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1.
Zhen Ci Yan Jiu ; 48(5): 508-14, 2023 May 25.
Artigo em Chinês | MEDLINE | ID: mdl-37247866

RESUMO

OBJECTIVE: To analyze the optimum stimulating parameters and acupoint combination law of electroacupuncture (EA) treatment of post-stroke sequelae (PSS) through the network visual data mining and analysis of the literature,so as to provide reference for clinical application. METHODS: The related articles of acupuncture treatment of PSS patients published from January 1, 2005 to December 31, 2021 were collected from databases of CNKI, Wanfang, Weipu(VIP), SinoMed, CHAOXING, DUXIU, PubMed, Ovid, Embase and Cochrane Library. After the articles were screened according to our formulated inclusion and exclusion criteria, a "Clinical Literature Database of EA Treatment of PSS" was established. The SPSS Modeler14.1 software was used for modeling (by using the parameters of EA, types of apoplexy sequelae, names of acupoints, methods of acupoint matching, acupoint-attributed meridians, etc.) and association rule analysis, and the Cytoscape 3.6.0 software was used for data network visualization analysis. RESULTS: A total of 354 articles were collected, including 13 types of PSS, among which the hemi-plegia accounts for the highest proportion (51.13%), followed by depression (17.51%) and dysphagia (14.97%). A total of 228 acupoints are used, with a total frequency-time of 1 690. Among the 8 PSS (hemiplegia, depression, dysphagia, cognitive impairment, urinary incontinence, urinary retention, speech disorders, constipation) with the frequency of application of acupoints greater than or equal to 3, 275 articles are involved, with the frequency of dense wave being the highest (123 times), followed by continuous waves (95 times). The stimulation frequency of EA appears 275 times, with the low frequency being the highest (188 times). For hemiplegia type of PSS, low frequency and continuous waves or dense waves are mostly used, and the high correlation acupoint groups are Zusanli(ST36)/Hegu(LI4), LI4/Quchi(LI11) and ST36/LI11. For depression, low frequency and dense waves are mostly used, and the high correlation acupoint groups are Baihui(GV20)/Yintang(EX-HN3), GV20/Shenting(GV24) and GV20/Neiguan(PC6). For swallowing disorder, the mostly used stimulation parameter is low frequency, and the high correlation acupoint groups are Lianquan(CV23)/ST36/Fenglong(ST40), Tongli(HT5)/Yifeng(TE17)/PC6/ST40, and TE17/HT5/PC6/LI4. CONCLUSION: EA therapy is frequently used in the treatment of PSS, for which ST36, LI4 and LI11 are most frequently used in the treatment of hemiplegia, with the stimulation parameters being low-frequency and continuous waves or dense waves. For depression, GV20, EX-HN3, GV24 and PC6 are used, with the stimulation parameters being low frequency and dense waves. For dysphagia, CV23, HT5, TE17, PC6, ST36, ST40 and LI4 are employed, with low frequency electrical stimulation.


Assuntos
Terapia por Acupuntura , Transtornos de Deglutição , Eletroacupuntura , Meridianos , Acidente Vascular Cerebral , Humanos , Pontos de Acupuntura , Mineração de Dados , Hemiplegia , Acidente Vascular Cerebral/complicações , Acidente Vascular Cerebral/terapia
2.
Bioorg Chem ; 133: 106382, 2023 04.
Artigo em Inglês | MEDLINE | ID: mdl-36716580

RESUMO

Acute pancreatitis (AP) is a frequent abdominal inflammatory disease. Despite the high morbidity and mortality, the management of AP remains unsatisfactory. Disulfiram (DSF) is an FDA-proved drug with potential therapeutic effects on inflammatory diseases. In this study, we aim to investigate the effect of DSF on pancreatic acinar cell necrosis, and to explore the underlying mechanisms. Cell necrosis was induced by sodium taurocholate or caerulein, AP mice model was induced by nine hourly injections of caerulein. Network pharmacology, molecular docking, and molecular dynamics simulation were used to explore the potential targets of DSF in protecting against cell necrosis. The results indicated that DSF significantly inhibited acinar cell necrosis as evidenced by a decreased ratio of necrotic cells in the pancreas. Network pharmacology, molecular docking, and molecular dynamics simulation identified RIPK1 as a potent target of DSF in protecting against acinar cell necrosis. qRT-PCR analysis revealed that DSF decreased the mRNA levels of RIPK1 in freshly isolated pancreatic acinar cells and the pancreas of AP mice. Western blot showed that DSF treatment decreased the expressions of RIPK1 and MLKL proteins. Moreover, DSF inhibited NF-κB activation in acini. It also decreased the protein expression of TLR4 and the formation of neutrophils extracellular traps (NETs) induced by damage-associated molecular patterns released by necrotic acinar cells. Collectively, DSF could ameliorate the severity of mouse acute pancreatitis by inhibiting RIPK-dependent acinar cell necrosis and the following formation of NETs.


