Your browser doesn't support javascript.
loading
Mostrar: 20 | 50 | 100
Resultados 1 - 15 de 15
Filtrar
1.
World J Clin Cases ; 11(35): 8276-8283, 2023 Dec 16.
Artigo em Inglês | MEDLINE | ID: mdl-38130611

RESUMO

BACKGROUND: Acute pancreatitis (AP) is a common inflammatory disease of the pancreas with high mortality rates. It is of great significance to take scientific intervention measures for patients with AP in time. AIM: To explore the effect of standardized nursing combined with mindfulness stress reduction training on the curative effect, negative emotion, and quality of life in patients with acute pancreatitis. METHODS: A total of 80 patients with acute pancreatitis admitted to The First People's Hospital of Jiangxia District Hospital from May 2021 to May 2023 were randomly divided into control group and observation group (n = 40). Patients in control group were given the standardized nursing intervention, and the observation group were given standardized nursing plus mindfulness stress reduction training intervention. The time of clinical symptom disappeared or improved, complication occurrence rate, emotional state, and quality of life score of the two groups were observed and compared. RESULTS: In comparison with the control group, the bowel sound recovery time, ventosity and abdominal pain improvement time, and venting and cacation time in observation group were shorter, and the total incidence rate of complications was reduced, showing statistically significant difference (P < 0.05). The scores of anxiety and depression in observation group were lower than those in control group (P < 0.05). Serum levels of tumour necrosis factor alpha, interleukin (IL)-6, IL-1ß and IL-8 in observation group were lower than those in control group (P < 0.05). The scores of life quality in physiology, psychology, environment and social relations in observation group were higher than those in control group, and the differences were statistically significant (P < 0.05). CONCLUSION: The application of standardized nursing intervention combined with mindfulness stress reduction training in patients with acute pancreatitis has a definite effect, which can help to ameliorate the clinical symptoms, anxiety and depression of patients, reduce the incidence rate of complications, and improve the prognosis of patients.

2.
J Hazard Mater ; 438: 129395, 2022 09 15.
Artigo em Inglês | MEDLINE | ID: mdl-35803190

RESUMO

Compost tea was alternatives of chemical pesticide for green agriculture, but there were no reports about antibiotic resistance genes (ARGs) in compost tea. This study investigated the effect of livestock manures, sewage sludge, their composting products and liquid fermentation on ARGs, mobile genetic elements (MGEs), metal resistance genes (MRGs) and antimicrobial properties of various compost tea. The results showed aerobic liquid fermentation reduced ARGs by 65.93 % and 45.20 % in the compost tea of chicken manure and sludge, enriched ARGs by 8.57 % and 37.41 % in the compost tea of pig manure and bovine manure, and increased MGEs and MRGs by 1.25 × 10-5-5.53 × 10-3 and 2.03 × 10-5-2.03 × 10-3 in the four compost tea. The correlation coefficient of tetracycline and sulfonamide resistance genes between compost product and compost tea were 0.98 and 0.91. aadA2-02, sul2 and tetX abundant in the compost tea were positively correlated with MGEs and MRGs. Furthermore, liquid fermentation enriched the potential host of tetracycline and vancomycin resistance genes. Tetracycline resistance genes occupied 62.7 % of total ARGs in the compost tea. Alcaligenes and Bacillus enriched by 0.78-39.31 % in the four compost tea, which metabolites had high antimicrobial activity. The potential host of ARGs accounted for 42.1 % bacteria abundance in the four compost tea.


