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1.
Front Pediatr ; 11: 1110632, 2023.
Artigo em Inglês | MEDLINE | ID: mdl-37528873

RESUMO

Objective: To explore the effect of esketamine nasal drops on pain in children after tonsillectomy using low-temperature plasma ablation. Methods: 76 children who underwent tonsillectomy between May 2020 and July 2021, were randomly divided into two groups of 38 cases each. Patients in the control group were treated with conventional medication, while those in the study group were treated with esketamine nasal drops, along with the routine drug treatment. Pain levels of children in the two groups were compared within 1-3 days post-surgery, and the pseudomembrane formation and shedding-off time and recovery time were statistically analyzed. Results: The pain level of children in the study group was lower than that of the control group 1-3 days post-surgery. The pseudomembrane formation and shedding-off time and recovery time in the study group were shorter than in the control group (P < 0.05). There was no significant difference in the incidence of adverse reactions between the two groups, and there were no serious adverse reactions in the two groups (P > 0.05). Conclusion: It is safe to use esketamine nasal drops in children after tonsillectomy using low temperature plasma ablation, and this is found to reduce pain and shorten the recovery time.

2.
Bioorg Chem ; 101: 104036, 2020 08.
Artigo em Inglês | MEDLINE | ID: mdl-32629283

RESUMO

Oleanolic acid (OA) and its semi-synthetic derivatives have been reported to have a wide range of biological activities. The introduction of electrophilic Michael acceptor group can increase the reactivity of OA to cellular targets and thus improve the anti-tumor activity. In this work, a series of novel α,ß-unsaturated carbonyl derivatives of OA were designed and synthesized. Their in vitro cytotoxic activity against MCF-7, HepG2 and HeLa cells were tested. Most derivatives exhibited improved cell growth inhibitory activity, especially for 3d with an IC50 of 0.77 µM in MCF-7 cells. Moreover, 3d inhibited the migration of MCF-7 and HeLa cells at the concentration of 4 µM. Flow cytometric analysis revealed that 3d induced cell apoptosis and S phase arrest in a concentration-dependent manner. Western blotting experiment demonstrated that 3d inhibited the phosphorylation of AKT and mTOR. These results suggest that this series of OA derivatives bearing exocyclic methylene ketone pharmacophore are promising anticancer agents as potential PI3K/AKT/mTOR pathway inhibitors.


Assuntos
Antineoplásicos/uso terapêutico , Ácido Oleanólico/uso terapêutico , Fosfatidilinositol 3-Quinases/efeitos dos fármacos , Proteínas Proto-Oncogênicas c-akt/efeitos dos fármacos , Antineoplásicos/farmacologia , Humanos , Estrutura Molecular , Ácido Oleanólico/farmacologia , Transdução de Sinais , Relação Estrutura-Atividade
3.
Med Sci Monit ; 25: 1053-1060, 2019 Feb 07.
Artigo em Inglês | MEDLINE | ID: mdl-30730866

RESUMO

BACKGROUND This study aimed to investigate the effectiveness of perioperative parecoxib sodium combined with transversus abdominis plane (TAP) block on postoperative pain management following hepatectomy in patients with hepatocellular carcinoma (HCC). MATERIAL AND METHODS One hundred patients with HCC who underwent hepatectomy were randomized into a study group (n=51) and a control group (n=49). The study group received 40 mg of parecoxib sodium 30 minutes before anesthetic induction, and 150 mg of 0.375% ropivacaine with 5 mg dexamethasone as TAP inhibitors, before closing the abdominal incision. The control group received 40 mg of placebo 30 minutes before anesthetic induction, without TAP block. Postoperatively, all patients received patient-controlled intravenous analgesia (PCIA) and evaluation with subjective visual analog scale (VAS) pain scores. Data on adverse events, postoperative ambulation (>6 hours/day), time of flatus and defecation, and hospitalization duration were recorded. RESULTS Pain scores of the study group were significantly lower compared with the control group on the first three postoperative days. No significant differences were found between the two groups in terms of adverse events. In the study group, the number of cases of postoperative ambulation was significantly more than the control group. The onset of flatus and defecation and duration of hospital stay in the study group were significantly shorter in the study group compared with the control group. CONCLUSIONS Parecoxib sodium combined with TAP block effectively reduced postoperative pain, improved ambulation, improved gastrointestinal function, and shortened hospitalization time following hepatectomy in patients with HCC without adverse effects.