Assuntos
Pancreatite , Camundongos , Animais , Pancreatite/tratamento farmacológico , Pancreatite/induzido quimicamente , Células Acinares , Dissulfiram/efeitos adversos , Ceruletídeo/efeitos adversos , Doença Aguda , Simulação de Acoplamento Molecular , Necrose , Proteína Serina-Treonina Quinases de Interação com Receptores/farmacologia , Proteína Serina-Treonina Quinases de Interação com Receptores/uso terapêutico
3.
Zhongguo Zhong Yao Za Zhi ; 47(5): 1243-1252, 2022 Mar.
Artigo em Chinês | MEDLINE | ID: mdl-35343151

RESUMO

The present study investigated the effect of Euphorbiae Pekinensis Radix(EPR) on intestinal flora structure before and after vinegar processing and explored the detoxification mechanism of vinegar-processed EPR. In this study, the extraction efficiency of casbane diterpenes from EPR with different solvents was investigated, and the optimal solvent was selected to enrich these components. After 14 days of intragastric administration of total diterpene extract of EPR and vinegar-processed EPR, 16 S rDNA sequencing technology was used to detect the structural changes of intestinal flora. The flora related to the intestinal toxicity of EPR was screened out based on the results of intestinal pathological damage by correlation analysis. The results showed that Soxhlet extraction with chloroform as extraction solvent could enrich Casbane diterpenes in EPR. As revealed by 16 S rDNA sequencing results, EPR could significantly change the structure of intestinal flora, which could be reversed by vinegar-processing EPR. Some intestinal flora candidates might be related to detoxification of vinegar processing. The correlation analysis of intestinal flora candidates and indexes related to intestinal mucosal injury showed that compared with EPR, vinegar-processed EPR could down-regulate the abundance of some pathogenic bacteria such as Mucispirillum, Bilophila, and Ruminiclostridium, and up-regulated some probiotics such as Enterorhabdus, Ruminococcaceae_UCG-014, Barnesiella, and Candidatus. The intestinal toxicity caused by EPR may be related to the disturbance of intestinal flora, and vinegar-processed EPR can improve intestinal flora disorder by up-regulating the abundance of probiotics and down-regulating the abundance of pathogenic bacteria to remodel the intestinal mucosal barrier and reduce toxicity.


Assuntos
Medicamentos de Ervas Chinesas , Microbioma Gastrointestinal , Ácido Acético/química , Colo , Medicamentos de Ervas Chinesas/química , Raízes de Plantas
4.
Artigo em Chinês | WPRIM (Pacífico Ocidental) | ID: wpr-928049

RESUMO

The present study investigated the effect of Euphorbiae Pekinensis Radix(EPR) on intestinal flora structure before and after vinegar processing and explored the detoxification mechanism of vinegar-processed EPR. In this study, the extraction efficiency of casbane diterpenes from EPR with different solvents was investigated, and the optimal solvent was selected to enrich these components. After 14 days of intragastric administration of total diterpene extract of EPR and vinegar-processed EPR, 16 S rDNA sequencing technology was used to detect the structural changes of intestinal flora. The flora related to the intestinal toxicity of EPR was screened out based on the results of intestinal pathological damage by correlation analysis. The results showed that Soxhlet extraction with chloroform as extraction solvent could enrich Casbane diterpenes in EPR. As revealed by 16 S rDNA sequencing results, EPR could significantly change the structure of intestinal flora, which could be reversed by vinegar-processing EPR. Some intestinal flora candidates might be related to detoxification of vinegar processing. The correlation analysis of intestinal flora candidates and indexes related to intestinal mucosal injury showed that compared with EPR, vinegar-processed EPR could down-regulate the abundance of some pathogenic bacteria such as Mucispirillum, Bilophila, and Ruminiclostridium, and up-regulated some probiotics such as Enterorhabdus, Ruminococcaceae_UCG-014, Barnesiella, and Candidatus. The intestinal toxicity caused by EPR may be related to the disturbance of intestinal flora, and vinegar-processed EPR can improve intestinal flora disorder by up-regulating the abundance of probiotics and down-regulating the abundance of pathogenic bacteria to remodel the intestinal mucosal barrier and reduce toxicity.