Assuntos
Compostagem , Animais , Antibacterianos/farmacologia , Bovinos , Resistência Microbiana a Medicamentos/genética , Genes Bacterianos , Esterco/microbiologia , Metais , Esgotos , Suínos , Chá , Tetraciclina
3.
J Biomed Nanotechnol ; 17(6): 1199-1207, 2021 Jun 01.
Artigo em Inglês | MEDLINE | ID: mdl-34167632

RESUMO

Tetramethylpyrazine (TMP), isolated from the rhizome of the traditional Chinese medicinal plant Chuanxiong (Ligusticum wallichii Franchat) shows therapeutic efficacy against osteoarthritis. After intra-articular injection, the retention time of TMP in the joint cavity is short, which limits its treatment effect. To avoid this problem, the present study explored the preparation of a TMP nanosuspension (TMP-NS) based on hydrophobic ion pairing. TMP-NS showed a particle size of approximately 588 nm and, after intra-articular injection in rats, it had longer retention in the articular cavity, higher TMP concentrations in joints, and greater anti-osteoarthritic efficacy than TMP solution. TMP-NS didn't cause significant inflammation at the joint. These results suggest that TMP-NS may strengthen and prolong the therapeutic efficacy of TMP against osteoarthritis without systemic toxicity.


Assuntos
Ligusticum , Osteoartrite , Animais , Injeções Intra-Articulares , Osteoartrite/tratamento farmacológico , Pirazinas , Ratos
4.
J Sep Sci ; 42(19): 3067-3076, 2019 Oct.
Artigo em Inglês | MEDLINE | ID: mdl-31347249

RESUMO

Ligustrazine was the active ingredient of the traditional Chinese medicine Chuanxiong Rhizoma. However, the content of ligustrazine is very low. We proposed a hypothesis that ligustrazine was produced by the mutual effects between endophytic Bacillus subtilis and the Ligusticum chuanxiong Hort. This study aimed to explore whether the endophytic B. subtilis LB5 could make use of Chuanxiong Rhizoma fermentation matrix to produce ligustrazine and clarify the mechanisms of action preliminarily. Ultra high performance liquid chromatography with quadrupole time-of-flight mass spectrometry analysis showed the content of ligustrazine in Chuanxiong Rhizoma was below the detection limit (0.1 ng/mL), while B. subtilis LB5 produced ligustrazine at the yield of 1.0268 mg/mL in the Chuanxiong Rhizoma-ammonium sulfate fermentation medium. In the fermented matrix, the reducing sugar had a significant reduction from 12.034 to 2.424 mg/mL, and rough protein content increased from 2.239 to 4.361 mg/mL. Acetoin, the biosynthetic precursor of ligustrazine, was generated in the Chuanxiong Rhizoma-Ammonium sulfate (151.2 mg/mL) fermentation medium. This result showed that the endophytic bacteria B. subtilis LB5 metabolized Chuanxiong Rhizoma via secreted protein to consume the sugar in Chuanxiong Rhizoma to produce a considerable amount of ligustrazine. Collectively, our preliminary research suggested that ligustrazine was the interaction product of endophyte, but not the secondary metabolite of Chuanxiong Rhizoma itself.


Assuntos
Bacillus subtilis/química , Medicamentos de Ervas Chinesas/análise , Pirazinas/análise , Rizoma/química , Bacillus subtilis/metabolismo , Cromatografia Líquida de Alta Pressão , Medicamentos de Ervas Chinesas/metabolismo , Fermentação , Espectrometria de Massas , Medicina Tradicional Chinesa , Pirazinas/metabolismo , Rizoma/metabolismo , Fatores de Tempo
5.
Zhongguo Zhong Yao Za Zhi ; 43(19): 3893-3898, 2018 Oct.
Artigo em Chinês | MEDLINE | ID: mdl-30453715

