RESUMO
The organic extract of Periplaneta americana L. (Dictyoptera; Blattidae) has been traditionally used in southwestern China as an alternative medicine against disorders such as hepatitis, trauma, gastric ulcers, burns, and heart disease. The present study describes bioassay-guided purification and chemotherapeutic evaluation of the 60% ethanolic fraction of P americana organic extracts (PAE60). The most effective cytotoxic fraction was determined by way of repeated in vitro screenings against 12 distinct cultured human carcinoma cell lines: Eca 109, BGC823, HO8910, LS174T, CNE, HeLa, K562, PC-3, A549, BEL 7404, HL-60, and KB, followed by in vivo antitumor assays of the lead fraction (PAE60). The complexity of enriched active fraction was qualitatively evaluated using thin layer chromatography. Reconstituted PAE60 was effective at inhibiting HL-60, KB, CNE, and BGC823 cell growth with IC(50) values <20 µg mL-(1). PAE60 reduced tumor growth in S180-bearing immunocompetent mice by 72.62% after 10 days following oral doses of 500 mg kg d-(1) compared with 78.75% inhibition following 40 mg kg d-(1) of cyclophosphamide (CTX). Thymus and spleen indices of S180-bearing mice treated with PAE60 were significantly greater (P < .05) than CTX treatment groups, suggesting potential immunomodulation of antitumor host defenses by PAE60. Antiviral activity was also investigated and PAE60 inhibited herpes simplex type-2 replication (IC(50) = 4.11 ± 0.64 µg mL-(1)) with a selectivity index (CC(50) to IC(50) ratio) of 64.84 in Vero cells but was less effective on type-1 virus (IC(50) of 25.6 ± 3.16 µg mL-(1)). These results support future clinical trials on P. americana as an alternative or complementary medicinal agent.
Assuntos
Antineoplásicos/química , Antineoplásicos/farmacologia , Periplaneta/química , Extratos de Tecidos/química , Extratos de Tecidos/farmacologia , Animais , Antivirais/química , Antivirais/farmacologia , Linhagem Celular Tumoral , Chlorocebus aethiops , Ciclofosfamida/farmacologia , Ensaios de Seleção de Medicamentos Antitumorais , Células HL-60 , Células HeLa , Herpesvirus Humano 1/efeitos dos fármacos , Herpesvirus Humano 2/efeitos dos fármacos , Humanos , Células K562 , Células KB , Masculino , Camundongos , Camundongos Endogâmicos BALB C , Camundongos Endogâmicos ICR , Distribuição Aleatória , Células VeroRESUMO
OBJECTIVE: To study the actions of transcription factors, T-bet and GATA-3, and their relevant signal transduction pathways on the immune-related pathogenesis with chronic aplastic anemia (CAA), and to investigate the immunological regulation mechanism of Shengxue Mixture (SXM) in regulating levels of Th cell imbalance, transcriptional factor and relevant signal pathways. METHODS: All CAA patients selected from Yueyang Hospital of Shanghai University of traditional Chinese medicine were equally randomized into the treated group and the control group, 20 patients in each group, and 20 healthy persons were selected as normal group, the former was treated with SXM according to patients' syndrome patterns, namely, SXM-1 was given to patients of Pi-Shen yang-deficiency pattern, and SXM-2 to those of Pi-Shen yin-deficiency pattern. Patients in the control group were treated with cyclosporin A (CsA). The mRNA expressions of T-bet, GATA-3, signal transducers and activators of transcription 4 (STAT4) and 6 (STAT6) in peripheral blood mononuclear cell (PBMNC) of patients were determined using real-time fluorescent quantitation polymerase chain reaction before and after treatment, meantime, the Th1/Th2 proportion in peripheral blood, and levels of IFN-gamma, IL-12 and IL-4 in PBMNC-cultured supernatant were detected by flow cytometry and enzyme linked immunosorbent assay. RESULTS: The mRNA expressions of PBMNC T-bet and STAT4, ratios of T-bet/GATA-3, Th1 proportion and Th1/Th2 ratio, levels of IFN-gamma and IL-12 in PBMNC-cultured supernatant were all significantly higher in CAA patients than in healthy controls (P < 0.01), which were lowered after treatment but didn't reach the normal range (all P < 0.01), excepting for IL-12 level. Comparisons of the changes between the two treated groups showed insignificant difference (P > 0.05). While the difference between patients and healthy persons in terms of GATA-3, STAT6, Th2 proportion, and IL-4 were insignificant (P > 0.05), either before or after treatment. CONCLUSIONS: Abnormal activation of IFN-gamma/T-bet and IL-12/ STAT4 pathways, as well as Th1/Th2 balance deviating to Th1 excursion play vital roles in the immunological pathogenesis of CAA. SXM and CsA could lower the aforesaid abnormal activation and correct Th1 hyper-polarization, so as to alleviate the over-activated cell-mediated immunity to eliminate hematopoietic depression in CAA patients.