Assuntos
Ácido Acético/química , Colo , Medicamentos de Ervas Chinesas/química , Microbioma Gastrointestinal , Raízes de Plantas
5.
Biochem Biophys Res Commun ; 527(2): 574-580, 2020 06 25.
Artigo em Inglês | MEDLINE | ID: mdl-32423805

RESUMO

Adipogenesis, a differentiation process that transitions preadipocytes to adipocytes, is key to understanding the biology of fat accumulation and obesity. During this process, there many crucial transcription factors, such as PPARγ and the C/EBP family. Here we show a transcription factor in preadipocytes --- Sox5, that has a function in porcine adipogenesis. In our porcine subcutaneous-derived preadipocyte differentiation model, we found Sox5 expression displayed a significant upregulation after initial induction and decreased afterwards, which resembles the PPARγ expression pattern. siRNA knockdown of Sox5 in porcine preadipocytes significantly promoted cell growth and accelerated cell cycle progression. After inducing differentiation, knockdown of Sox5 notably down-regulated the expression of adipogenic marker genes: PPARγ, aP2, FAS and impaired lipid accumulation. Mechanistically, the deletion of Sox5 down-regulated the BMP R-Smads signal pathway, a crucial signal pathway for controlling preadipocyte fate commitment and adipogenesis. After using BMP4 recombinant protein to activate the BMP R-Smads signal, Sox5 function was partially rescued. In conclusion, our findings uncovered a function of Sox5 in porcine adipogenesis and reveal an interaction between Sox5 and BMP signaling.


Assuntos
Adipogenia , Proteínas Morfogenéticas Ósseas/metabolismo , Fatores de Transcrição SOXD/genética , Transdução de Sinais , Proteínas Smad/metabolismo , Suínos/fisiologia , Animais , Proteínas Morfogenéticas Ósseas/genética , Células Cultivadas , Regulação para Baixo , Interferência de RNA , Fatores de Transcrição SOXD/metabolismo , Proteínas Smad/genética , Suínos/genética , Regulação para Cima
6.
Zhongguo Zhong Yao Za Zhi ; 43(12): 2516-2521, 2018 Jun.
Artigo em Chinês | MEDLINE | ID: mdl-29950069

RESUMO

To investigate the toxicity changes of Euphorbiae Ebracteolatae Radix (EER) before and after vinegar processing, toxic diterpenoids were concentrated with chloroform as extraction solvent from EER. Then the residue was extracted for non-chloroform extract with 95% ethanol and water after extraction with chloroform. The chloroform extraction of vinegar processed EER was prepared with the same method. The mice received the drug by oral administration. Moisture content in mice feces, duodenum and colon tissue, aquaporin AQP1, AQP3, AQP4 protein expression levels were assayed as the indexes to investigate the toxicity variation of chloroform fraction, non-chloroform fraction, as well as intestinal tract toxicity before and after vinegar processing of EER. The results showed that the chloroform fraction extracted from EER could significantly increase the moisture content in mice feces, duodenum and colon, and decrease AQP1 protein expression level, increase AQP3 and AQP4 protein expression levels in the colon. The intestinal toxicity of the chloroform extract was significantly higher than that of non-chloroform extract. The moisture content in mice feces, duodenum and colon was significantly decreased, and the AQPs protein expression tended to be normal in the colon after vinegar processing. The results showed that the chloroform fraction extracted from EER could lead to diarrhea, intestinal edema, and the intestinal toxicity action was associated with interfering AQPs protein expression and promoting intestinal fluid transport disorder in mice. Vinegar-processing could reduce intestinal toxicity of EER, so vinegar processing was considered to be the scientific processing method of EER.


Assuntos
Ácido Acético , Aquaporinas/metabolismo , Colo/efeitos dos fármacos , Diterpenos/toxicidade , Medicamentos de Ervas Chinesas/toxicidade , Euphorbia/toxicidade , Animais , Aquaporina 1 , Aquaporina 3 , Aquaporina 4 , Colo/metabolismo , Camundongos , Raízes de Plantas/toxicidade
7.
Zhongguo Zhong Yao Za Zhi ; 43(12): 2580-2585, 2018 Jun.
Artigo em Chinês | MEDLINE | ID: mdl-29950079