RESUMO

Ligustrazine is an important active ingredient of the traditional Chinese medicine Chuanxiong Rhizoma, but its content is a controversial topic. The endophytes of medicinal plants have the ability to produce the same active substances as the host, so this report focused on the endophytic Bacillus subtilis, to study the origin of ligustrazine in Chuanxiong Rhizoma preliminarily by inoculating the isolated endophytic B. subtilis to the Chuanxiong Rhizoma medium in vitro for solid state fermentation. Tissue grinding method was used to isolate the endogenetic B. subtilis. The morphological features, conventional physiological and biochemical reactions and 16S rRNA molecular techniques were combined to identify the endogenetic strains. Then, the strains that grew well in the medicinal matrix of Chuanxiong Rhizoma were screened out for further fermentation studies. The solid-state fermentation was performed at 37 °C for 30 d using Chuanxiong Rhizoma fermentation medium (40 g Chuanxiong Rhizoma powder, 100 mL sterile water, 121 °C, sterilization for 25 minutes). UPLC was used to detect the contents of ligustrazine, acetoin in the Chuanxiong Rhizoma fermentation medium and Chuanxiong Rhizoma. All the five strains were Gram-positive and had spores. Phylogenetic analysis of the 16S rRNA sequence showed that the endophytes were B. subtilis. The results of UPLC showed that ligustrazine was detected in the Chuanxiong Rhizoma fermentation medium inoculated with endogenetic B. subtilis LB3, LB3-2-1, LB4, LB5 and LB6-2, while not detected neither in blank Chuanxiong Rhizoma fermentation medium nor in Chuanxiong Rhizoma. This study showed that the endogenetic B. subtilis of Ligusticum chuanxiong Hort. can make use of Chuanxiong Rhizoma fermentation medium to produce ligustrazine. Endogenetic B. subtilis has a certain correlation with the accumulation of ligustrazine in Rhizoma Chuanxiong. We speculate that the ligustrazine may be derived from the catabolism of endogenetic B. subtilis in Ligusticum chuanxiong.


Assuntos
Bacillus subtilis , Ligusticum/química , Ligusticum/microbiologia , Pirazinas/análise , Endófitos , Fermentação , Filogenia , RNA Ribossômico 16S , Rizoma/química
6.
J Pharm Biomed Anal ; 161: 455-463, 2018 Nov 30.
Artigo em Inglês | MEDLINE | ID: mdl-30216794

RESUMO

Gentianopsis barbata, Halenia corniculata, and Gentianella acuta were widely distributed throughout China and commonly used in traditional Chinese medicine. However, owing to similar living environments and morphological features, locals often had trouble distinguishing between these three species. In this present study, chromatograms at 350 nm were obtained and the composition and content of their chemical compounds determined using HPLC-DAD/ESI-MS2. In total, 35 chemical compounds were detected, 32 of which were identified, 25 of which were xanthones, 6 flavonoids, and 1 chlorogenic acid. The 350 nm chromatograms of these three species displayed evident differences. The individual compounds and their occurrence and content in different parts of the plant within different species were included in our results. This basic data will be useful for future pharmacological study. The total compositions of flavonoids and xanthones were approximately comparable in G. barbata and H. corniculata. Meanwhile, xanthones were predominant in G. acuta. From the perspective of chemical compound compositions, the leaf is recommended as the most valuable medicinal section for each of these three species.


Assuntos
Ácido Clorogênico/análise , Medicamentos de Ervas Chinesas/química , Flavonoides/análise , Gentianaceae/química , Xantonas/análise , Cromatografia Líquida de Alta Pressão , Estruturas Vegetais/química , Espectrometria de Massas por Ionização por Electrospray
7.
Biomed Pharmacother ; 102: 539-548, 2018 Jun.
Artigo em Inglês | MEDLINE | ID: mdl-29587240

