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1.
China Journal of Chinese Materia Medica ; (24): 3913-3921, 2023.
Artículo en Chino | WPRIM | ID: wpr-981524

RESUMEN

The present study aimed to investigate the inhibitory effect and mechanism of Isodon terricolous-medicated serum on lipopolysaccharide(LPS)-induced hepatic stellate cell(HSC) activation. LPS-induced HSCs were divided into a blank control group, an LPS model group, a colchicine-medicated serum group, an LPS + blank serum group, an I. terricolous-medicated serum group, a Toll-like receptor 4(TLR4) blocker group, and a TLR4 blocker + I. terricolous-medicated serum group. HSC proliferation was detected by methyl thiazolyl tetrazolium(MTT) assay. Enzyme-linked immunosorbent assay(ELISA) was used to measure type Ⅰ collagen(COL Ⅰ), COL Ⅲ, transforming growth factor-β1(TGF-β1), intercellular adhesion molecule-1(ICAM-1), α-smooth muscle actin(α-SMA), vascular cell adhesion molecule-1(VCAM-1), cysteinyl aspartate-specific proteinase-1(caspase-1), and monocyte chemotactic protein-1(MCP-1). Real-time PCR(RT-PCR) was used to detect mRNA expression of TLR4, IκBα, and NOD-like receptor thermal protein domain associated protein 3(NLRP3), nuclear factor-κB(NF-κB) p65, gasdermin D(GSDMD), and apoptosis-associated speck-like protein containing a CARD(ASC) in HSCs. Western blot(WB) was used to detect the protein levels of TLR4, p-IκBα, NF-κB p65, NLRP3, ASC, and GSDMD in HSCs. The results showed that I. terricolous-medicated serum could inhibit the proliferation activity of HSCs and inhibit the secretion of COL Ⅰ, COL Ⅲ, α-SMA, TGF-β1, caspase-1, MCP-1, VCAM-1, and ICAM-1 in HSCs. Compared with the LPS model group, the I. terricolous-medicated serum group, the colchicine-medicated serum group, and the TLR4 blocker group showed down-regulated expression of p-IκBα, NLRP3, NF-κB p65, GSDMD, and ASC, and up-regulated expression of IκBα. Compared with the TLR4 blocker group, the TLR4 blocker + I. terricolous-medicated serum group showed decreased expression of TLR4, p-IκBα, NLRP3, NF-κB p65, GSDMD, and ASC, and increased expression of IκBα. In conclusion, I. terricolous-medicated serum down-regulates HSC activation by inhibiting the TLR4/NF-κB/NLRP3 signaling pathway.


Asunto(s)
FN-kappa B/metabolismo , Células Estrelladas Hepáticas , Factor de Crecimiento Transformador beta1/metabolismo , Inhibidor NF-kappaB alfa/metabolismo , Molécula 1 de Adhesión Intercelular/metabolismo , Isodon , Proteína con Dominio Pirina 3 de la Familia NLR/metabolismo , Receptor Toll-Like 4/metabolismo , Molécula 1 de Adhesión Celular Vascular/metabolismo , Lipopolisacáridos/farmacología , Transducción de Señal , Colchicina/farmacología , Caspasas
2.
China Journal of Chinese Materia Medica ; (24): 433-436, 2022.
Artículo en Chino | WPRIM | ID: wpr-927986

RESUMEN

The genus Rabdosia is famous for the abundance of diverse and novel ent-kaurane diterpenoids. However, only a few ent-kauranoids have been discovered from R. flexicaulis since the investigation on its chemical constituents is not systematic. To find novel bioactive diterpenoids, the ethyl acetate extract of the above ground part of R. flexicaulis in Daofu County, Sichuan Province was obtained by column chromatography. One new compound and five known ones were identified as flexicaulin E(1), forrestin B(2), inf-lexarabdonin D(3), 7α-hydroxydehydroabietic acid(4), 15-hydroxydehydroabietic acid(5), and pomiferin F(6) by spectral techniques. Compounds 1-3 were the ent-kaurane diterpenoids isolated from this species for the first time. Compounds 4-6, aromatic abie-tanoids, were isolated from the genus Rabdosia for the first time.