Assuntos
Isoxazóis/farmacologia , Manejo da Dor/métodos , Dor Pós-Operatória/tratamento farmacológico , Músculos Abdominais/efeitos dos fármacos , Adulto , Idoso , Analgesia Controlada pelo Paciente/métodos , Analgésicos Opioides/administração & dosagem , Anestésicos Locais/administração & dosagem , Carcinoma Hepatocelular/tratamento farmacológico , Carcinoma Hepatocelular/cirurgia , China , Feminino , Hepatectomia , Humanos , Neoplasias Hepáticas/tratamento farmacológico , Neoplasias Hepáticas/cirurgia , Masculino , Pessoa de Meia-Idade , Bloqueio Nervoso/métodos , Medição da Dor/métodos , Complicações Pós-Operatórias/tratamento farmacológico , Estudos Prospectivos , Ropivacaina/farmacologia
4.
Bioorg Chem ; 85: 357-363, 2019 04.
Artigo em Inglês | MEDLINE | ID: mdl-30658235

RESUMO

In this paper, the mechanism of orobanone analogues formation via aromatization rearrangement of curcumol was minutely explored. Aromatization of curcumol with acetone under acidic condition was selected as the model reaction. The formation of a stable aromatic system was the driving force for this reaction. Based on the model reaction, other four new orobanone analogues were prepared through curcumol reacting with different carbonyl compounds. The results showed that the stability of carbocation, which was generated from the carbonyl compounds, and the steric hindrance were main factors affecting the aromatization. We also synthesized the analogue of aromaticane B using compound 2. In vitro anti-proliferative activity of some derivatives were tested by MTT assay. Two derivatives showed weak anti-tumor effect on two cancer cell lines (HepG2 and MCF7) under normoxia. Four orobanone analogue 2, 5, 6 and 9 significantly inhibited hypoxia-induced HIF-1 luciferase reporter activity in HeLa cells with the IC50 values of 13.6, 6.6, 2.4 and 18.2 µM, respectively.


Assuntos
Fator 1 Induzível por Hipóxia/antagonistas & inibidores , Sesquiterpenos/farmacologia , Antineoplásicos/síntese química , Antineoplásicos/farmacologia , Hipóxia Celular/fisiologia , Linhagem Celular Tumoral , Proliferação de Células/efeitos dos fármacos , Humanos , Fator 1 Induzível por Hipóxia/genética , Sesquiterpenos/síntese química , Transcrição Gênica/efeitos dos fármacos
5.
Artigo em Inglês | MEDLINE | ID: mdl-28638871

RESUMO

BACKGROUND: Kidney tonifying - spleen strengthening method being one of the modalities for treatment of astheno-oligozoospermia is currently commonly used in the clinical setting. To investigate the mechanism of YiShenJianPi (YSJP) Recipe, used in Traditional Chinese Medicine to benefit "the kidney" and strengthen "the spleen". MATERIALS AND METHODS: Oligoasthenozoospermia, male BALB/c mice were randomly divided into normal control, disease model, positive control, low-dosage and high-dosage groups. Oligoasthenozoospermia was induced by tripterygium glucosides intragastric administration before treatment started. Through using computer-aided sperm analysis to test the changes in sperm quality, utilizing flow cytometry to test the percentage of sperm with normal mitochondrial transmembrane potential (JC-1 + %), utilizing X-ray microscopy to observe epididymal sperm ultra-microstructure placing special emphasis and photographing the differences in mitochondria of the flagellum region. RESULTS: Compared with DM, sperm quality of the treated mice was significantly better (P<0.05, respectively). Compared with PC, the LD group had significantly better quality sperms, while the parameters in the HD group were numerically better. Compared with NC, all other groups had significantly lower percentage of sperms with normal mitochondrial membrane potential. In PC, LD and HD groups, the percentage of sperms with normal mitochondrial membrane potential was significantly higher than that of D. The 9+9+2 mitochondrial sheath structure was complete in NC but damaged in DM. In the treatment groups, this structure was fairly clear. CONCLUSION: YSJP improved semen quality with oligoasthenozoospermia by improving sperm mitochondrial membrane potential and restoring sperm mitochondrial ultrastructure.


