , Camundongos , Pessoa de Meia-Idade , RNA Mensageiro/genética , RNA Mensageiro/metabolismo , Ratos , Ratos Sprague-Dawley , Síndrome , Receptores Toll-Like/metabolismo
20.
J Ethnopharmacol ; 129(3): 361-6, 2010 Jun 16.
Artigo em Inglês | MEDLINE | ID: mdl-20380875

RESUMO

ETHNOPHARMACOLOGICAL RELEVANCE: Scutellaria baicalensis Georgi (Lamiaceae) is often included as an ingredient in traditional Chinese compound prescriptions for the treatment of fever-related or inflammatory conditions. AIM OF THE STUDY: The present work was to further uncover the analgesic mechanisms of baicalin (a known principal constituent of Scutellaria baicalensis) by investigating its effects on the expression of TRPV1 mRNA as well as on its functions as mediators of calcium entrance into the cytoplasm of dorsal root ganglion (DRG) neurons in vitro. MATERIALS AND METHODS: By using CPT as an agent to eliminate the non-neuronal cells and using serum-free neurobasal as culture medium, primary cultures of rat DRG neurons with high purity and viability were established. On this basis, effects of baicalin on both the expression of TRPV1 mRNA and on the function of TRPV1 in vitro under two various temperature conditions were studied. The TRPV1 mRNA expression levels were examined by using qRT-PCR and analyzed by the method of 2(-DeltaDeltaCT). The elevation amplitudes of intracellular [Ca(2+)]i evoked by TRPV1 agonist capsaicin in DRG neurons were examined by the calcium fluorescence imaging method under confocal microscopy. RESULTS: Baicalin was shown to down-regulate the mRNA expression levels of TRPV1 at both 37 and 39 degrees C, and under the latter temperature, the intracellular fluorescent intensity evoked by capsaicin was significantly decreased following incubation with baicalin in vitro. We also demonstrated that the actions of baicalin to TRPV1 were not achieved through pathways of TRPA1 or TRPV subfamily members. CONCLUSIONS: Collectively, these results provide compelling evidence that the down-regulated actions of baicalin to TRPV1 in DRG neurons might account for part of the anti-nociceptive mechanism of baicalin.


Assuntos
Anti-Inflamatórios não Esteroides/farmacologia , Flavonoides/farmacologia , Gânglios Espinais/efeitos dos fármacos , Neurônios/efeitos dos fármacos , Canais de Cátion TRPV/biossíntese , Animais , Animais Recém-Nascidos , Anti-Inflamatórios não Esteroides/isolamento & purificação , Cálcio/metabolismo , Capsaicina/farmacologia , Técnicas de Cultura de Células , Sobrevivência Celular/efeitos dos fármacos , Células Cultivadas , Meios de Cultura Livres de Soro , Regulação para Baixo , Flavonoides/isolamento & purificação , Gânglios Espinais/citologia , Gânglios Espinais/metabolismo , Microscopia Confocal , Estrutura Molecular , Neurônios/metabolismo , Ratos , Ratos Sprague-Dawley , Reação em Cadeia da Polimerase Via Transcriptase Reversa , Scutellaria baicalensis/química , Canais de Cátion TRPV/agonistas , Canais de Cátion TRPV/antagonistas & inibidores
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