RESUMO
The use of light-assisted cathode is regarded as an effective approach to reduce the overpotential of lithium carbon dioxide (Li - CO2) batteries. However, the inefficient electron-hole separation and the complex discharge-charge reactions hamper the efficiency of CO2 photocatalytic reaction in battery. Herein, a highly reversible force-assisted Li - CO2 battery has been established for the first time by employing a Bi0.5Na0.5TiO3 nanorods piezoelectric cathode. The high-energy electron and holes generated by the piezoelectric cathode with ultrasonic force can effectively enhance the carbon dioxide reduction reaction (CDRR) and carbon dioxide evolution reaction (CDER) kinetics, thereby reducing the overpotentials during the discharge-charge processes. Moreover, the morphology of the discharge product (Li2CO3) can be modified via the dense surface electrons of the piezoelectric cathode, resulting in the promoted decomposition kinetics of Li2CO3 in charging progress. Thus, the force-assisted Li - CO2 battery with the unique piezoelectric cathode can adjust the output and input energy by ultrasonic wave, and provides an ultra-low charging platform of 3.52 V, and exhibits excellent cycle stability (a charging platform of 3.42 V after 100 h cycles). The investigation of the force-assisted process described herein provides significant insights to solve overpotential in the Li - CO2 batteries system.
RESUMO
At present, photoassisted Li-air batteries are considered to be an effective approach to overcome the sluggish reaction kinetics of the Li-air batteries. And, the organic liquid electrolyte is generally adopted by the current conventional photoassisted Li-air batteries. However, the superior catalytic activity of photoassisted cathode would in turn fasten the degradation of the organic liquid electrolyte, leading to limited battery cycling life. Herein, we tame the above limitation of the traditional liquid electrolyte system for Li-CO2 batteries by constructing a photoassisted all-solid-state Li-CO2 battery with an integrated bilayer Au@TiO2/Li1.5Al0.5Ge1.5(PO4)3 (LAGP)/LAGP (ATLL) framework, which can essentially improve battery stability. Taking advantage of photoelectric and photothermal effects, the Au@TiO2/LAGP layer enables the acceleration of the slow kinetics of the carbon dioxide reduction reaction and evolution reaction processes. The LAGP layer could resolve the problem of liquid electrolyte decomposition under illumination. The integrated double-layer LAGP framework endows the direct transportation of heat and Li+ in the entire system. The photoassisted all-solid-state Li-CO2 battery achieves an ultralow polarization of 0.25 V with illumination, as well as a high round-trip efficiency of 92.4%. Even at an extremely low temperature of -73 °C, the battery can still deliver a small polarization of 0.6 V by converting solar energy into heat to achieve self-heating. This study is not limited to the Li-air batteries but can also be applied to other battery systems, constituting a significant step toward the practical application of all-solid-state photoassisted Li-air batteries.
RESUMO
Bone marrow mesenchymal stem cells (BMSCs) are a kind of pluripotent stem cells derived from bone marrows, which can not only support hematopoiesis, but also have capabilities of multidifferentiation, high-proliferation and self-renewing. They have become one of hotspots in stem cell studies. Studies on in vitro intervention with BMSCs with TCMs have made remarkable progress in recent years. According to the findings, some traditional Chinese medicines can promote proliferation of BMSCs, some can inhibit the apoptosis of BMSCs, while others can induce BMSCs to differentiate into multiple cell types, such as osteoblast. Furthermore, some studies also involved relevant action mechanisms. The authors summarized the advance in relevant studies by reference to relevant literatures of this field.
Assuntos
Apoptose/efeitos dos fármacos , Células da Medula Óssea/citologia , Diferenciação Celular/efeitos dos fármacos , Medicina Tradicional Chinesa/métodos , Células-Tronco Mesenquimais/citologia , Células-Tronco Mesenquimais/efeitos dos fármacos , Animais , Proliferação de Células/efeitos dos fármacos , HumanosRESUMO
A new piperidine alkaloid and three known tetranortriterpenoids were isolated from the methanol extracts of the rhizomes of Arisaema decipiens Schott (Araceae) and their chemical structures were identified as (-)-(2R*,3S*,6S*)-N,2-dimethyl-3-hydroxy-6-(9-phenylnonyl) piperidine (1), 6-deacetylnimbin (2), 28-deoxonimbolide (3) and nimbin (4). The N-methylated derivative (1a) of 1 was synthesized. Compound 1 exhibited weak inhibitory activity against the MCF-7 cell line, while compound 1a showed potential inhibitory activity against the MCF-7 cell line with an IC50 value of 4.6 µM and weak inhibitory activity against K562 and SK-OV-3 cells. This plant in genus Arisaema is firstly reported as the source of limonoids that are considered a natural antitumor herbal medicine.