RESUMO

To establish the fingerprints of biles of pig, cattle and sheep, HPLC was used with Acclaim™ RSLC 120 C18 column (3.0 mm×100 mm, 2.2 µm, 120 Å), the column temperature 35 °C, acetonitrile-1% perchloric acid as mobile phase, gradient elution, 0.5 mL·min⁻¹ flow rate, and detection wavelength at 200 nm. The fingerprint was generated by using Similarity Evaluation Software of Chromatographic Fingerprint of Chinese Medicine (2004A Edition). The fingerprint peaks were identified by reference substances and verified by ELSD and LC-MS/MS. Then, the biles of pig, cattle and sheep were detected to contain 14, 9 and 8 common fingerprint peaks respectively, and the similarity was greater than 0.92. To analyze each technical parameter, GHDCA in pig bile and TCA in cattle and sheep bile were selected as reference peak. The precision, repeatability and stability all meet the requirements of fingerprint establishment. The RSD of the relative retention time of the fingerprint peaks was less than 1.5%, and the RSD of the relative peak area was less than 5%. The fingerprint peaks in pig bile were THDCA, TCDCA, GHDCA and GCDCA, and TCA, TCDCA, GCA, GCDCA and GDCA in cattle and sheep bile. The main components of pig, cattle and sheep bile were conjugated bile acids, but there were significant differences in bile acids between pig bile and cattle, sheep biles. The HPLC method established in this paper is simple, rapid and reproducible, and could be applied to the identification and quality control of biles.


Assuntos
Bile/química , Materia Medica/análise , Animais , Bovinos , Cromatografia Líquida de Alta Pressão , Controle de Qualidade , Ovinos , Suínos , Espectrometria de Massas em Tandem
8.
Artigo em Chinês | WPRIM (Pacífico Ocidental) | ID: wpr-687425

RESUMO

To investigate the toxicity changes of Euphorbiae Ebracteolatae Radix (EER) before and after vinegar processing, toxic diterpenoids were concentrated with chloroform as extraction solvent from EER. Then the residue was extracted for non-chloroform extract with 95% ethanol and water after extraction with chloroform. The chloroform extraction of vinegar processed EER was prepared with the same method. The mice received the drug by oral administration. Moisture content in mice feces, duodenum and colon tissue, aquaporin AQP1, AQP3, AQP4 protein expression levels were assayed as the indexes to investigate the toxicity variation of chloroform fraction, non-chloroform fraction, as well as intestinal tract toxicity before and after vinegar processing of EER. The results showed that the chloroform fraction extracted from EER could significantly increase the moisture content in mice feces, duodenum and colon, and decrease AQP1 protein expression level, increase AQP3 and AQP4 protein expression levels in the colon. The intestinal toxicity of the chloroform extract was significantly higher than that of non-chloroform extract. The moisture content in mice feces, duodenum and colon was significantly decreased, and the AQPs protein expression tended to be normal in the colon after vinegar processing. The results showed that the chloroform fraction extracted from EER could lead to diarrhea, intestinal edema, and the intestinal toxicity action was associated with interfering AQPs protein expression and promoting intestinal fluid transport disorder in mice. Vinegar-processing could reduce intestinal toxicity of EER, so vinegar processing was considered to be the scientific processing method of EER.

9.
Artigo em Chinês | WPRIM (Pacífico Ocidental) | ID: wpr-687415

RESUMO

To establish the fingerprints of biles of pig, cattle and sheep, HPLC was used with Acclaim™ RSLC 120 C₁₈ column (3.0 mm×100 mm, 2.2 μm, 120 Å), the column temperature 35 °C, acetonitrile-1% perchloric acid as mobile phase, gradient elution, 0.5 mL·min⁻¹ flow rate, and detection wavelength at 200 nm. The fingerprint was generated by using Similarity Evaluation Software of Chromatographic Fingerprint of Chinese Medicine (2004A Edition). The fingerprint peaks were identified by reference substances and verified by ELSD and LC-MS/MS. Then, the biles of pig, cattle and sheep were detected to contain 14, 9 and 8 common fingerprint peaks respectively, and the similarity was greater than 0.92. To analyze each technical parameter, GHDCA in pig bile and TCA in cattle and sheep bile were selected as reference peak. The precision, repeatability and stability all meet the requirements of fingerprint establishment. The RSD of the relative retention time of the fingerprint peaks was less than 1.5%, and the RSD of the relative peak area was less than 5%. The fingerprint peaks in pig bile were THDCA, TCDCA, GHDCA and GCDCA, and TCA, TCDCA, GCA, GCDCA and GDCA in cattle and sheep bile. The main components of pig, cattle and sheep bile were conjugated bile acids, but there were significant differences in bile acids between pig bile and cattle, sheep biles. The HPLC method established in this paper is simple, rapid and reproducible, and could be applied to the identification and quality control of biles.