Asunto(s)
Diterpenos , Diterpenos de Tipo Kaurano , Isodon/química , Estructura Molecular , Extractos Vegetales/química
3.
China Journal of Chinese Materia Medica ; (24): 319-323, 2019.
Artículo en Chino | WPRIM | ID: wpr-774602

RESUMEN

The chemical constituents of the water extraction of the aerial parts of Isodon henryi were investigated by various chromatographic methods including D-101 macroporous adsorptive resins,silica gel,sephadex LH-20,and semi-preparative HPLC. As a result,ten compounds were separated and purified. By analyses of the UV,IR,MS,NMR spectra,their structures were determined as rabdosinate( 1),lasiokaurin( 2),epinodosinol( 3),rabdosichuanin C( 4),epinodosin( 5),hebeirubescensin k( 6),rubescensin C( 7),enmenol( 8),oridonin( 9),and enmenol-1-β-glucoside( 10). Compounds 1-8 and 10 were isolated from I. henryi for the first time. Compounds 2 and 9 showed inhibitory effects against four tumor cells,with IC50 values of 2. 25-9. 32 μmol·L-1.


Asunto(s)
Isodon , Química , Espectroscopía de Resonancia Magnética , Estructura Molecular , Fitoquímicos , Componentes Aéreos de las Plantas , Química , Extractos Vegetales , Química
4.
Chinese Journal of Natural Medicines (English Ed.) ; (6): 456-464, 2018.
Artículo en Inglés | WPRIM | ID: wpr-812385

RESUMEN

Nine new ent-kaurane diterpenoids, named scopariusols L-T (1-9), were isolated from the aerial parts of Isodon scoparius. Their structures were characterized mainly by analyzing the NMR and HR-ESI-MS data, and the absolute configuration of 1 was determined by single-crystal X-ray diffraction. Compound 1 was active against five human tumor cell lines (HL-60, SMMC-7721, A-549, MCF-7, and SW-480), and it also inhibited NO production in LPS-stimulated RAW264.7 cells, with an IC value of 0.6 μmol·L.


Asunto(s)
Animales , Humanos , Ratones , Antineoplásicos Fitogénicos , Química , Farmacología , Línea Celular Tumoral , Cristalografía por Rayos X , Diterpenos de Tipo Kaurano , Química , Farmacología , Ensayos de Selección de Medicamentos Antitumorales , Medicamentos Herbarios Chinos , Química , Farmacología , Células HL-60 , Isodon , Química , Lipopolisacáridos , Farmacología , Macrófagos , Estructura Molecular , Óxido Nítrico , Resonancia Magnética Nuclear Biomolecular , Componentes Aéreos de las Plantas , Química
5.
Chinese Journal of Natural Medicines (English Ed.) ; (6): 456-464, 2018.
Artículo en Inglés | WPRIM | ID: wpr-773596

RESUMEN

Nine new ent-kaurane diterpenoids, named scopariusols L-T (1-9), were isolated from the aerial parts of Isodon scoparius. Their structures were characterized mainly by analyzing the NMR and HR-ESI-MS data, and the absolute configuration of 1 was determined by single-crystal X-ray diffraction. Compound 1 was active against five human tumor cell lines (HL-60, SMMC-7721, A-549, MCF-7, and SW-480), and it also inhibited NO production in LPS-stimulated RAW264.7 cells, with an IC value of 0.6 μmol·L.


Asunto(s)
Animales , Humanos , Ratones , Antineoplásicos Fitogénicos , Química , Farmacología , Línea Celular Tumoral , Cristalografía por Rayos X , Diterpenos de Tipo Kaurano , Química , Farmacología , Ensayos de Selección de Medicamentos Antitumorales , Medicamentos Herbarios Chinos , Química , Farmacología , Células HL-60 , Isodon , Química , Lipopolisacáridos , Farmacología , Macrófagos , Estructura Molecular , Óxido Nítrico , Resonancia Magnética Nuclear Biomolecular , Componentes Aéreos de las Plantas , Química
6.
Bol. latinoam. Caribe plantas med. aromát ; 15(1): 29-40, ene. 2016. ilus, graf, tab
Artículo en Inglés | LILACS | ID: biblio-907515