Assuntos
Anemia Aplástica/tratamento farmacológico , Anemia Aplástica/metabolismo , Diagnóstico Diferencial , Medicamentos de Ervas Chinesas/uso terapêutico , Fitoterapia , Adolescente , Adulto , Idoso , Idoso de 80 Anos ou mais , Anemia Aplástica/imunologia , Criança , Doença Crônica , Citocinas/metabolismo , Feminino , Fator de Transcrição GATA3/genética , Fator de Transcrição GATA3/metabolismo , Humanos , Masculino , Medicina Tradicional Chinesa , Pessoa de Meia-Idade , RNA Mensageiro/genética , RNA Mensageiro/metabolismo , Transdução de Sinais , Proteínas com Domínio T/genética , Proteínas com Domínio T/metabolismo , Equilíbrio Th1-Th2 , Adulto JovemRESUMO
ETHNOPHARMACOLOGICAL RELEVANCE: Laggera alata, as a traditional Chinese herbal medicine, has been widely used to ameliorate some ailments associated with inflammation including hepatitis in folk. AIM OF THE STUDY: Based on anti-inflammatory activity of total phenolics from Laggera alata (TPLA), to further validate the remarkable curative effect Laggera alata in hepatitis, hepatoprotective effect of TPLA was examined. MATERIALS AND METHODS: TPLA was prepared and its principle components were quantificationally analyzed. The hepatoprotective effects of TPLA were studied using a CCl(4)-induced injury model in primary cultured neonatal rat hepatocytes, and a CCl(4)-induced acute and chronic damage model in vivo. RESULTS: TPLA significantly reduced cellular leakage of hepatocyte aspartate aminotransferase (AST) and alanine aminotransferase (ALT) and improved cell viability in vitro. TPLA markedly decreased the serum AST and ALT levels of the mice, the levels of AST, ALT, total protein, albumin, and sialic acid in rat serum, and the hydroxyproline level in rat liver. Meanwhile, severe hepatic lesions induced by CCl(4) in mice/rats were remarkably improved by the administration of TPLA. CONCLUSIONS: This investigation verifies the hepatoprotective effect of TPLA in vitro/in vivo and clarifies its active components dicaffeoylquinic acids responsible for hepatoprotective potential.
Assuntos
Asteraceae/química , Doença Hepática Induzida por Substâncias e Drogas/tratamento farmacológico , Hepatócitos/efeitos dos fármacos , Fitoterapia , Extratos Vegetais/uso terapêutico , Ácido Quínico/análogos & derivados , Alanina Transaminase/sangue , Animais , Aspartato Aminotransferases/sangue , Proteínas Sanguíneas/efeitos dos fármacos , Tetracloreto de Carbono , Sobrevivência Celular/efeitos dos fármacos , Modelos Animais de Doenças , Avaliação Pré-Clínica de Medicamentos , Medicamentos de Ervas Chinesas/uso terapêutico , Hepatócitos/metabolismo , Hepatócitos/patologia , Hidroxiprolina/metabolismo , Masculino , Camundongos , Camundongos Endogâmicos ICR , Ácido N-Acetilneuramínico/sangue , Extratos Vegetais/química , Ratos , Ratos Sprague-Dawley , Albumina Sérica/efeitos dos fármacosRESUMO
A new dibenzofuran named 1,2,4-trimethyl-7,8-dimethoxy-dibenzofuran (1), together with seven known compounds, euparin (2), 2,5-diacetyl-6-hydroxy-benzofuran (3), 2-acetyl-5,6-dimethoxy-benzofuran (4), gummosogenin (5), lupeol (6), stigmasterol (7) and (E)-2,5-dihydroxy-cinnamic acid (8), were isolated from the roots of Ligularia caloxantha, a Chinese medicinal plant. The structures of the compounds were elucidated by spectroscopic methods.