Assuntos
Antineoplásicos/química , Antineoplásicos/farmacologia , Arisaema/química , Medicamentos de Ervas Chinesas/química , Medicamentos de Ervas Chinesas/farmacologia , Limoninas/análise , Limoninas/química , Piperidinas/síntese química , Piperidinas/farmacologia , Alcaloides/química , Alcaloides/isolamento & purificação , Alcaloides/farmacologia , Antineoplásicos/síntese química , Antineoplásicos/isolamento & purificação , Neoplasias da Mama/tratamento farmacológico , Neoplasias da Mama/patologia , Linhagem Celular Tumoral , Ensaios de Seleção de Medicamentos Antitumorais , Etnicidade , Feminino , Humanos , Limoninas/síntese química , Limoninas/isolamento & purificação , Limoninas/farmacologia , Imageamento por Ressonância Magnética , Neoplasias Ovarianas/tratamento farmacológico , Neoplasias Ovarianas/patologia , Piperidinas/química , Piperidinas/isolamento & purificação , Rizoma/químicaRESUMO
Promoting human embryonic stem cell (hESC)-derived-neural progenitor survival in the pro-apoptotic niche is pivotal for stem cell replacement therapy. The present study was designed to investigate the protective effect of hepatocyte growth factor (HGF) on hESC-derived neural progenitor injured by hydrogen peroxide (H(2)O(2)) exposure. Treatment of hESC-derived neural progenitor cells with HGF prior to H(2)O(2) exposure conferred protective effect against oxidative stress-induced apoptosis. HGF treatment increased both phosphoinositide 3-kinase (PI3K)/Akt and extracellular signal-regulated kinase1/2 (ERK1/2) phosphorylation. However, selective inhibition of each pathway supported that the activation of PI3K/AKT, but not ERK1/2, provides survival advantage to the neural progenitor cells. Further investigation indicated that HGF pretreatment could attenuate the decrease of the expression of Bcl-2 protein induced by H(2)O(2), whereas the level of Bax was not affected. Additionally, we observed that H(2)O(2)-induced decrease of mitochondrial transmembrane potential, release of cytochrome c and increase of caspase-3 activation were alleviated by HGF pretreatment. These effects of HGF could be reversed by inhibition of the PI3K/Akt and ERKs pathways, indicating PI3K/Akt and ERKs signaling might be involved in HGF-mediated regulation of mitochondrial apoptotic pathway mediated by H(2)O(2). The neuroprotective effect of HGF might potentially be useful in stem cell-based therapies for neurodegenerative disorders.
Assuntos
Apoptose/efeitos dos fármacos , Células-Tronco Embrionárias/efeitos dos fármacos , Fator de Crescimento de Hepatócito/farmacologia , Peróxido de Hidrogênio/farmacologia , Células-Tronco Neurais/efeitos dos fármacos , Fármacos Neuroprotetores/farmacologia , Caspase 3/metabolismo , Células Cultivadas , Citocromos c/metabolismo , Células-Tronco Embrionárias/citologia , Humanos , Potencial da Membrana Mitocondrial/efeitos dos fármacos , Proteína Quinase 1 Ativada por Mitógeno/metabolismo , Proteína Quinase 3 Ativada por Mitógeno/metabolismo , Células-Tronco Neurais/citologia , Estresse Oxidativo/efeitos dos fármacos , Fosfatidilinositol 3-Quinases/fisiologia , Fosforilação , Proteínas Proto-Oncogênicas c-akt/fisiologia , Proteínas Proto-Oncogênicas c-bcl-2/metabolismoRESUMO
The range of vertebrates that serve as intermediate hosts for parasites in the genus Sarcocystis remains incompletely defined. Here, we provide the first report of infections in treeshrews, describe the morphology of encysted parasites using light and transmission electron microscopy, and place this agent within a phylogenetic context by sequencing and comparing its 18S ribosomal DNA to that of related parasites. Muscle infections were diagnosed in four of 45 wild treeshrews captured in the vicinity of Kunming, Yunnan Province, Mainland China. Thread-like cysts (10.773+/-2.411mm in length, 0.106+/-0.009mm in width) had walls (0.538-0.746microm thick) that lacked perpendicular protrusions. The interior of the cyst was packed full with cyst merozoites, the shape of which was typical of Sarcocystis. The primary cyst wall consisted of a thin membrane supported by osmiophilic material, 31-60nm in thickness. The ground substance was about 105-526nm thickness. Cysts conformed to typical of 'type 1' sarcocysts. Freshly examined and frozen specimens did not differ in their cyst wall structure, however, the appearance of bradyzoites did differ: the conoid, rhoptries and micronemes were all visible in fresh bradyzoites; in stored bradyzoites, by contrast, the rhoptries appeared smaller, and although the conoid was visible, the micronemes were not. 18S rRNA gene was distinct from any previously reported sequence in GenBank. Their genetic and morphological uniformity suggest that these parasites, derived from treeshrews, represent a single biological species, Sarcocystis tupaia, sp. nov.