Assuntos
Astenozoospermia/tratamento farmacológico , Medicamentos de Ervas Chinesas/administração & dosagem , Tripterygium/toxicidade , Animais , Astenozoospermia/induzido quimicamente , Astenozoospermia/fisiopatologia , Glicosídeos/toxicidade , Humanos , Masculino , Potencial da Membrana Mitocondrial/efeitos dos fármacos , Camundongos , Camundongos Endogâmicos BALB C , Mitocôndrias/efeitos dos fármacos , Motilidade dos Espermatozoides , Espermatozoides/citologia , Espermatozoides/efeitos dos fármacos
6.
Eur J Med Chem ; 112: 196-208, 2016 Apr 13.
Artigo em Inglês | MEDLINE | ID: mdl-26896708

RESUMO

A series of flavone-7-phosphoramidate derivatives were synthesized and tested for their antiproliferative activity in vitro against human hepatoma cell line HepG2 and human normal hepatic cell line L-O2. Compound 8d, 16d and 17d, incorporating the amino acid alanine, exhibited high inhibitory activity on HepG2 cell line with IC50 values of 9.0 µmol/L, 5.5 µmol/L and 6.6 µmol/L. The introduction of acyl groups played a pivotal role in the selective inhibition toward human hepatoma HepG2 cells, except for compound 8a, 9a and 16b. Compound 8d, 16d and 17d could significantly induce G2/M arrest in HepG2 cells. Specially, Compound 16d could lead early apoptosis in HepG2 cells.


Assuntos
Amidas/química , Amidas/farmacologia , Antineoplásicos/química , Antineoplásicos/farmacologia , Proliferação de Células/efeitos dos fármacos , Flavonas/química , Flavonas/farmacologia , Ácidos Fosfóricos/química , Ácidos Fosfóricos/farmacologia , Apoptose/efeitos dos fármacos , Pontos de Checagem do Ciclo Celular/efeitos dos fármacos , Linhagem Celular , Células Hep G2 , Humanos , Fígado/citologia , Fígado/efeitos dos fármacos , Fígado/patologia , Neoplasias Hepáticas/tratamento farmacológico , Neoplasias Hepáticas/patologia
7.
Zhong Yao Cai ; 37(11): 2034-8, 2014 Nov.
Artigo em Chinês | MEDLINE | ID: mdl-26027127

RESUMO

OBJECTIVE: To explore antithrombotic effects and mechanisms of total alkaloids (VnA) and single alkaloids (Al - A6) from Veratrum nigrum. METHODS: The effects of VnA and Al - A6 on thrombosis and coagulation parameters (APTT, PT and TT) were examined in rat in vivo, while their effects on platelet aggregation induced by ADP and thrombin were determined in rabbit in vitro. RESULTS: VnA and Al ~ A5 decreased thrombus wet weight and platelet aggregation, increased TT, while they had no influence on APTT or PT. A6 had no obvious effect on thrombus wet weight, platelet aggregation or coagulation parameters. CONCLUSIONS: VnA and Al ~ A5 have antithrombotic activities on venous thrombosis. The effective component in VnA is A2 probably. The antithrombotic effects are possibly related to the inhibition of platelet aggregation and the extension of TT. The cevanine type skeleton of steroidal alkaloids is necessary for antithrombotic activities and the ester substitute at C3 can enhance antithrombotic activities.


Assuntos
Alcaloides/farmacologia , Trombose Venosa/tratamento farmacológico , Veratrum/química , Alcaloides/química , Animais , Coagulação Sanguínea , Testes de Coagulação Sanguínea , Agregação Plaquetária , Inibidores da Agregação Plaquetária , Coelhos , Ratos , Relação Estrutura-Atividade , Trombina
8.
Chin J Integr Med ; 18(3): 222-9, 2012 Mar.
Artigo em Inglês | MEDLINE | ID: mdl-22466949

RESUMO

OBJECTIVE: To assess the efficacy and safety of external application of Chinese herbal drugs (ex-CHD) in the treatment of psoriasis. METHODS: Literature regarding randomized clinical trials (RCTs) of psoriasis treatments with ex-CHD, either alone or combined with Western medicine (WM) or physiotherapy, controlled by untreated, placebo or WM treatment were found in electronic databases, including PubMed/MEDLINE, EMBASE, Cochrane Library, Cochrane Central Register of Controlled Trials, China Biology Medicine Disc (CBM), Chinese National Knowledge Infrastructure (CNKI), Wanfang database and VIP database from their inception through July 2011. Study selection, data extraction, quality assessment, and data analyses were conducted according to the Cochrane standards. RESULTS: A total of 10 randomized trials (involving 1,435 patients) were included. Because both test and control drugs used in the RCTs were different from each other, the effects can only be described singly and calculated. Regarding the total effective rate for the treatment of psoriasis, ex-CHD in combination with ultraviolet radiation b (UVB) or narrow band ultraviolet radiation b (NB-UVB), which was reported in 6 trials, was superior to UVB alone. One study reported that ex-CHD and externally applied WM had equivalent effects. In another study, ex-CHD showed better results than placebo. However, another two comparisons of ex-CHD and WM (all in combining with oral WM) showed uncertain outcomes. Nine trials reported adverse reactions. Of these, 7 RCTs included statistical analysis. The results showed that the side-effects that occurred in ex-CHD combined with UVB were less severe than those caused by UVB alone, but the incidence was roughly the same as WM. CONCLUSION: The evidence supporting the efficacy of ex-CHD with respect to treating psoriasis is quite limited and must be strengthened by high-quality studies.


