RESUMO
Qing Dai (Naturalis Indigo) is a traditional Chinese medicine (TCM) used as a topical agent in moderate psoriasis, targeting interleukin-17 (IL-17). In this study, it was prepared from the aerial parts of Strobilanthes cusia. Three undescribed indole alkaloid derivatives, indigodoles A-C, along with seven known compounds were isolated from this preparation of Qing Dai and their structures were elucidated from spectroscopic data, including NMR, MS, UV, IR, optical rotation, and CD. As well, most compounds were tested against IL-17. Indigodole C and tryptanthrin could significantly inhibit IL-17 production of Th17 cells. In addition, indigodole A and indirubin showed notably anti-IL-17 gene expression in dose-dependent effects without cytotoxicities toward Th17 and Jurkat cells, respectively. Overall, our studies indicate that the aforementioned indole alkaloids could contribute to anti-IL 17 properties of Qing Dai.
Assuntos
Acanthaceae/química , Medicamentos de Ervas Chinesas/química , Alcaloides Indólicos/química , Alcaloides Indólicos/farmacologia , Interleucina-17/antagonistas & inibidores , Medicina Tradicional Chinesa , Componentes Aéreos da Planta/química , Animais , Interleucina-17/biossíntese , Camundongos , Modelos Moleculares , Conformação Molecular , Células Th17/efeitos dos fármacos , Células Th17/metabolismoRESUMO
The aim of this work is to establish an optimal process for generating liposomal berberine and assessing its anticancer ability against human hepatic carcinoma in a murine xenograft model. Of various forms of liposomal berberine with different lipid compositions, preparation by various methods, the one that contained 5 mol% polyethenyl glycol (PEG) that was produced by a thin-film hydration/extrusion method exhibited the highest encapsulation efficiency (E.E.) of berberine (14%). Additionally, in vitro studies reveal that this batch of liposomal berberine inhibited the growth of HepG2 cells 2.5 times as effectively as berberine solution since the half maximal inhibitory concentration (IC(50)) of berberine solution was 4.23 µg berberine/mL while that of liposomal berberine was only 1.67 µg berberine/mL, and this inhibition effect was based on the induction of apoptosis through the caspase/mitochondria-dependent pathway. Additionally, the results of in vivo studies indicate that the liposome effectively reduced the rate of elimination of berberine in both plasma and tissues, and liposomal berberine effectively reduced the size and weight of tumors as compared with the untreated tumor control group. Therefore, this work demonstrates that liposome is a good carrier for berberine to inhibit the tumor growth in HepG2 tumor-bearing mice.
Assuntos
Antineoplásicos Fitogênicos/farmacologia , Berberina/farmacologia , Carcinoma Hepatocelular/tratamento farmacológico , Neoplasias Hepáticas/tratamento farmacológico , Animais , Antineoplásicos Fitogênicos/administração & dosagem , Apoptose/efeitos dos fármacos , Berberina/administração & dosagem , Carcinoma Hepatocelular/patologia , Caspases/metabolismo , Excipientes/química , Células Hep G2 , Humanos , Concentração Inibidora 50 , Lipossomos , Neoplasias Hepáticas/patologia , Masculino , Camundongos , Camundongos Nus , Mitocôndrias/metabolismo , Polietilenoglicóis/química , Ensaios Antitumorais Modelo de XenoenxertoRESUMO
The objective of this study is to investigate the nano-fabrication method for ginseng extract powders (GEPs) and detect the differences in physical and chemical properties, and cytotoxicity of GEPs before and after fabrication. White ginseng was used as the raw material to produce the GEPs (Sample A). After grinding, the GEPs passed a 40-mesh sieve (particle size < 105 microm) and was named as Sample B. The residue (particle size > 105 microm) was named as Sample C. Samples A and B were used for nanofabrication though the use of a high-energy ball mill. Sample B was ground for 3 hr (Sample D) and 1 hr (Sample E), while Sample A was ground for 3 hr (Sample F) and 1 hr (Sample G). Nanoparticles of GEPs with ranges of 300 nm approximately 1 microm and 500 nm approximately 3 microm were produced. The heavy metal content (As, Cd, Co, Cu, Fe, Hg, Mn, Ni, Pb, Se and W) of Samples A-G were all under the maximum residue limit. Sample C contained a higher amount of yellow crystal material and had the highest ginsenoside contents and antioxidant capacity. There were enrichments of ginsenosides (approximately 1.3 fold) and antioxidant capacities (approximately 1.6 fold) in Sample C compared to Sample A. Moreover, after nano-fabrication, the antioxidant capacity was not changed significantly. However, the cellular growth enhancement ability was increased significantly. Samples F and G had the higher cellular growth enhancement ability and improved the cellular growth of L929 cells about 1.3 times as compared to Sample A. In future studies, Sample C will be used for nanofabrication in order to enhance the curative efficiency of ginseng.