Assuntos
Interações Hospedeiro-Parasita , Sarcocystis/classificação , Sarcocystis/fisiologia , Sarcocistose/veterinária , Tupaia/parasitologia , Animais , China , DNA de Protozoário/análise , DNA Ribossômico/análise , Feminino , Genes de RNAr , Masculino , Dados de Sequência Molecular , Músculos/parasitologia , Filogenia , RNA Ribossômico 18S/genética , Sarcocystis/genética , Sarcocystis/isolamento & purificação , Sarcocistose/parasitologia , Análise de Sequência de DNA , Especificidade da EspécieRESUMO
Three new humulane-type sesquiterpenes, 8-O-(p-coumaroyl)-5beta-hydroperoxy-1(10)E,4(15)-humuladien-8alpha-ol (1), 8-O-(3-nitro-p-coumaroyl)-1(10)E,4(15)-humuladien-5beta,8alpha-diol (2) and 8-O-(p-coumaroyl)-1(10)E,4(5)E-humuladien-8-ol (3), and a new copaborneol derivative, 1-O-p-coumaroyl-copaborneol (4), have been isolated from the methanol extract of Pileacavaleriei Lévl. subsp. crenata C. J. Chen. Their structures were elucidated using spectroscopic methods. Cytotoxic and antimicrobial activities of the isolated compounds were evaluated.
Assuntos
Antibacterianos/química , Antineoplásicos Fitogênicos/química , Sesquiterpenos/química , Urticaceae/química , Antibacterianos/isolamento & purificação , Antibacterianos/farmacologia , Antineoplásicos Fitogênicos/isolamento & purificação , Antineoplásicos Fitogênicos/farmacologia , Linhagem Celular Tumoral , Ensaios de Seleção de Medicamentos Antitumorais , Humanos , Testes de Sensibilidade Microbiana , Conformação Molecular , Extratos Vegetais/química , Sesquiterpenos/isolamento & purificação , Sesquiterpenos/farmacologiaRESUMO
Bioassay-directed fractionation of the leaves of the medicinal plant Isodon xerophilus led to the isolation of a series of potential antitumor molecules. Thirteen new (1-13) and 23 (14-36) known diterpenoids were isolated and identified, representing ent-kauranoids of several structural types. The structures of 1-13 were determined by means of spectroscopic studies. The absolute configurations of the new compounds were clarified by CD spectroscopic studies or were postulated on biogenetic grounds. All compounds obtained were evaluated for their cytotoxic activity against the K562, MKN45, and HepG2 cell lines. Compounds 1, 2, 11, 16-19, 23, 26-28, 30, and 32 demonstrated significant cytotoxic activity for one or more cell lines.