Assuntos
Asteraceae/química , Benzofuranos/isolamento & purificação , Medicamentos de Ervas Chinesas/química , Benzofuranos/química , Estrutura Molecular , Raízes de Plantas/químicaRESUMO
OBJECTIVE: Adopting methods of cell culture to explore the effects and mechanisms of Jianpi Bushen Huoxue Prescription (JPBSHXP), a traditional Chinese compound herbal medicine for strengthening spleen, reinforcing kidney and activating blood circulation, in inhibiting hematopoietic cells apoptosis in a mouse model of aplastic anemia (AA). METHODS: Blood serum of AA mice was made from an AA mouse model. Blood serums containing different traditional Chinese compound herbal medicine were made from rats after intragastric administration of JPBSHXP and its related decoctions, respectively. Bone marrow cells of normal mice were incubated by these blood serums for 24 hours, respectively. The apoptosis of the bone marrow cells were assayed by flow cytometry and transmission electron microscopy (TEM). RESULTS: It was indicated that the bone marrow cells of normal mice incubated with blood serum of AA mice displayed typical apoptosis. The apoptosis rates of bone marrow cells of the AA mice incubated by blood serum containing different traditional Chinese herbal medicine were decreased. The effect of Bushen (reinforcing kidey) Recipe was better than Jianpi (strengthening spleen) Recipe and Huoxue (activating blood circulation) Recipe, while the effect of JPBSHXP was the best. TEM results showed that the effect of Bushen Recipe was better than that of the Jianpi Recipe and the Huoxue Recipe, while the effect of JPBSHXP was the best. CONCLUSION: JPBSHXP and its related decoctions can significantly decrease the apoptosis rate of bone marrow mononuclear cells of the AA mice. It is inferred that JPBSHXP can promote bone marrow hematogenesis.
Assuntos
Anemia Aplástica/tratamento farmacológico , Apoptose/efeitos dos fármacos , Células da Medula Óssea/patologia , Medicamentos de Ervas Chinesas/farmacologia , Células-Tronco Hematopoéticas/patologia , Anemia Aplástica/imunologia , Anemia Aplástica/patologia , Animais , Feminino , Masculino , Camundongos , Camundongos Endogâmicos BALB C , Camundongos Endogâmicos DBA , Ratos , Ratos Sprague-DawleyRESUMO
With the fast development of medicinal animals as new drugs, research on Periplaneta americana become hot recently. Several drugs which mainly consisted of P. americana were approved for clinical applications. The chemical constituents and pharmacological bioactivities of this insect were summarized herein, which provides informativon for further researches on this medicinal animal.
Assuntos
Antineoplásicos/farmacologia , Materia Medica/farmacologia , Periplaneta/química , Aminoácidos/isolamento & purificação , Aminoácidos/farmacologia , Animais , Antibacterianos/farmacologia , Cardiotônicos/farmacologia , Cicloparafinas/isolamento & purificação , Cicloparafinas/farmacologia , Materia Medica/isolamento & purificação , Estrutura Molecular , Neuropeptídeos/isolamento & purificação , Neuropeptídeos/farmacologiaRESUMO
OBJECTIVE: To observe the clinical effect of Shengxueling (SXL) on idiopathic thrombocytopenic purpura (ITP), and study the possible mechanism. METHODS: Eighty-six cases of ITP were randomly divided into two groups. The SXL group, 56 patients treated with SXL, a traditinal Chinese medicine and 30 patients administered with prednisone were taken as control. Each group took drugs for 3 months and was under follow-up observation. RESULTS: In the SXL group, the total effective rate was 85.71%, similar to prednisone 83.33% (P > 0.05) for 3 months, but the total effective rate of SXL (91.07%) were obviously better than that of the control group (53.33%) (P < 0.01) for 6 months and had no obvious adverse reaction. The patients bleeding was alleviated or stopped, the general condition was improved. At the same time, blood platelet count (PLT) was increased, platelet associated immunoglobulin (PAIg) and interleukin-4 (IL-4) were markedly dropped, the level of natural killers cells activity (NKa) increased, the rate of T lymphocyte subsets gradually returned to normal level. Megakaryocyte tended to maturation on bone marrow smear after treatment. All differences above were statistically significant. CONCLUSION: SXL is an effective and safe medicine for ITP. Its mechanism could regulate cytoimmune, inhibit platelet antibody to reduce the destruction of platelet, increase the number of platelet, promote the division and maturation of megakaryocyte, facilitate the production and release of platelet, lower the fragility of capillary, prevent and cure hemorrhagic tendency.