10.
Zhongguo Zhong Yao Za Zhi ; 42(1): 125-129, 2017 Jan.
Artigo em Chinês | MEDLINE | ID: mdl-28945036

RESUMO

This study was to investigate the effect of vinegar processing on esculentosides in n-BuOH fraction and the contents of the main toxic components esculentoside B (EsB) and esculentoside C (EsC) in Phytolaccae Radix pieces. n-BuOH fraction of Phytolaccae Radix pieces was processed with vinegar according to the processing method in Chinese Pharmacopoeia. HPLC-MS-MS was adopted to analyze the esculentosides composition changes in n-BuOH fraction before and after vinegar processing. HPLC-ELSD was used to detect EsC and EsB contents in raw and vinegar processed Phytolaccae Radix pieces, and investigate the content changes before and after vinegar processing. Results showed that the esculentosides contents in n-BuOH fraction were significantly decreased except esculentoside A (EsA); there were significant changes in saponins compositions, but no new compounds were generated in n-BuOH fraction after vinegar processing. The contents of EsC and EsB were 0.12% and 0.20% respectively in raw Phytolaccae Radix, and decreased to 0.048% and 0.094% accordingly after vinegar processing. It showed that vinegar processing could significantly change the composition of esculentosides in n-BuOH fraction from Phytolaccae Radix and reduce the contents of toxic components EsC and EsB, indicating the scientificity of vinegar processing for Phytolaccae Radix.


Assuntos
Ácido Acético/química , Medicamentos de Ervas Chinesas/toxicidade , Ácido Oleanólico/análogos & derivados , Phytolaccaceae/química , Química Farmacêutica , Cromatografia Líquida de Alta Pressão
11.
Zhongguo Zhong Yao Za Zhi ; 42(24): 4722-4726, 2017 Dec.
Artigo em Chinês | MEDLINE | ID: mdl-29493137

RESUMO

To investigate the effects of ginkgolide A (GA), ginkgolide B (GB) and ginkgolide K (GK) on platelet aggregation in rabbits, and compare the similarities and differences among these three components. The effects of different doses of ginkgolide A, B and K on platelet aggregation induced by platelet activating factor (PAF) were observed by using in vitro experiment. The results showed that three compounds could inhibit platelet aggregation induced by PAF in vitro, and the intensity was GK> GB> GA. It was further found that all of them can mobilize [Ca2+]i and enhance intracellular c-AMP level in a dose-dependent manner, which was consistent to the ability to antagonize PAF receptor. These findings indicated that GK was highly selective for PAF receptor, and may inhibit platelet aggregation by activating cAMP signaling pathway and inhibiting intracellular [Ca2+]i mobilization; GB and GA also had strong antagonism to PAF receptor, but the effect was weaker than that of GK.


Assuntos
Ginkgolídeos/farmacologia , Lactonas/farmacologia , Agregação Plaquetária/efeitos dos fármacos , Animais , Cálcio/análise , AMP Cíclico/análise , Coelhos
12.
Zhongguo Zhong Yao Za Zhi ; 42(24): 4716-4721, 2017 Dec.
Artigo em Chinês | MEDLINE | ID: mdl-29493136

RESUMO

To study the antagonistic effect of ginkgolide homologues on platelet-activating factor (PAF)-induced platelet aggregation and investigate its neuroprotective effect. PAF was used as a coagulant, and ginkgolides were added to the rabbit blood samples respectively. The inhibitory effect of each compound on platelet aggregation was detected by turbidimetry. In L-glutamate induced primary cortical neuron cell injury model, MTT assay was used to detect cell viability. Intracellular free Ca2+ concentration in neurons was measured by using the fluorescent Ca2+ indicator Fura-2 AM. Morphological observation and Hoechst 33258 staining were used to detect the inhibitory effect of ginkgolide on neuronal apoptosis. The results showed that the inhibitory effect on PAF-induced platelet aggregation activity in ginkgolide homologues was ginkgolide K (GK), ginkgolide B (GB), ginkgolide A (GA), ginkgolide C (GC), ginkgolide M (GM), ginkgolide J (GJ) and ginkgolide (GL) from high to low. GB and GK (1-100 µmol•L ⁻¹) could significantly reduce the cell damage caused by L-glutamate, with survival rate increasing, intracellular calcium concentration reducing and cell morphology restoring. This paper has identified the activities and characteristics of various compounds of ginkgolide homologues on PAF-induced platelet aggregation as well as its neuroprotective effect.


Assuntos
Ginkgolídeos/farmacologia , Fármacos Neuroprotetores/farmacologia , Fator de Ativação de Plaquetas , Agregação Plaquetária/efeitos dos fármacos , Animais , Apoptose , Cálcio/análise , Células Cultivadas , Neurônios/efeitos dos fármacos , Coelhos
13.
Journal of Practical Radiology ; (12): 1209-1212, 2017.
Artigo em Chinês | WPRIM (Pacífico Ocidental) | ID: wpr-608947