Assuntos
Antineoplásicos Fitogênicos , Diterpenos do Tipo Caurano , Medicamentos de Ervas Chinesas , Isodon/química , Plantas Medicinais/química , Antineoplásicos Fitogênicos/química , Antineoplásicos Fitogênicos/isolamento & purificação , Antineoplásicos Fitogênicos/farmacologia , Diterpenos do Tipo Caurano/química , Diterpenos do Tipo Caurano/isolamento & purificação , Diterpenos do Tipo Caurano/farmacologia , Ensaios de Seleção de Medicamentos Antitumorais , Medicamentos de Ervas Chinesas/química , Medicamentos de Ervas Chinesas/isolamento & purificação , Medicamentos de Ervas Chinesas/farmacologia , Humanos , Estrutura Molecular , Ressonância Magnética Nuclear Biomolecular , Folhas de Planta/químicaRESUMO
Isodon xerophilus has been used as a herbal cold tea for the prevention and treatment of sore throat and inflammation in southernwestern China. A phytochemical study on the ethyl acetate (EtOAc) soluble fraction of I. xerophilus leaves led to the isolation of two new ent-kauranoids, xerophinoids A (1) and B (2), together with 14 known diterpenoids. The structures of xerophinoids A (1) and B (2) were illustrated using spectroscopic methods including 1D and 2D NMR analyses. To study their biological activities, the effects of xerophinoids A (1) and B (2) on nitrite production, tumor necrosis factor (TNF)-alpha and interleukin (IL)-1beta were examined. In addition, xerophinoids A (1) and B (2) also exhibited potent cytotoxicity against several human tumor cell lines (IC50 < 11 microM), but they had no toxicity on human T-lymphocyte (C8166).
Assuntos
Diterpenos do Tipo Caurano/isolamento & purificação , Isodon/química , Folhas de Planta/química , Animais , Antineoplásicos Fitogênicos/farmacologia , Morte Celular/efeitos dos fármacos , Linhagem Celular Tumoral , Diterpenos do Tipo Caurano/química , Diterpenos do Tipo Caurano/farmacologia , Humanos , Modelos Moleculares , Estrutura Molecular , RatosRESUMO
Two new compounds, rubescensins Q and R (1 and 2), and a new acetonide derivative (3) of lasiodonin, together with thirteen known analogues, oridonin (4), ponicidin (5), wikstroemioidin B (6), lasiodonin (7), lasiokaurin (8), enmenol (9), 1-O-beta-D-glucopyranosyl-enmenol (10), trichokaurin (11), the acetonide of maoyecrystal F (12), rabdoternins A-D (13-16), have been isolated from Isodon rubescens var. taihangensis. The structures of the new compounds were elucidated on the basis of spectroscopic methods, especially the 2D NMR spectral analysis. Compound 3 exhibited cytotoxicity against K562, Bcap37, CA, CNE, BIU87, BGC823, and HeLa cell lines.
Assuntos
Antineoplásicos Fitogênicos/isolamento & purificação , Diterpenos do Tipo Caurano/isolamento & purificação , Isodon/química , Antineoplásicos Fitogênicos/química , Antineoplásicos Fitogênicos/farmacologia , Diterpenos do Tipo Caurano/química , Diterpenos do Tipo Caurano/farmacologia , Humanos , Espectroscopia de Ressonância Magnética , ProibitinasRESUMO
AIM: To study the biochemistry of lanthanides, the cooperative action of inorganic and organic anti-tumor drugs. METHODS: A series of rare earth complexes were synthesized with Ln(NO3) 6H2O, Phen and 5-Fu. Their anti-tumor activity was measured by the improved MTT, SRB methods. RESULTS: The formula of complex Ln[(Phen)2(5-Fu)3(NO3)](NO3)2(Ln = Y, La, Ce, Sm, Gd, Dy, Er; Phen = 1, 10-phenanthroline; 5-Fu = fluorouracil) was characterized by elemental analyses, molar conductivity, IR, TGA, and 13C NMR spectra. The preliminary biological activity studies indicated that Lanthanide complex has strong anti-tumor activity in vitro. CONCLUSION: The complex might have anti-tumor cooperation action.
Assuntos
Antineoplásicos/síntese química , Proliferação de Células/efeitos dos fármacos , Elementos da Série dos Lantanídeos/química , Antineoplásicos/química , Antineoplásicos/farmacologia , Linhagem Celular Tumoral , Cério/química , Sinergismo Farmacológico , Disprósio/química , Érbio/química , Fluoruracila/química , Gadolínio/química , Humanos , Lantânio/química , Fenantrolinas/química , Samário/química , Relação Estrutura-Atividade , Ítrio/químicaRESUMO
Maoecrystal V (1), a novel C(19) diterpenoid possessing a unique 6,7-seco-6-nor-15(8-->9)-abeo-5,8-epoxy-ent-kaurane skeleton, was isolated from the leaves of a Chinese medicinal herb, Isodon eriocalyx. Its structure was determined by comprehensive NMR and MS spectroscopic analysis and confirmed by single-crystal X-ray diffraction study. Compound 1 showed remarkable inhibitory activity toward HeLa cells with IC(50) = 0.02 microg/mL (cis-platin: IC(50) = 0.99 microg/mL).