Assuntos
Medicina Tradicional Chinesa , Fitoterapia , Preparações de Plantas/uso terapêutico , Púrpura Trombocitopênica Idiopática/terapia , Adolescente , Adulto , Plaquetas/metabolismo , Medula Óssea/patologia , Feminino , Glucocorticoides/uso terapêutico , Hemorragia/etiologia , Hemorragia/fisiopatologia , Humanos , Imunoglobulinas/sangue , Interleucina-4/sangue , Células Matadoras Naturais/patologia , Contagem de Linfócitos , Masculino , Pessoa de Meia-Idade , Fitoterapia/efeitos adversos , Preparações de Plantas/efeitos adversos , Contagem de Plaquetas , Prednisona/uso terapêutico , Púrpura Trombocitopênica Idiopática/sangue , Púrpura Trombocitopênica Idiopática/complicações , Púrpura Trombocitopênica Idiopática/patologia , Subpopulações de Linfócitos T/patologia , Resultado do TratamentoRESUMO
OBJECTIVE: To observe the clinical effect of Shengxueling Granule (SXLG) in treating idiopathic thrombocytopenic purpura (ITP), and to study its possible mechanism. METHODS: Eighty-six cases of ITP were divided into two groups randomly. Fifty-six cases in the treatment group were treated with SXLG, a traditional Chinese medicine, and 30 cases administered with Western medicine (prednisone) were taken as control. Patients in each group took drugs for three months and were under follow-up observation. RESULTS: In SXLG-treated group, the total effective rate in 3 months was 85.71%, similar to 83.33% in prednisone-treated group (P>0.05), while the total effective rate in 6 months in the SXLG-treated group was 91.07%, higher than 53.33% of the prednisone-treated group (P<0.01), and no obvious side-effects were observed. The patients' bleeding was alleviated or stopped, and their general condition was improved. And the blood platelet count (BPC) was increased, the platelet associated immunoglobulin (PAIg) and interleukin-4 (IL-4) were markedly dropped, the level of natural killer cells activity (NKCA) increased, and the rate of T lymphocyte subsets gradually returned to normal level. Megakaryocytes tended toward maturation on bone marrow smear after SXLG treatment. All differences above were statistically significant. CONCLUSION: SXLG is an effective and safe medicine for ITP. It can regulate the cellular immunity, inhibit the platelet antibody to reduce the destruction of the platelet and to increase the number of platelet, promote the differentiation and maturation of megakaryocyte, facilitate the production and release of platelet, lower the fragility of capillary, and prevent the hemorrhagic tendency.
Assuntos
Medicamentos de Ervas Chinesas/uso terapêutico , Púrpura Trombocitopênica Idiopática/tratamento farmacológico , Adolescente , Adulto , Plaquetas/efeitos dos fármacos , Plaquetas/metabolismo , Criança , Feminino , Humanos , Imunoglobulinas/efeitos dos fármacos , Imunoglobulinas/metabolismo , Interleucina-4/metabolismo , Células Matadoras Naturais/efeitos dos fármacos , Células Matadoras Naturais/metabolismo , Masculino , Medicina Tradicional Chinesa , Pessoa de Meia-Idade , Fitoterapia , Preparações de Plantas/uso terapêutico , Prednisona/uso terapêutico , Linfócitos T/efeitos dos fármacos , Linfócitos T/metabolismo , Resultado do TratamentoRESUMO
According to TCM theory of the wholistic concept and the principles of syndrome differentiation and treatment, the characteristics of the pathogenesis of aplastic anemia (AA) were summarized and corresponding treatment was put forward on the basis of clinical observation and the study of literature. In the pathogenesis of AA, the deficiency of spleen and kidney is the primary aspect, fire attacking blood vessels is the secondary aspect and there is change because of blood stasis. In treatment, the method of invigorating spleen and tonifying kidney is adopted in order to get at the root, and releasing fire to stop bleeding is adopted in order to bring about a temporary solution, and activating blood circulation to dissipate blood stasis is adopted in order to produce blood. The outline should be caught hold of that consumption is primary aspect and fire is secondary aspect and there is change because of blood stasis in order to obtain satisfactory curative effect.