RESUMO

Objective To evaluate the usefulness of diffusion-weighted imaging(DWI) in the diagnosis and differential diagnosis of gallbladder wall thickening diseases.Methods 42 patients with gallbladder wall thickening (16 patients with carcinoma and 26 patients with benign lesion) were included in this study.All patients performed conventional MRI and DWI.The diagnostic performances of three methods (conventional MRI,visual assessment of color fusion image from DWI and T2WI,and ADC measurement) were evaluated by two radiologists.Results The area under the receiver operating characteristic curve were 0.570,0.849,0.901 for conventional MRI,visual assessment and ADC measurement respectively.The accuracy,sensitivity and specificity were 59.5%,62.5%,57.7% for conventional MRI,85.7%,81.2%,88.5% for visual assessment of color fusion image,and 83.3%,80.0%,85.2% for ADC measurement,respectivily.The mean ADC value of gallbladder cacinoma[(1.15±0.35)×10-3mm2/s]was significantly less than that of gallbladder benign lesion [(1.99±0.61)×10-3mm2/s](P<0.01).Conclusion The DWI(visual assessment of color fusion image and ADC measurement)might be a useful tool for diagnosis and differential diagnosis of the gallbladder wall thickening diseases.

14.
Artigo em Chinês | WPRIM (Pacífico Ocidental) | ID: wpr-230983

RESUMO

This study was to investigate the effect of vinegar processing on esculentosides in n-BuOH fraction and the contents of the main toxic components esculentoside B (EsB) and esculentoside C (EsC) in Phytolaccae Radix pieces. n-BuOH fraction of Phytolaccae Radix pieces was processed with vinegar according to the processing method in Chinese Pharmacopoeia. HPLC-MS-MS was adopted to analyze the esculentosides composition changes in n-BuOH fraction before and after vinegar processing. HPLC-ELSD was used to detect EsC and EsB contents in raw and vinegar processed Phytolaccae Radix pieces, and investigate the content changes before and after vinegar processing. Results showed that the esculentosides contents in n-BuOH fraction were significantly decreased except esculentoside A (EsA); there were significant changes in saponins compositions, but no new compounds were generated in n-BuOH fraction after vinegar processing. The contents of EsC and EsB were 0.12% and 0.20% respectively in raw Phytolaccae Radix, and decreased to 0.048% and 0.094% accordingly after vinegar processing. It showed that vinegar processing could significantly change the composition of esculentosides in n-BuOH fraction from Phytolaccae Radix and reduce the contents of toxic components EsC and EsB, indicating the scientificity of vinegar processing for Phytolaccae Radix.

15.
Artigo em Chinês | WPRIM (Pacífico Ocidental) | ID: wpr-338213

RESUMO

To study the antagonistic effect of ginkgolide homologues on platelet-activating factor (PAF)-induced platelet aggregation and investigate its neuroprotective effect. PAF was used as a coagulant, and ginkgolides were added to the rabbit blood samples respectively. The inhibitory effect of each compound on platelet aggregation was detected by turbidimetry. In L-glutamate induced primary cortical neuron cell injury model, MTT assay was used to detect cell viability. Intracellular free Ca2+ concentration in neurons was measured by using the fluorescent Ca2+ indicator Fura-2 AM. Morphological observation and Hoechst 33258 staining were used to detect the inhibitory effect of ginkgolide on neuronal apoptosis. The results showed that the inhibitory effect on PAF-induced platelet aggregation activity in ginkgolide homologues was ginkgolide K (GK), ginkgolide B (GB), ginkgolide A (GA), ginkgolide C (GC), ginkgolide M (GM), ginkgolide J (GJ) and ginkgolide (GL) from high to low. GB and GK (1-100 μmol•L ⁻¹) could significantly reduce the cell damage caused by L-glutamate, with survival rate increasing, intracellular calcium concentration reducing and cell morphology restoring. This paper has identified the activities and characteristics of various compounds of ginkgolide homologues on PAF-induced platelet aggregation as well as its neuroprotective effect.

16.
Artigo em Chinês | WPRIM (Pacífico Ocidental) | ID: wpr-338212

RESUMO

To investigate the effects of ginkgolide A (GA), ginkgolide B (GB) and ginkgolide K (GK) on platelet aggregation in rabbits, and compare the similarities and differences among these three components. The effects of different doses of ginkgolide A, B and K on platelet aggregation induced by platelet activating factor (PAF) were observed by using in vitro experiment. The results showed that three compounds could inhibit platelet aggregation induced by PAF in vitro, and the intensity was GK> GB> GA. It was further found that all of them can mobilize [Ca2+]i and enhance intracellular c-AMP level in a dose-dependent manner, which was consistent to the ability to antagonize PAF receptor. These findings indicated that GK was highly selective for PAF receptor, and may inhibit platelet aggregation by activating cAMP signaling pathway and inhibiting intracellular [Ca2+]i mobilization; GB and GA also had strong antagonism to PAF receptor, but the effect was weaker than that of GK.