Assuntos
Diterpenos/química , Isodon/química , Cristalografia por Raios X , Diterpenos/isolamento & purificação , Diterpenos/farmacologia , Ensaios de Seleção de Medicamentos Antitumorais , Células HeLa , Humanos , Espectroscopia de Ressonância Magnética , Espectrometria de Massas , Modelos MolecularesRESUMO
BACKGROUND & OBJECTIVE: It had been reported that nuclear factor kappa b (NF kappa B) was associated with in vitro angiogenesis, but its role in angiogenesis of human ovarian carcinoma (HOC) had not been reported yet. The objective of this paper was to investigate the role and the mechanism of NF kappa B in HOC angiogenesis in chick chorioallantcic membrane (CAM). METHODS: The HOC TYK cells were implanted into 10-day CAM by 1 x 10(9)/per egg to establish the HOC CAM model. (1) With 20 eggs, the levels of NF kappa B, integrin alpha V beta 3, basic fibroblast growth factor (bFGF) at 0 h, 6 h, 12 h, 24 h, 48 h, 72 h time point after cells implanted were determined with ELISA. (2) The relationship among NF kappa B, bFGF,alpha V beta 3 and the effect of them on HOC angiogenesis in CAM were determined. Another 80 eggs were divided into 6 groups, normal saline (NS) (control group, 16 eggs), anti- NF kappa B (A group, 16 eggs), anti-bFGF (B group, 16 eggs), anti-NF kappa B + anti-bFGF(D group, 8 eggs) were added respectively into CAM at 6h time point after the cells implanted, and then anti-integrin alpha V beta 3 (C group, 16 eggs), anti-NF kappa B +anti-alpha V beta 3 (E group, 8 eggs) antibodies were added at 12h time point. Eight eggs from NS, A, B, C groups were taken out to determine the levels of NF kappa B, alpha V beta 3, bFGF at 48 h after the antibodies were added. The other eggs were incubated up to 5 days, and the vessel area/area were determined with image analysis. RESULTS: (1)The levels of NF kappa B and bFGF increased significantly at 6h, and that of V beta 3 increase significantly at 12 h time point after implantation (P< 0.01) (0.185+/-0.01, 0.771+/-0.16, 0.231+/-0.02), the peaks of the three levels were reached at 48 h (P< 0.01) (0.337+/-0.01, 1.639+/-0.01, 0.349+/-0.01). The levels of bFGF was significantly higher than those of NF kappa B and alpha V beta 3 at each time point (P< 0.01), but there were no significant difference between NF kappa B and alpha V beta 3 (P >0.05). (2)The levels of NF kappa B,bFGF, and alpha V beta 3 in A and B groups were significantly lower than those of NS group (P< 0.01) (0.098+/-0.02, 0.156+/-0.02, 0.329+/-0.01; 1.106+/-0.33, 0.412+/-0.01, 1.591+/-0.13; 0.138+/-0.03, 0.114+/-0.02, 0.322+/-0.01). And the level of alpha V beta 3 in C group were significantly reduced compared with those of NS group (P< 0.01) (0.119+/-0.02, 0.322+/-0.01), while the levels of NF kappa B and bFGF had no change between the two groups (P>0.05). The VA/A of the five groups of A, B, C, D, and E were significantly lower than that of NS group (P< 0.05) (26.10+/-13.71, 34.12+/-4.85, 25.50+/-11.41,14.32+/-3.11, 24.36+/-4.95, 66.62+/-17.64), and that of D group were significantly reduced compared with A group (P< 0.05) (14.32+/-3.11, 26.10+/-13.71), but there were no significant difference among the four groups of A, B, C, and E (P >0.05). CONCLUSIONS: NF kappa B can stimulate the angiogenesis of ovarian carcinoma with bFGF by upregulating the expression of alpha V beta 3, bFGF, which can be used as a marker of angiogenesis and a therapy target molecule of ovarian carcinoma.