RESUMO

BACKGROUND AND PURPOSE: Tea drinking has positive effects on bone health and may prevent and treat osteoporosis, especially in older and postmenopausal women. Tea polysaccharide (TPS) is a major bioactive constituent in tea. Despite its profound effects on human health, whether TPS has anti-osteoporotic effects remains largely unknown. As such, we investigated the anti-osteoporotic effects of TPS. METHODS: In vitro, TPS effects on osteoclastogenesis were examined using osteoclast precursor RAW264.7 cells. TPS effects on osteoclastogenesis-related expression of marker genes and proteins were determined by gene expression and immunoblotting analyses, respectively. For in vivo studies, 12-week-old female Wistar rats were divided randomly into a sham-operated group (sham) and four ovariectomized (OVX) subgroups: OVX with vehicle (model) and OVX with low-, medium-, and high-dose TPS (0.32, 0.64 and 1.28 g/kg body weight/day, respectively). TPS was administered intragastrically to rats for 13 weeks. Body weight, blood biochemical parameters, organ weight, organ coefficients, femoral length, bone mineral density (BMD), biomechanical properties, and bone microarchitecture were documented. RESULTS: TPS inhibited osteoclast differentiation significantly and dose-dependently, and its inhibitory effect was not due to toxicity to RAW264.7 cells. TPS suppressed expression of osteoclastogenesis-related marker genes and proteins significantly. In in vivo studies, medium-dose TPS treatment ameliorated OVX-induced calcium loss significantly. Low-dose TPS treatment decreased the activity of acid phosphatase (ACP) in OVX rats significantly. In addition, TPS treatment improved other blood biochemical parameters and femoral biomechanical properties to a certain extent. More importantly, TPS treatment ameliorated bone microarchitecture in OVX rats strikingly because of increased cortical bone thickness and trabecular bone area in the femur. CONCLUSION: TPS can inhibit receptor activator nuclear factor-kappa B ligand (RANKL)-induced osteoclastogenesis in RAW264.7 cells and ameliorate ovariectomy-induced osteoporosis in rats.


Assuntos
Osteoclastos/patologia , Osteogênese/efeitos dos fármacos , Osteoporose/tratamento farmacológico , Osteoporose/etiologia , Ovariectomia/efeitos adversos , Polissacarídeos/uso terapêutico , Ligante RANK/farmacologia , Chá/química , Animais , Biomarcadores/metabolismo , Diferenciação Celular/efeitos dos fármacos , Feminino , Fêmur/efeitos dos fármacos , Fêmur/patologia , Regulação da Expressão Gênica/efeitos dos fármacos , Camundongos , Tamanho do Órgão/efeitos dos fármacos , Osteoclastos/efeitos dos fármacos , Osteoclastos/metabolismo , Osteoporose/sangue , Osteoporose/patologia , Polissacarídeos/farmacologia , Células RAW 264.7 , Ratos Wistar , Aumento de Peso/efeitos dos fármacos
8.
Phytochemistry ; 146: 16-24, 2018 Feb.
Artigo em Inglês | MEDLINE | ID: mdl-29207319

RESUMO

Mu Dan Pi is a traditional Chinese medicine used to treat inflammation, cancer, allergies, diabetes, angiocardiopathy, and neurodegenerative diseases. In this study, the metabolome variation within Mu Dan Pi collected from 372 tree peony cultivars was systematically investigated. In total, 42 metabolites were identified, comprising of 14 monoterpene glucosides, 11 tannins, 8 paeonols, 6 flavonoids, and 3 phenols. All cultivars revealed similar metabolite profiles, however, they were further classified into seven groups on the basis of their varying metabolite contents by hierarchical cluster analysis. Traditional cultivars for Mu Dan Pi were found to have very low metabolite contents, falling into clusters I and II. Cultivars with the highest amounts of metabolites were grouped in clusters VI and VII. Five potential cultivars, namely, 'Bai Yuan Qi Guan', 'Cao Zhou Hong', 'Da Zong Zi', 'Sheng Dan Lu', and 'Cheng Xin', with high contents of monoterpene glycosides, tannins, and paeonols, were further screened. Interestingly, the majority of investigated cultivars had relatively higher metabolite contents compared to the traditional medicinal tree peony cultivars.