RESUMEN

Pedalitin, isolated from the aerial part of Rabdosia japonica (Labiatae), inhibited soybean lipoxygenase-1 (EC 1.13.11.12, Type I) with an IC50 of 152.5 uM. The progress curves for an enzyme reaction, pedalitin inactivate the lipoxygenase-1 in a time dependent, irreversible manner, exhibiting kinetics with a kinact/KI of 59.6 +/- 10 mM-1min-1. In the pseudoperoxidase activity, pedalitin is very slowly oxidized by the soybean lipoxygenase-1 catalyzed decomposition of lipid hydroperoxides.


Pedalitina, aislada de las partes aereas de Rabdosia japonica inhibió a la lipooxigenasa-1 (EC 1.13.11.12 tipo I) con un IC50 de 152.5 uM. La curva de progreso para una acción enzimática, pedalitina inactivó a la lipooxigenasa-1 de una manera dependiente del tiempo, de una manera irreversible, exhibiendo una cinética con una kinact/KI de 59.6 +/- mM-1min-1. En la actividad pseudoperoxidasa, pedalitina es oxidada lentamente por la descomposición de la lípido hidroperóxido de la lipooxigenasa-1 de poroto de soya.


Asunto(s)
Flavonas/aislamiento & purificación , Flavonas/farmacología , Isodon/química , Inhibidores de la Lipooxigenasa/farmacología , Glycine max/enzimología , Cinética , Inhibidores de la Lipooxigenasa/aislamiento & purificación , Factores de Tiempo
7.
China Journal of Chinese Materia Medica ; (24): 1543-1547, 2015.
Artículo en Chino | WPRIM | ID: wpr-351311

RESUMEN

This research established an HPLC method for determination of six C-Glycoside flavones of warer-soluble total flavonoids from Isodon lophanthoides var. gerardianus (Benth.) H. Hara, and studied the antitumor activity of the warer-soluble total flavonoids. The HPLC system consisted of Kromasil 100-5 C18 (4.6 mm x 250 mm, 5 microm) column and a solution system of methanol, acetonitrile and 0.5% formic acid gradient elution at a flow rate of 0. 8 mL x min(-1) and the wavelength of detector was at 334 nm. The column temperature was 25 degrees C. The antitumor activity of water-soluble flavonoids was assayed using HepG2 cell as the tested cell. The linear ranges of vicenin II, vicenin III, isoschaftoside, schaftoside, vitexin, 6, 8-di-C-a-L-arabinosylapigenin were 0.25-2.53, 0.12-1.20, 0.37-3.69, 0.16-1.63, 0.19-1.92, 0.14-1.42 microg, respectively. The average recoveries (n = 6) were 99.6% (RSD 0.87%), 100.2% (RSD 2.0%), 99.6% (RSD 1.8%), 97.9% (RSD 1.5%), 98.8% (RSD 1.2%), 98.6% (RSD 1.2%), respectively. After exposure in 24, 48, 72 h, the total flavonoids showed inhibitory effect on the proliferation of HepG2 cells with IC50 as the evaluation index, the IC50 values of 1.89, 1.71, 1.51 g x L(-1), respectively. The method is quick, simple and accurate with good re- producibility, and can be used for determination of vicenin II, vicenin III, isoschaftoside, schaftoside, vitexin, 6, 8-di-C-a-L-arabino- sylapigenin in the warer-soluble total flavonoids from L lophanthoides var. gerardianus. The warer-soluble total flavonoids from L lophanthoides have inhibitory effect on the proliferation of HepG2 cells.