Assuntos
Medicamentos de Ervas Chinesas/administração & dosagem , Medicamentos de Ervas Chinesas/uso terapêutico , Psoríase/tratamento farmacológico , Administração Tópica , Medicamentos de Ervas Chinesas/efeitos adversos , Humanos , Fototerapia , Ensaios Clínicos Controlados Aleatórios como Assunto , Resultado do Tratamento
9.
Zhongguo Zhong Yao Za Zhi ; 31(11): 904-6, 2006 Jun.
Artigo em Chinês | MEDLINE | ID: mdl-17048630

RESUMO

OBJECTIVE: Discuss the functional mechanism of treating male infertility with Bushen Shengjing pill (BS). METHOD: Fill the SD rat with adenine so as to injure the germ cell which will produce the model rat with kidney yang deficiency. Measure the activity of SOD and NOS, the amount of NO and MDA in the testicle. RESULT: BS can promote the activity of SOD, reduce the activity of NOS and the amount of NO and MDA. CONCLUSION: BS has the function of protecting the germ cell which is closely related to the function that the pill can promote the activity of SOD, reduce the activity of NOS and the amount of NO and MDA.


Assuntos
Medicamentos de Ervas Chinesas/farmacologia , Nefropatias/metabolismo , Óxido Nítrico Sintase/metabolismo , Óxido Nítrico/metabolismo , Deficiência da Energia Yang/metabolismo , Adenina , Animais , Combinação de Medicamentos , Medicamentos de Ervas Chinesas/isolamento & purificação , Fármacos para a Fertilidade Masculina/farmacologia , Nefropatias/induzido quimicamente , Masculino , Malondialdeído/metabolismo , Plantas Medicinais/química , Distribuição Aleatória , Ratos , Ratos Sprague-Dawley , Espermatogênese/efeitos dos fármacos , Superóxido Dismutase/metabolismo , Testículo/metabolismo , Deficiência da Energia Yang/induzido quimicamente
10.
Eur J Med Chem ; 41(9): 1084-9, 2006 Sep.
Artigo em Inglês | MEDLINE | ID: mdl-16875760

RESUMO

Stilbene derivatives have wide range of activities. In an effort to find other potential activities of this kind of compounds, 17 derivatives, including resveratrol, were synthesized. Twelve of them were evaluated for their antiviral potential against severe acute respiratory syndrome (SARS)-CoV-induced cytopathicity in Vero E6 cell culture. The result showed that SARS virus was totally inhibited by compounds 17 and 19 (

Assuntos
Coronavírus Relacionado à Síndrome Respiratória Aguda Grave/efeitos dos fármacos , Coronavírus Relacionado à Síndrome Respiratória Aguda Grave/fisiologia , Estilbenos/síntese química , Estilbenos/farmacologia , Replicação Viral/efeitos dos fármacos , Animais , Chlorocebus aethiops , Estrutura Molecular , Estilbenos/química , Relação Estrutura-Atividade , Células Vero
11.
Zhong Xi Yi Jie He Xue Bao ; 3(3): 174-7, 2005 May.
Artigo em Chinês | MEDLINE | ID: mdl-15885160

RESUMO

Chinese traditional surgery, an important branch of traditional Chinese medicine, has contributed greatly to the people's health in the history. With the fast development of modern medicine, Chinese traditional surgery is faced with serious challenges and its shortcomings have appeared more and more evident. In this article, the authors analyzed some problems in the development of Chinese traditional surgery and the opportunities for its further development, and suggested that the superiorities of Chinese traditional surgery should be enhanced in its future development.


Assuntos
Cirurgia Geral/tendências , Medicina Tradicional Chinesa/tendências , China , Diagnóstico Diferencial , Cirurgia Geral/história , História do Século XVII , História do Século XVIII , História do Século XX , Humanos , Medicina Tradicional Chinesa/história
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