Assuntos
NF-kappa B/metabolismo , Neovascularização Patológica/metabolismo , Neoplasias Ovarianas/metabolismo , Animais , Linhagem Celular Tumoral , Embrião de Galinha , Membrana Corioalantoide/irrigação sanguínea , Feminino , Fator 2 de Crescimento de Fibroblastos/metabolismo , Humanos , Integrina alfaVbeta3/metabolismo , Neoplasias Ovarianas/patologiaRESUMO
Five new ent-kauranoids, xindongnins C - G ( 1 - 5), together with five known ones, xindongnins A and B ( 6 and 7), melissoidesin G ( 8), dawoensin A ( 9), and glabcensin V ( 10), were isolated from the leaves of Isodon rubescens var. rubescens, and structurally elucidated. Compounds 1, 4, and 6 - 10 showed inhibitory effects against human tumor K562 cells with IC (50) values ranging from 0.3 to 7.3 microg/mL. The structure of 6 was revised on the basis of its 2D-NMR spectral data.
Assuntos
Antineoplásicos Fitogênicos/farmacologia , Diterpenos do Tipo Caurano/farmacologia , Isodon , Fitoterapia , Extratos Vegetais/farmacologia , Antineoplásicos Fitogênicos/administração & dosagem , Antineoplásicos Fitogênicos/uso terapêutico , Diterpenos do Tipo Caurano/administração & dosagem , Diterpenos do Tipo Caurano/química , Diterpenos do Tipo Caurano/uso terapêutico , Humanos , Concentração Inibidora 50 , Células K562/efeitos dos fármacos , Extratos Vegetais/administração & dosagem , Extratos Vegetais/química , Extratos Vegetais/uso terapêutico , Folhas de PlantaRESUMO
Four new ent-kaurane diterpenoids lushanrubescensins F-I (1-4), together with 11 known ones, lasiodonin (5), oridonin (6), ponicidin (7), isodonoiol (8), isodonal (9), rabdosin B (10), rabdoternins A and B (11 and 12), enmenol (13), epinodosin (14), and inflexusin (15), were isolated from Isodon rubescens var. lushanensis, and the structures were elucidated by spectroscopic analysis. The inhibitory effect against the K562, Bcap37, BGC823, BIU87, CA, CNE, and Hela cell lines of compounds 3 and 5-10 were evaluated.
Assuntos
Diterpenos do Tipo Caurano/química , Diterpenos do Tipo Caurano/farmacologia , Diterpenos/química , Diterpenos/farmacologia , Isodon , Linhagem Celular Tumoral , Diterpenos/isolamento & purificação , Diterpenos do Tipo Caurano/isolamento & purificação , Células HeLa , Humanos , Células K562 , ProibitinasRESUMO
Five new ent-kaurane diterpenoids, enanderianins K-O (1-5), and one new ent-abietane diterpenoid, enanderianin P (6), together with five known ent-kaurane diterpenoids, rabdocoetsin A (7), rabdocoetsin B (8), rabdocoetsin D (9), megathyrin A (10), megathyrin B (11) were isolated from the aerial parts of Isodon enanderianus. Their structures were determined by spectral means. Some diterpenoids were tested for their cytotoxicity against the human tumor K562 cells. Compounds 1, 2, 6, 8, 9 showed significant inhibitory activities against K562 cells with IC50 values ranging from 0.13 to 0.87 microg/mL.
Assuntos
Antineoplásicos Fitogênicos/farmacologia , Diterpenos/farmacologia , Isodon , Fitoterapia , Extratos Vegetais/farmacologia , Antineoplásicos Fitogênicos/química , Diterpenos/química , Humanos , Concentração Inibidora 50 , Células K562/efeitos dos fármacos , Componentes Aéreos da Planta , Extratos Vegetais/químicaRESUMO
Four new ent-kaurane diterpenoids, sculponeatins F-I (1-4), together with six known compounds, sculponeatin E (5), epi-nodosin (6), epi-nodosinol (7), enmein (8), and macrocalyxoformins A and B (9 and 10), were isolated from the leaves of Isodon sculponeata. Also obtained were ursolic acid, 2alpha,3beta-dihydroxy-urs-12-en-28-oic acid, 2alpha,3beta,19alpha-trihydroxy-urs-12-en-28-oic acid, beta-sitosterol, daucosterol, quercetin, pedalitin, rosmarinic acid, caffeic acid and ethyl caffeic acid. Their structures were determined by spectral methods (1D-, 2D-NMR and MS). Some diterpenoids were tested for their cytotoxicity to inhibit three kinds of human tumor cells K562, A549 and T24. Compounds 3, 4, 6, 8, and 10 showed significant inhibitory effect toward K562 with IC(50) values ranging from 3.2 microg/ml to 8.2 microg/ml, while 3 and 6 exhibited potent antitumor activity against T24, but none exhibited cytotoxicity toward the cells of A549.