17.
Cancer Sci ; 107(10): 1506-1519, 2016 Oct.
Artigo em Inglês | MEDLINE | ID: mdl-27501331

RESUMO

Advanced lung cancer has poor prognosis owing to its low sensitivity to current chemotherapy agents. Therefore, discovery of new therapeutic agents is urgently needed. In this study, we investigated the antitumor effects of peperomin E, a secolignan isolated from Peperomia dindygulensis, a frequently used Chinese folk medicine for lung cancer treatment. The results indicate that peperomin E has antiproliferative effects, promoting apoptosis and cell cycle arrest in non-small-cell lung cancer (NSCLC) cell lines in a dose-dependent manner, while showing lower toxicity against normal human lung epidermal cells. Peperomin E inhibited tumor growth in A549 xenograft BALB/c nude mice without significant secondary adverse effects, indicating that it may be safely used to treat NSCLC. Furthermore, the mechanisms underlying the anticancer effects of peperomin E have been investigated. Using an in silico target fishing method, we observed that peperomin E directly interacts with the active domain of DNA methyltransferase 1 (DNMT1), potentially affecting its genome methylation activity. Subsequent experiments verified that peperomin E decreased DNMT1 activity and expression, thereby decreasing global methylation and reactivating the epigenetically silenced tumor suppressor genes including RASSF1A, APC, RUNX3, and p16INK4, which in turn activates their mediated pro-apoptotic and cell cycle regulatory signaling pathways in lung cancer cells. The observations herein report for the first time that peperomin E is a potential chemotherapeutic agent for NSCLC. The anticancer effects of peperomin E may be partly attributable to its ability to demethylate and reactivate methylation-silenced tumor suppressor genes through direct inhibition of the activity and expression of DNMT1.


Assuntos
Benzodioxóis/farmacologia , DNA (Citosina-5-)-Metiltransferases/antagonistas & inibidores , Inativação Gênica , Genes Supressores de Tumor , Neoplasias Pulmonares/genética , Ativação Transcricional/efeitos dos fármacos , Animais , Antineoplásicos/farmacologia , Apoptose/efeitos dos fármacos , Benzodioxóis/química , Linhagem Celular Tumoral , Sobrevivência Celular/efeitos dos fármacos , DNA (Citosina-5-)-Metiltransferases/química , DNA (Citosina-5-)-Metiltransferases/metabolismo , Metilação de DNA , Modelos Animais de Doenças , Pontos de Checagem da Fase G1 do Ciclo Celular/efeitos dos fármacos , Humanos , Neoplasias Pulmonares/metabolismo , Camundongos , Modelos Moleculares , Conformação Molecular , Ligação Proteica , Relação Estrutura-Atividade
18.
Zhongguo Zhong Yao Za Zhi ; 41(14): 2571-2575, 2016 Jul.
Artigo em Chinês | MEDLINE | ID: mdl-28905588

RESUMO

In order to compare the effect of sulfur fumigation processing and direct hot air heating technology on puerarin contents and efficacy of Puerariae Thomsonii Radix, the fresh roots of Pueraria thomsonii were cut into small pieces and prepared into direct sunshine drying samples, direct hot air drying samples, and sulfur fumigation-hot air drying samples. Moisture contents of the samples were then determined. The puerarin contents of different samples were compared by HPLC method. Moreover, the models of drunkenness mice were established, and then with superoxide dismutase (SOD) content as the index, aqueous decoction extracts of Puerariae Thomsonii Radix samples with sulfur fumigation processing and non-sulfur fumigation processing methods were administrated by ig; the effects of sulfur fumigation on contents of SOD in mice liver and serum were determined, and the sulfur fumigation samples and non-sulfur fumigation samples were investigated for moth and mildew under different packaging and storage conditions. Results showed that the sulfur fumigation samples significantly changed the puerarin content from Puerariae Thomsonii Radix. The content of puerarin was decreased gradually when increasing the times of sulfur fumigation and amount of sulfur. SOD content in drunken mice liver and serum was significantly decreased when increasing the times of sulfur fumigation, showing significant difference with both direct sunshine drying group and direct hot air drying group. Moth and mildew were not found in the sulfur fumigation samples and direct hot air drying samples whose moisture contents were lower than the limit in Pharmacopoeia. Research showed that sulfur fumigation can significantly reduce the content of main active ingredients and reduce the efficacy of Puerariae Thomsonii Radix, indicating that the quality of Puerariae Thomsonii Radix was significantly decreased after sulfur fumigation. However, the contents of the main active ingredients, efficacy and storage results of the direct hot air drying samples were similar to those in direct sunshine drying samples, so the hot air drying process was a nice drying technology which could be promoted for use.