Asunto(s)
Humanos , Antineoplásicos Fitogénicos , Farmacología , Línea Celular Tumoral , Proliferación Celular , Cromatografía Líquida de Alta Presión , Medicamentos Herbarios Chinos , Farmacología , Flavonas , Farmacología , Isodon , Química , Monosacáridos , Farmacología
8.
Chinese Journal of Natural Medicines (English Ed.) ; (6): 767-775, 2015.
Artículo en Inglés | WPRIM | ID: wpr-812484

RESUMEN

The present study was designed to evaluate the protective effects of ethanol extracts of Rabdosia japonica var. glaucocalyx (Maxim.) Hara (RJ) on lipopolysaccharide (LPS)-induced acute lung injury (ALI) in mice and the possible underlying mechanisms of action. The mice were orally administrated with RJ extract (16, 32 or 64 mg(kg(-1)) daily for consecutive7 days before LPS challenge. The ung specimens and the bronchoalveolar lavage fluid (BALF) were collected for histopathological examinations and biochemical analyses. Pretreatment with RJ significantly enhanced superoxide dismutase (SOD) activity and reduced the wet-to-dry weight (W/D) ratio, the levels of nitric oxide (NO) and protein leakage, and myeloperoxidase (MPO) activity in mice with ALI, in a dose-dependent manner. RJ reduced complement deposition and significantly attenuated LPS-induced ALI by reducing productions of inflammatory mediators, such as tumor necrosis factor-α (TNF-α), interleukin-6 (IL-6), and interleukin-1β (IL-1β). The results demonstrated that RJ may attenuate LPS-induced ALI via reducing the production of pro-inflammatory mediators, and reducing complement deposition and radicals.


Asunto(s)
Animales , Masculino , Ratones , Lesión Pulmonar Aguda , Quimioterapia , Antiinflamatorios , Farmacología , Usos Terapéuticos , Antioxidantes , Metabolismo , Farmacología , Usos Terapéuticos , Proteínas del Sistema Complemento , Metabolismo , Mediadores de Inflamación , Metabolismo , Isodon , Química , Lipopolisacáridos , Pulmón , Metabolismo , Óxido Nítrico , Metabolismo , Peroxidasa , Metabolismo , Fitoterapia , Extractos Vegetales , Farmacología , Usos Terapéuticos , Superóxido Dismutasa , Metabolismo
9.
Chinese Journal of Natural Medicines (English Ed.) ; (6): 383-389, 2015.
Artículo en Inglés | WPRIM | ID: wpr-812531

RESUMEN

The present study was designed to determine the chemical constituents of EtOAc extracts of the aerial parts of Isodon wikstroemioides. Compounds 1-8 were isolated and purified by normal-phase silica gel and reversed-phase C18silica gel column chromatography and HPLC. Their structures were elucidated by extensive spectroscopic methods. Most of them were evaluated for their in vitro cytotoxicity against human cancer HL-60, SMMC-7721, A-549, MCF-7, and SW-480 cells and their inhibitory activity against nitric oxide (NO) production in LPS-activated RAW264.7 macrophages. Among the eight 11, 20-epoxy-ent-kauranoids isolated, compounds 1-6 (isowikstroemins H-M) were new diterpenoids. Compounds 1, 3, and 7 exhibited significant cytotoxicity with IC50 values ranging from (0.84 ± 0.02) to (4.09 ± 0.34) μmol · L(-1), while compounds 4 and 5 showed selective cytotoxicity. In addition, compounds 1, 3, 4, and 7 exhibited inhibitory activity against nitric oxide (NO) production in LPS-activated RAW264.7 macrophages. These results provide a basis for future development of these compounds as anti-cancer and anti-inflammatory agents.


Asunto(s)
Humanos , Antiinflamatorios , Antineoplásicos Fitogénicos , Línea Celular Tumoral , Diterpenos de Tipo Kaurano , Concentración 50 Inhibidora , Isodon , Química , Lipopolisacáridos , Farmacología , Macrófagos , Metabolismo , Neoplasias , Quimioterapia , Óxido Nítrico , Fitoterapia , Componentes Aéreos de las Plantas , Extractos Vegetales
10.
Biol. Res ; 47: 1-6, 2014. tab
Artículo en Inglés | LILACS | ID: biblio-950753