Assuntos
Antineoplásicos Fitogênicos/farmacologia , Diterpenos/farmacologia , Isodon , Fitoterapia , Antineoplásicos Fitogênicos/química , Diterpenos/química , Ensaios de Seleção de Medicamentos Antitumorais , Humanos , Concentração Inibidora 50 , Espectroscopia de Ressonância Magnética , Espectrometria de Massas , Folhas de Planta , Células Tumorais Cultivadas/efeitos dos fármacosRESUMO
Eleven new diterpenoids, adenanthins B-L (1-11), together with five known analogues, calcicolin B (12), adenanthin (13), weisiensin A (14), nervosanin (15), and forrestin C (16), were isolated from the aerial parts of Isodon adenantha. The structures of 1-11 were elucidated on the basis of spectral methods, as well as the X-ray crystallographic analysis of 11. Compounds 2, 5, and 14 showed significant inhibitory activities against K562 cells, with IC(50) values less than 4.0 microg/mL, respectively.
Assuntos
Diterpenos/isolamento & purificação , Plantas Medicinais/química , Diterpenos/química , Diterpenos/farmacologia , Ensaios de Seleção de Medicamentos Antitumorais , Humanos , Concentração Inibidora 50 , Leucemia , Medicina Tradicional do Leste Asiático , Conformação Molecular , Estrutura Molecular , Ressonância Magnética Nuclear Biomolecular , Tomografia Computadorizada por Raios X , Células Tumorais Cultivadas/efeitos dos fármacosRESUMO
Three new ent-kaurane diterpenoids laxiflorin E (1), laxiflorin H (6) and laxiflorin I (8) were isolated from the leaves of Isodon eriocalyx var. laxiflora, along with nine known diterpenoids, eriocalyxin A (2), laxiflorin C (3), laxiflorin D (4), laxiflorin A (5), maoecrystal S (7), maoecrystal Q (9), eriocalyxin B (10), maoecrystal C (11) and enmelol (12). The structures of the new compounds were determined by spectroscopic methods. Compounds 1-5 are 6,7-seco-ent-kaurane-7,20-olide diterpenoids, and 6-12 belong to 7,20-epoxy-ent-kauranoids. The spectral data of enmelol (12) are reported here for the first time. Ten of these compounds were tested for their cytotoxicity toward K562 and T24 human tumor cells. Compounds 1, 3 and 10 showed significant inhibitory effects on K562 cells with IC50 values 0.077, 0.569 and 0.373 microg/mL, and compounds 1 and 10 also demonstrated significant inhibitory activities toward T24 cells with IC50 values 0.709 and 0.087 microg/mL. Compounds 8 and 11 also displayed inhibitory effect on both two kinds of cells with IC 50 value less than 6.5 microg/mL.
Assuntos
Antineoplásicos Fitogênicos/farmacologia , Diterpenos/farmacologia , Lamiaceae , Antineoplásicos Fitogênicos/química , Antineoplásicos Fitogênicos/isolamento & purificação , Divisão Celular/efeitos dos fármacos , Diterpenos/química , Diterpenos/isolamento & purificação , Humanos , Concentração Inibidora 50 , Células K562 , Espectroscopia de Ressonância Magnética , Células Tumorais CultivadasRESUMO
Eight new abietane diterpenoids, coleon U 11-acetate (1), 16-acetoxycoleon U 11-acetate (2), and xanthanthusins F-K (3-8), together with five known analogues, coleon U (9), 16-O-acetylcoleon C (10), coleon U-quinone (11), 8alpha,9alpha-epoxycoleon U-quinone (12), and xanthanthusin E (13), were isolated from the aerial parts of Coleus xanthanthus. The structures of 1-8 were elucidated on the basis of spectral methods. Compounds 1, 5, and 11-13 were evaluated for their cytotoxicity against K562 human leukemia cells.