Assuntos
Medicamentos de Ervas Chinesas/análise , Fumigação , Temperatura Alta , Isoflavonas/análise , Pueraria/química , Enxofre/química , Animais , Camundongos , Superóxido Dismutase/análise
19.
Zhongguo Zhong Yao Za Zhi ; 41(2): 216-219, 2016 Jan.
Artigo em Chinês | MEDLINE | ID: mdl-28861966

RESUMO

To research the intestinal toxicity of n-BuOH fraction in Phytolacca Radix before and after being processed with vinegar. Toxic n-BuOH fractions were separated from Phytolacca Radix. In the animal model, the level of intestinal edema, water content of intestine and stool, IC50 values of HT-29 and IEC-6 were detected with MTT method to compare the changes in toxicity of n-BuOH fractions from Phytolacca Radix before and after being processed with vinegar. n-BuOH fractions of Phytolacca Radix could cause intestinal edema in mice, increase the edema of duodenum, jejunum and the water content in stool, inhibit the proliferation of HT-29 cells and IEC-6 cells, indicating its intestinal toxicity, with HT-29 IC50 at 14.59 mg•L⁻¹ and IEC-6 IC50 at 43.77 mg•L⁻¹. After being processed with vinegar, the level of intestinal edema, edema of duodenum and jejunum and the water content in stool and inhibition ratio of cells line were reduced, with HT-29 IC50 at 58.51 mg•L⁻¹ and IEC-6 IC50 at 84.37 mg•L⁻¹. After being processed with vinegar, the toxicity of n-BuOH fractions from Phytolacca Radix decreased obviously.


Assuntos
Medicamentos de Ervas Chinesas/administração & dosagem , Medicamentos de Ervas Chinesas/isolamento & purificação , Edema/tratamento farmacológico , Phytolacca/química , Ácido Acético/química , Animais , Química Farmacêutica , Medicamentos de Ervas Chinesas/química , Edema/imunologia , Humanos , Intestinos/efeitos dos fármacos , Intestinos/imunologia , Masculino , Camundongos , Camundongos Endogâmicos ICR , Raízes de Plantas/química
20.
Zhongguo Zhong Yao Za Zhi ; 41(6): 1087-1092, 2016 Mar.
Artigo em Chinês | MEDLINE | ID: mdl-28875675

RESUMO

This study was to investigate the mechanism of gingerols antagonizing the inflammatory effect of toxic raphides from Pinella pedatisecta. Mice peritonitis models induced by toxic raphides from P. pedatisecta were applied to observe the effect of gingerols on inflammatory mediators PGE2 in the exudates of abdominal inflammation in mice; rats peritoneal macrophage in vitro culture models were adopted to study the anti-inflammatory effects of gingerol against toxic raphides, with TNF-α and IL-1ß in supernatant as indexes. Scanning electron microscopy was used to observe the changes in surface morphology of macrophages treated by raphides and gingerols. Macrophages-neutrophils co-cultured models were used to study the antagonism of gingerols against the effect of toxic raphides' stimulation on neutrophils migration. Results showed that gingerols could significantly inhibit the production of PGE2 in the exudates of abdominal inflammation induced by toxic raphides from P. pedatisecta in mice. Gingerols could significantly inhibit the toxic raphides from P. pedatisecta to induce the release of inflammatory factors, with certain dose dependence. Scanning electron microscopy showed that gingerols could significantly inhibit phagocytosis of macrophages, cytomembrane injury, and neutrophils migration induced by toxic raphides from P. pedatisecta. The results showed that the antagonism mechanism of gingerols against the toxic raphides from P. pedatisecta may be associated with inhibiting the pro-inflammatory toxicity including macrophage activation, inflammatory factors release, and neutrophils migration.


Assuntos
Anti-Inflamatórios/administração & dosagem , Catecóis/antagonistas & inibidores , Medicamentos de Ervas Chinesas/toxicidade , Álcoois Graxos/antagonistas & inibidores , Inflamação/tratamento farmacológico , Pinellia/toxicidade , Animais , Catecóis/administração & dosagem , Modelos Animais de Doenças , Antagonismo de Drogas , Álcoois Graxos/administração & dosagem , Humanos , Inflamação/etiologia , Inflamação/imunologia , Interleucina-1beta/imunologia , Macrófagos/efeitos dos fármacos , Macrófagos/imunologia , Masculino , Camundongos , Camundongos Endogâmicos ICR , Neutrófilos/efeitos dos fármacos , Neutrófilos/imunologia , Fagocitose/efeitos dos fármacos , Pinellia/química , Ratos , Ratos Sprague-Dawley , Fator de Necrose Tumoral alfa/imunologia
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