RESUMEN

BACKGROUND: Isodon rugosus is used traditionally in the management of hypertension, rheumatism, tooth-ache and pyrexia. Present study was arranged to investigate I. rugosus for phytoconstituents, phytotoxic and cytotoxic activities to explore its toxicological, pharmacological potentials and to rationalize its ethnomedicinal uses. Briefly, qualitative phytochemical analysis of the plant extracts were carried out for the existence of alkaloids, flavonoids, saponins, oils, glycosides, anthraquinones, terpenoids, sterols and tannins. Plant crude methanolic extract (Ir.Cr), its subsequent fractions; n-hexane (Ir.Hex), chloroform (Ir.Chf), ethyl acetate (Ir.EtAc), aqueous (Ir.Aq) and saponins (Ir.Sp) in different concentrations were tested for phytotoxic and cytotoxic activities using radish seeds and brine shrimps (Artemia salina) respectively. The phytotoxic activity was determined by percent root length inhibition (RLI) and percent seeds germination inhibition (SGI) while the cytotoxicity was obtained with percent lethality of the brine shrimps. RESULTS: Ir.Cr was tested positive for the presence of alkaloids, glycosides, flavonoids, oils, terpenoids, saponins, tannins and anthraquinones. Among different fractions Ir.Sp, Ir.Chf, Ir.EtAc, and Ir.Cr were most effective causing 93.55, 89.32, 81.32 and 58.68% inhibition of seeds in phytotoxicity assay, with IC50 values of 0.1, 0.1, 0.1 and 52 µg/ml respectively. Similarly, among all the tested samples, Ir.Sp exhibited the highest phytotoxic effect causing 91.33% root length inhibition with IC50 of 0.1 µg/ml. Ir.Sp and Ir.Chf were most effective against brine shrimps showing 92.23 and 76.67% lethality with LC50 values of 10 and 12 µg/ml respectively. CONCLUSIONS: It may be inferred from the current investigations that I. rugosus contains different secondary metabolites and is a potential source for the isolation of natural anticancer and herbicidal drug molecules. Different fractions exhibited phytotoxic and cytotoxic activities, thus providing pharmacological basis for ethnomedicinal uses of this plant.


Asunto(s)
Animales , Saponinas/análisis , Extractos Vegetales/farmacología , Isodon/química , Fitoterapia , Artemia/efectos de los fármacos , Taninos/análisis , Terpenos/análisis , Flavonoides/análisis , Aceites de Plantas/análisis , Cloroformo , Antraquinonas/análisis , Raíces de Plantas/crecimiento & desarrollo , Citotoxinas , Componentes Aéreos de las Plantas/química , Metanol , Alcaloides/análisis , Glicósidos/análisis , Hexanos
11.
Biol. Res ; 47: 1-10, 2014. graf, tab
Artículo en Inglés | LILACS | ID: biblio-950772

RESUMEN

BACKGROUND: Based on the ethnomedicinal uses and the effective outcomes of natural products in various diseases, this study was designed to evaluate Isodon rugosus as possible remedy in oxidative stress, alzheimer's and other neurodegenerative diseases. Acetylecholinestrase (AChE) and butyrylcholinesterase (BChE) inhibitory activities of crude methanolic extract (Ir.Cr), resultant fractions (n-hexane (Ir.Hex), chloroform (Ir.Cf), ethyl acetate (Ir.EtAc), aqueous (Ir.Aq)), flavonoids (Ir.Flv) and crude saponins (Ir.Sp) of I. rugosus were investigated using Ellman's spectrophotometric method. Antioxidant potential of I. rugosus was determined using DPPH, H2O2 and ABTS free radicals scavenging assays. Total phenolic and flavonoids contents of plant extracts were determined and expressed in mg GAE/g dry weight and mg RTE/g of dry sample respectively. RESULTS: Among different fractions Ir.Flv and Ir.Cf exhibited highest inhibitory activity against AChE (87.44 ± 0.51, 83.73 ± 0.64%) and BChE (82.53 ± 0.71, 88.55 ± 0.77%) enzymes at 1 mg/ml with IC50 values of 45, 50 for AChE and 40, 70 µg/ml for BChE respectively. Activity of these fractions were comparable to galanthamine causing 96.00 ± 0.30 and 88.61 ± 0.43% inhibition of AChE and BChE at 1 mg/ml concentration with IC50 values of 20 and 47 µg/ml respectively. In antioxidant assays, Ir.Flv, Ir.Cf, and Ir.EtAc demonstrated highest radicals scavenging activities in DPPH and H2O2 assays which were comparable to ascorbic acid. Ir.Flv was found most potent with IC50 of 19 and 24 µg/ml against DPPH and H2O2 radicals respectively. Whereas antioxidant activates of plant samples against ABTS free radicals was moderate. Ir.Cf, Ir.EtAc and Ir.Cr showed high phenolic and flavonoid contents and concentrations of these compounds in different fractions correlated well to their antioxidant and anticholinestrase activities. CONCLUSION: It may be inferred from the current investigations that the Ir.Sp, Ir.Flv and various fractions of I. rugosus are good sources of anticholinesterase and antioxidant compounds. Different fractions can be subjected to activity guided isolation of bioactive compounds effective in neurological disorders.