Assuntos
Composição de Medicamentos/métodos , Nanoestruturas/química , Nanoestruturas/ultraestrutura , Nanotecnologia/métodos , Panax/química , Extratos Vegetais/química , Teste de Materiais , Tamanho da Partícula , PósRESUMO
AIM OF THE STUDY: Traditional Chinese medicine herbs (TCMHs) are used in medicines as well as in daily dietary supplements in Asia. In this study, we employed pNF-kappaB-Luc or pIFN-gamma-Luc and BALB/c mice peritoneal macrophages or splenocytes to investigate both the immune and inflammatory effects of six selected plant species. MATERIALS AND METHODS: Specifically, we used ethyl acetate fractions of Astragalus membranaceus (Fisch.) Bunge var. mongholicus (Bunge) Hsiao (Fabaceae) (AM), Andrographis paniculata (Burm. f.) Nees (Acanthaceae) (AP), Angelica sinensis (Oliv.) Diels (Apiaceae) (AS), Eucommia ulmodes Oliv. (Eucommiaceae) leaves (EU leaves), Isatis indigotica Fort. (Brassicaceae) (II) and Morus alba L. (Moraceae) (MA). RESULTS: We found that ethyl acetate fractions of AP, AS and MA significantly decreased NF-kappaB luciferase activity and also the secretion of NO and PGE(2) in LPS/IFN-gamma stimulated mouse peritoneal macrophages (p<0.05). In contrast, they did not affect IFN-gamma luciferase activity or IFN-gamma production in concanavalin A (Con A)-activated mouse splenocytes. Our results indicated that the anti-inflammatory properties of these plant extracts might be resulted from the inhibition of pro-inflammatory mediators (e.g., NO and PGE(2)), at least in part via suppression of a signaling pathway such as NF-kappaB. CONCLUSIONS: Collectively, we have found that three potent bioactive TCMH species exerted significant NF-kappaB inhibitory activity and acted in a cell type dependent fashion.
Assuntos
Anti-Inflamatórios/farmacologia , Dinoprostona/biossíntese , Fatores Imunológicos/farmacologia , Macrófagos Peritoneais/efeitos dos fármacos , Magnoliopsida , Óxido Nítrico/biossíntese , Extratos Vegetais/farmacologia , Andrographis , Angelica sinensis , Animais , Feminino , Interferon gama/metabolismo , Interleucina-6/metabolismo , Luciferases/metabolismo , Macrófagos Peritoneais/metabolismo , Camundongos , Camundongos Endogâmicos BALB C , Mitógenos , Morus , NF-kappa B/metabolismo , Extratos Vegetais/efeitos adversos , Baço/metabolismo , Fator de Necrose Tumoral alfa/metabolismoRESUMO
The neuroprotective effect of schizandrin on the glutamate (Glu)-induced neuronal excitotoxicity and its potential mechanisms were investigated using primary cultures of rat cortical cells. After exposure of primary cultures of rat cortical cells to 10 microM Glu for 24 h, cortical cell cultures exhibited remarkable apoptotic death. Pretreatment of the cortical cell cultures with schizandrin (10, 100 microM) for 2 h significantly protected cortical neurons against Glu-induced excitotoxicity. The neuroprotective activity of schizandrin was the most potent at the concentration of 100 microM. Schizandrin reduced apoptotic characteristics by DAPI staining in Glu-injured cortical cell cultures. In addition, schizandrin diminished the intracellular Ca2+ influx, inhibited the subsequent overproduction of nitric oxide (NO), reactive oxygen species (ROS), and cytochrome c, and preserved the mitochondrial membrane potential. Furthermore, schizandrin also increased the cellular level of glutathione (GSH) and inhibited the membrane lipid peroxidation malondialdehyde (MDA). As indicated by Western blotting, schizandrin attenuated the protein level changes of procaspase-9, caspase-9, and caspase-3 and cleaved poly(ADP-ribose) polymerase (PARP). Taken together, these results suggest that schizandrin protected primary cultures of rat cortical cells against Glu-induced apoptosis through a mitochondria-mediated pathway and oxidative stress.
Assuntos
Córtex Cerebral/efeitos dos fármacos , Ciclo-Octanos/farmacologia , Ácido Glutâmico/toxicidade , Lignanas/farmacologia , Neurônios/efeitos dos fármacos , Fármacos Neuroprotetores/farmacologia , Compostos Policíclicos/farmacologia , Animais , Apoptose/efeitos dos fármacos , Cálcio/metabolismo , Caspases/metabolismo , Células Cultivadas , Córtex Cerebral/embriologia , Córtex Cerebral/enzimologia , Córtex Cerebral/patologia , Citocromos c/metabolismo , Maleato de Dizocilpina/farmacologia , Relação Dose-Resposta a Droga , Antagonistas de Aminoácidos Excitatórios/farmacologia , Glutationa/metabolismo , Peroxidação de Lipídeos/efeitos dos fármacos , Potencial da Membrana Mitocondrial/efeitos dos fármacos , Mitocôndrias/efeitos dos fármacos , Neurônios/enzimologia , Neurônios/patologia , Óxido Nítrico/metabolismo , Estresse Oxidativo/efeitos dos fármacos , Poli(ADP-Ribose) Polimerases/metabolismo , Ratos , Espécies Reativas de Oxigênio/metabolismoRESUMO
BACKGROUND: Dry eye is a very common ocular disease characterized by eye dryness and photophobia. It often influences the patient's normal life. This study evaluated the therapeutic effects of the Chinese herb, Chi-Ju-Di-Huang-Wan, for treatment of dry eye patients. It is one of the most commonly prescribed Chinese herbs used for eyes, however, there are no scientific reports about its effect. METHODS: This study included 80 dry eye patients. The patients were randomly divided into two groups. The experimental group was treated with topical eye drops and Chi-Ju-Di-Huan-Wan. The control group was given topical eye drops and placebo. All patients received tear film examinations including Schirmer's test, Rose Bengal test, fluorescein stain test, break up time test and questionnaires. RESULTS: The results of the tear film tests were analysed by two independent t-tests between the two groups. No significant differences between the two groups according to the Schirmer's test were found. There was a significant difference in the Rose Bengal test at week 2 and tear break up time at week 4 (p = 0.04, 0.04, individually). CONCLUSION: Chi-Ju-Di-Huang-Wan is an effective stabilizer of tear film and decreases the abnormality of corneal epithelium. It provides an alternative choice for dry eye treatment.