Assuntos
Medicamentos de Ervas Chinesas/isolamento & purificação , Paeonia/química , Compostos Fitoquímicos/isolamento & purificação , Medicamentos de Ervas Chinesas/química , Medicina Tradicional Chinesa , Estrutura Molecular , Compostos Fitoquímicos/química , Raízes de Plantas/química
9.
Front Pharmacol ; 8: 324, 2017.
Artigo em Inglês | MEDLINE | ID: mdl-28620304

RESUMO

Background and Objective: Tea drinking is associated with positive effects on bone health and may protect against osteoporosis, especially in elderly women. Pu-erh tea has many beneficial effects on human health; however, whether Pu-erh tea has anti-osteoporotic potential remains unclear. Thus, we investigated the effects of Pu-erh tea extract (PTE) on ovariectomy-induced osteoporosis in rats and on osteoclastogenesis in vitro. Methods: Female Wistar rats were divided into six groups: the sham, model, and Xian-Ling-Gu-Bao capsule (XLGB) groups, and the low-, medium-, and high-dose PTE groups. Ovariectomized (OVX) rats were used as an animal model of osteoporosis. The animals were intragastrically administered distilled water, XLGB, or different concentrations of PTE for 13 weeks. Body weight, blood biochemical indicators, relative organ coefficients, femoral bone mineral density (BMD), bone biomechanical properties, and bone microarchitecture were examined and analyzed. Additionally, the in vitro effects of PTE on osteoclastic activities were investigated using the RAW 264.7 cell line as an osteoclast differentiation model. The effects of PTE on osteoclast differentiation and the expression of osteoclast-specific genes and proteins were determined. Results: PTE reduced OVX-induced body weight gain after 6 weeks of treatment, and the high-dose exerted a significant effect. High-dose PTE significantly ameliorated OVX-induced estradiol (E2) deficiency. PTE treatment maintained calcium and phosphorus homeostasis and improved other blood biochemical parameters to various degrees. In addition, PTE treatment improved organ coefficients of the femur, uterus, and vagina and improved femoral BMD and bone biomechanical properties. PTE treatment strikingly ameliorated bone microarchitecture. Moreover, in the in vitro studies, osteoclast differentiation using the differentiation cell model was significantly inhibited by PTE without cytotoxic effects. Additionally, PTE efficaciously suppressed the expression of key osteoclast-specific genes and proteins. Conclusion: PTE can ameliorate ovariectomy-induced osteoporosis in rats and suppress osteoclastogenesis in vitro.

10.
Food Chem ; 219: 490-495, 2017 Mar 15.
Artigo em Inglês | MEDLINE | ID: mdl-27765256

RESUMO

Vaccinium glaucoalbum, a perennial evergreen shrub, is naturally distributed in high-altitude areas. In this study, the composition and content of polyphenolic compounds in the fruit and leaf of V. glaucoalbum were characterized. In total, 24 chemical compounds were detected and identified by HPLC-DAD and HPLC-ESI-MS2. Among all the compounds determined, 15 were anthocyanins and detected in fruit, 5 were flavonols and monitored in leaf, and 4 were chlorogenic acids and found in both fruit and leaf. The total anthocyanin content (TAC) of fruit (682mg/100gFW) was the highest among wild Vaccinium berries in China which have been investigated for now, and the total flavonol content of leaf was 2764mg/100gFW. The antioxidant activity of both fruit and leaf was assessed by DPPH and FRAP assays. Given its high TAC and strong antioxidant activity, the fruit of V. glaucoalbum has great potential in functional food.


Assuntos
Antioxidantes/metabolismo , Frutas/metabolismo , Extratos Vegetais/metabolismo , Folhas de Planta/metabolismo , Polifenóis/metabolismo , Vaccinium/metabolismo , Antocianinas/metabolismo , China , Cromatografia Líquida de Alta Pressão , Flavonóis/metabolismo , Espectrometria de Massas
11.
Food Chem ; 187: 20-8, 2015 Nov 15.
Artigo em Inglês | MEDLINE | ID: mdl-25976993