Asunto(s)
Saponinas/análisis , Flavonoides/análisis , Extractos Vegetales/química , Inhibidores de la Colinesterasa/análisis , Isodon/química , Antioxidantes/análisis , Picratos/metabolismo , Acetilcolinesterasa/efectos de los fármacos , Saponinas/aislamiento & purificación , Espectrofotometría/métodos , Ácidos Sulfónicos/metabolismo , Flavonoides/aislamiento & purificación , Compuestos de Bifenilo/metabolismo , Butirilcolinesterasa/efectos de los fármacos , Cloroformo , Depuradores de Radicales Libres/metabolismo , Estrés Oxidativo/efectos de los fármacos , Concentración 50 Inhibidora , Isodon/clasificación , Isodon/enzimología , Componentes Aéreos de las Plantas/química , Mezclas Complejas , Metanol , Benzotiazoles/metabolismo , Radicales Libres/análisis , Hexanos , Peróxido de Hidrógeno/metabolismo , Medicina Tradicional , Acetatos
12.
China Journal of Chinese Materia Medica ; (24): 4216-4221, 2014.
Artículo en Chino | WPRIM | ID: wpr-341881

RESUMEN

The seeds of Rabdosia rubescens were as the materials to research the impacts of different lead (Pb2+) concentrations(0, 135, 270, 540, 1 080 mg x L(-1)) on seed germination and seedling growth. The results show that: Low concentration of lead had no obvious effect on early germination of the seed, the germination vigor and germination speed were lightly higher but not significantly differed at the level of Pb concentration 135 mg x L(-1) with control group; Mid-high concentration of Pb solution (270-1 080 mg x L(-1)) significantly inhibited the seed germination and seedling growth, which reduced the seed germination rate, germination vigor, germination index, embryo root length and shoot length, growth index with increasing of Pb concentrations. There was a inhibitory effect on embryo shoot length and root length at mid-high lead concentrations stress, and stronger inhibitory effect on root , which was more sensitive than shoot to Pb stress(P < 0.05). Pb bioaccumulation coefficient (BC) was 0.76-2.59, increased with concentration of Pb; Pb enrichment in seedling mainly caused the growth inhibition. The fitting model predictive analyses show, the critical concentration of Pb, which causes the germination rate and biomass fresh weight reducing 10%, is 195.18, 101.65 mg x L(-1).


Asunto(s)
Germinación , Isodon , Plomo , Toxicidad , Plantones , Semillas , Estrés Fisiológico
13.
China Journal of Chinese Materia Medica ; (24): 2343-2347, 2013.
Artículo en Chino | WPRIM | ID: wpr-315028

RESUMEN

An HPLC method was developed for simultaneous quantitation of rosmarinic acid, oridonin and chrysoplenetin in the aerial parts of Isodon rubescens. Samples were analyzed on an Ultimate C18 column (4.6 mm x 250 mm, 5 microm) with methanol and water containing 0.1% formic acid as mobile phases in a linear gradient mode. The flow rate was 1.0 mL x min(-1) and the temperature was set at 30 degrees C. The PDA detector wavelengths were set at 338 nm for rosmarinic and chrysoplenetin and at 242 nm for oridonin. The linear ranges were 0.222-2.78, 0.227-2.84 and 0.005-0.071 microg for rosmarinic acid, oridonin and chrysoplenetin, respectively. The average recoveries of the three constituents were 102.9% (RSD 1.9%), 99.6% (RSD 1.1%) and 102.5% (RSD 0.94%), respectively. This method was proved to be accurate and repeatable, and can be used for quality control of the aerial parts of I. rubescens.


Asunto(s)
Cromatografía Líquida de Alta Presión , Métodos , Cinamatos , Depsidos , Diterpenos de Tipo Kaurano , Medicamentos Herbarios Chinos , Flavonoides , Isodon , Química , Extractos Vegetales , Plantas Medicinales , Química
14.
China Journal of Chinese Materia Medica ; (24): 199-203, 2013.
Artículo en Chino | WPRIM | ID: wpr-318693

RESUMEN

To study the chemical constituents of Rabdosia japonica var. glaucocalyx and their anti-complementary activity on the basis of preliminary studies. Target isolation guided by anti-complementary activity test, compounds in the chloroform and n-butanol fractions were isolated and purified by silica gel and Sephadex LH-20 column chromatographies, and preparative HPLC. The structures were identified by various spectroscopic data including ESI-MS, 1H-NMR and 13C-NMR data. The compounds were evaluated for anti-complementary activity in vitro. Eleven compounds were isolated from the chloroform and n-butanol soluble fractions and identified as stigmasterol (1), stigmas-9 (11) -en-3-ol (2), glaucocalyxin D (3), kamebakaurin (4), maslinic acid (5), corosolic acid (6), minheryins I (7), diosmetin (8), caffeic acid ethylene ester (9), caffeic acid (10) and vitexin (11). Isoquercetrin, rutin, quercetin, 3-methylquercetin, luteolin, 7-methylluteolin, and apigenin which were isolated from the preliminary studies together with compounds 9 and 10 showed inhibition of the complement system by the classical pathway. Compounds 2, 4, 6-9 and 11 were obtained from this plant for the first time. Caffeic acid (10) showed the strongest activity in vitro with a CH50 value of 0.041 g x L(-1).


Asunto(s)
Animales , Cricetinae , Femenino , Masculino , Antioxidantes , Farmacología , Ácidos Cafeicos , Farmacología , Cromatografía , Cromatografía Líquida de Alta Presión , Ensayo de Actividad Hemolítica de Complemento , Métodos , Inactivadores del Complemento , Química , Farmacología , Medicamentos Herbarios Chinos , Química , Eritrocitos , Ésteres , Etilenos , Farmacología , Isodon , Química , Espectroscopía de Resonancia Magnética , Componentes Aéreos de las Plantas , Química , Reguladores del Crecimiento de las Plantas , Farmacología , Ovinos , Espectrometría de Masa por Ionización de Electrospray
15.
Chinese Journal of Natural Medicines (English Ed.) ; (6): 43-47, 2012.
Artículo en Inglés | WPRIM | ID: wpr-812713

RESUMEN

AIM@#To study the chemical constituents in the flowers and fruits of Rabdosia excisa.@*METHODS@#The compounds were isolated and purified by silica gel column chromatography and their structures were identified by spectroscopic methods.@*RESULTS@#Sixteen compounds isolated from the flowers and fruits of this plant were identified as: stigm asterol (I), α-amyrin palmitate (II), ursolic acid (III), 2α, 3α, 19-trihydroxy-urs-12-en-28-oic acid (IV), 2α-hydroxyursolic acid (V), maslinic acid (VI), isodonal (VII), maoyecrystal E (VIII), kamebakaurin (XI), macrocalyxin G (X), epinodosinol (XI), rabdosichuanin C (XII), kamebacetal A (XIII), oridonin (XIV), enmenol-glucoside (XV), and lasiononin (XVI).@*CONCLUSION@#All the constituents were found in Rabdosia excisa for the first time, except constituents III, IX, XII and XIV.