RESUMO

Water lily, a member of the Nymphaeaceae family, can be made into tea on the basis of outstanding fragrance characteristics and health care functions. In this study, 16 flavonoids were identified and quantified in tea infusions prepared from the petals of 33 water lily cultivars using HPLC-DAD and HPLC-ESI-MS/MS. The infusions were analyzed with HS-SPME coupled with GC-MS; 29 volatile compounds were detected, of which nine were found to be scent components. The cultivars were clustered into three clusters characterized according to scent components. The 'Conqueror' and 'Virginia' cultivars had the highest antioxidant activities. The concentrations of polyphenols and flavonoids showed significant positive correlations with antioxidant activity as measured by DPPH, ABTS(+), and FRAP assays. This study is valuable for a fuller understanding of this important tea and can also be used for the development of water lily.


Assuntos
Antioxidantes/análise , Flavonoides/análise , Nymphaea/química , Chás de Ervas/análise , Compostos Orgânicos Voláteis/análise , Cromatografia Líquida de Alta Pressão , Flores/química , Cromatografia Gasosa-Espectrometria de Massas , Polifenóis/análise , Espectrometria de Massas em Tandem
12.
Artigo em Inglês | MEDLINE | ID: mdl-24963331

RESUMO

The antiviral activity of total flavonoid extracts from Selaginella moellendorffii Hieron and its main constituents amentoflavone were investigated against coxsackie virus B3 (CVB3). When added during or after viral infection, the extracts and amentoflavone prevented the cytopathic effect (CPE) of CVB3, as demonstrated in a 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyl tetrazolium bromide (MTT) colorimetric assay, with a 50% inhibitory concentration (IC50) from 19 ± 1.6 to 41 ± 1.2 µ g/mL and 25 ± 1.2 to 52 ± 0.8 µ g/mL, respectively. KM mice were used as animal models to test the extracts' activity in vivo. Oral administration of the total flavonoid extracts at 300 mg/kg/day significantly reduced mean viral titers in the heart and kidneys as well as mortality after infection for 15 days. The experimental results demonstrate that in vitro and in vivo the model mice infected with CVB3 can be effectively treated by the total flavonoid extracts from Selaginella moellendorffii Hieron.

13.
Zhongguo Zhen Jiu ; 33(5): 451-4, 2013 May.
Artigo em Chinês | MEDLINE | ID: mdl-23885625

RESUMO

As a famous TCM physician and acupuncturist in our country, professor GUAN Ji-duo, who was determined to study medicine and save life from a child, has been engaged in teaching and clinical work of acupuncture and moxibustion for more than sixty years. With a lifetime writing and tireless teaching, he has made every effect, from small clue to see what is coming, to be well-versed in the learning of both ancient and modern times and learn widely from others' points to devote all his life for the development and innovation of acupuncture and moxibustion. With deep study on syndrome differentiation of meridians, he has focused on acupoint combination, advocated on painless insertion of needle, and made "smokeless moxa-stick" to form a unique academic thought. At the age of more than 90, professor GUAN still insists on outpatient clinic, which is highly respected.


Assuntos
Terapia por Acupuntura/história , Acupuntura/história , Acupuntura/educação , China , História do Século XX , História do Século XXI , Humanos , Masculino , Moxibustão/história , Recursos Humanos
14.
Artigo em Chinês | MEDLINE | ID: mdl-21038687

RESUMO

OBJECTIVE: To study protective effect and pathogenesis of complex salvia miltiorrhiza (DanShen) on acute mercury poisoning in rabbits. METHODS: Models of acute mercury poisoning was made in rabbits. The effect of complex salvia miltiorrhiza on blood urea nitrogen (BUN), copper-protein (CP), lactate dehydrogenase (LDH), acid phosphatase (ACP) and the malondialdehyde (MDA) in plasma, superoxide dismutase (SOD) in erythrocyte and MDA, SOD in tissues homogenate were observed. RESULTS: The administration of complex salvia miltiorrhiza after mercury injection 0.5 h and 9.5 h, decreased BUN, CP, MDA, LDH and ACP, and prevented the reduction of SOD. Compared with mercury poisoning group, the difference was statistical significant (P < 0.05, P < 0.01). CONCLUSION: It is suggested that acute mercury poisoning may result in renal damage but also multiple organ tissues, and complex salvia miltiorrhiza possesses protective effect, through stabilized membranes.


Assuntos
Medicamentos de Ervas Chinesas/farmacologia , Intoxicação por Mercúrio/sangue , Fenantrolinas/farmacologia , Salvia miltiorrhiza , Animais , Medicamentos de Ervas Chinesas/uso terapêutico , Feminino , Masculino , Intoxicação por Mercúrio/tratamento farmacológico , Fenantrolinas/uso terapêutico , Coelhos
15.
J Med Chem ; 45(12): 2651-8, 2002 Jun 06.
Artigo em Inglês | MEDLINE | ID: mdl-12036374

RESUMO

Moffatt oxidation of 2',3'-O-isopropylideneuridine (1a) and treatment of the crude 5'-aldehyde with formylmethylene-stabilized Wittig reagent gave the vinylogously extended 7'-aldehyde2a. Condensation of 2a with ethoxycarbonyl- or dibromomethylene phosphorane reagents gave the conjugated dienes 6a and 4a, respectively. Deacetonization gave diene ester 7a [5'(E),7'(E); with s-trans conformation] and dibromodiene 5a [5'(E)], respectively. Analogously, 2',3'-O-isopropylideneadenosine (1b) was Wittig-extended into the conjugated dibromodiene 5b [5'(E)] and dienoic ester 7b [5'(E),7'(E)]. Furthermore, palladium-catalyzed coupling of the vinyl 6'(E)-stannanes 14 with (E) and (Z) ethyl 3-iodoacrylate gave stereodefined access to dienoic esters 7 (E,E) and 16 (E,Z). Incubation of AdoHcy hydrolase with 100 microM of 5b resulted in partial inhibition of the enzyme without any apparent change in the enzyme's nicotinamide adenine dinucleoside (NAD(+)) content. In contrast, 7b and 16b produced time- and concentration-dependent inactivation of S-adenosyl-L-homocysteine (AdoHcy) hydrolase producing significant decreases in the enzyme's NAD(+) content. However, 7b and 16b upon incubation with AdoHcy hydrolase were not metabolized suggesting that these compounds are type I mechanism-based inhibitors. No specific antiviral activity was noted for 5a,b, 7a,b, and 16a,b against any of the viruses tested; dibromodiene 5b proved cytotoxic at a concentration > or =6.7 microM and cytostatic at > or =11 microM, while dienoic esters 16a,b showed activity against both varicella-zoster virus (at 10 microM, 16a) and cytomegalovirus (at 10 microM, 16a; 18 microM, 16b).


Assuntos
Adenosina/análogos & derivados , Adenosina/síntese química , Alcadienos/síntese química , Antineoplásicos/síntese química , Antivirais/síntese química , Carboidratos/química , Hidrolases/antagonistas & inibidores , Uridina/análogos & derivados , Uridina/síntese química , Adenosina/química , Adenosina/farmacologia , Adenosil-Homocisteinase , Alcadienos/química , Alcadienos/farmacologia , Antineoplásicos/química , Antineoplásicos/farmacologia , Antivirais/química , Antivirais/farmacologia , Linhagem Celular , Citomegalovirus/efeitos dos fármacos , Avaliação Pré-Clínica de Medicamentos , Inibidores Enzimáticos/síntese química , Inibidores Enzimáticos/química , Inibidores Enzimáticos/farmacologia , HIV-1/efeitos dos fármacos , HIV-2/efeitos dos fármacos , Herpesvirus Humano 3/efeitos dos fármacos , Humanos , Uridina/química , Uridina/farmacologia
SELEÇÃO DE REFERÊNCIAS
DETALHE DA PESQUISA