Asunto(s)
Flores , Química , Frutas , Química , Isodon , Química , Estructura Molecular , Extractos Vegetales , Química
16.
China Journal of Chinese Materia Medica ; (24): 2203-2206, 2011.
Artículo en Chino | WPRIM | ID: wpr-283227

RESUMEN

<p><b>OBJECTIVE</b>To study the chemical constituents of aerial part of Rabdosia serra.</p><p><b>METHOD</b>The compounds were isolated by extraction, coloum chromatography over silica gel and ODS, and preparative HPLC. Their structures were identified by various spectroscopic methods including MS, IR, 1D and 2D NMR data.</p><p><b>RESULT</b>Six compounds were isolated from R. serra and were characterized as ent-1alpha, 7alpha, 14beta, 20-tetrahydroxy-11, 16-kauradien-15-one (1), kamebakaurin (2), dihydrokamebakaurin (3), rabdoinflexin A (4), daucosterol( 5), and beta-sitosterol (6).</p><p><b>CONCLUSION</b>Compound 1 is a new compound, and coumpound 3 was obtained from this plant for the first time.</p>


Asunto(s)
Isodon , Química
17.
Journal of Central South University(Medical Sciences) ; (12): 170-173, 2011.
Artículo en Chino | WPRIM | ID: wpr-814587

RESUMEN

OBJECTIVE@#To evaluate the clinical therapeutic effect of Rabdosia rubescens aqueous extract on chronic pharyngitis and its safety.@*METHODS@#One hundred and two patients suffered from chronic pharyngtis were randomly divided into an interventional group (n=51) and a placebo group (n=51). These volunteers were given 220 mL test materials once a day double-blindly for 30 days. All patients took routine physical examinations, and their throat symptom and pharynx signs were observed before and after the experiment.@*RESULTS@#After the patients had consumed Rabdosia rubescens aqueous extract and the placebo for 30 days, the improvement rates of main clinical symptom and signs in the interventional group were 67.31% and 61.54%, while those in placebo group were 19.23% and 11.54%, with significant difference (P0.05). But after 30 days, the integral of main clinical symptom and signs in the interventional group significantly decreased (P<0.05), compared with itself before the experiment and the placebo group.@*CONCLUSION@#Rabdosia rubescens aqueous extract is safe and effective for patients with chronic pharyngitis.


Asunto(s)
Adulto , Femenino , Humanos , Masculino , Persona de Mediana Edad , Enfermedad Crónica , Método Doble Ciego , Medicamentos Herbarios Chinos , Usos Terapéuticos , Isodon , Química , Faringitis , Quimioterapia , Fitoterapia
18.
China Journal of Chinese Materia Medica ; (24): 1772-1775, 2011.
Artículo en Chino | WPRIM | ID: wpr-354126

RESUMEN

<p><b>OBJECTIVE</b>To investigate the constituents of the stem of Rabdosia excisa.</p><p><b>METHOD</b>Compounds were separated and purified by silica gel column chromatography and their structures were determined by spectroscopic method.</p><p><b>RESULT</b>Thirteen compounds isolated from this plant were identified as rabdesimte( 1 ), maoyecrystal E (2), 6beta,11alpha,15alpha-trihydroxy-6,7-seco-6,20-epoxy-1alpha, 7-ol-ide-ent-kaur-16-en (3), enmenol-glucoside (4), oridonol (5), macrocalyxin G (6), rabdosichuanin C (7), beta-sitosterol (8), ursolic acid (9), 2alpha-hydroxyursolic acid (10), maslinic acid ( 11 ), 2alpha,3alpha,19-trihydroxy-urs-12-en-28-oicacid (12), and daucosterol (13).</p><p><b>CONCLUSION</b>Except for compounds 5, 8, 9 and 13, the remaining compounds were found in R. excisa for the first time.</p>


Asunto(s)
Diterpenos , Química , Isodon , Química , Extractos Vegetales , Química , Tallos de la Planta , Química , Plantas Medicinales , Química , Triterpenos , Química
19.
Chinese Journal of Biotechnology ; (12): 1218-1224, 2009.
Artículo en Chino | WPRIM | ID: wpr-296935

RESUMEN

Effects of Rabdocoetsin B (Rabd-B), a diterpenoid extracted from Isodon coetsa, on t(8;21) leukemic cells was tested by CCK-8 assay and Flow cytometry. The A549 cells stably expressing pGC-E1-ZU1-GFP were treated with Rabd-B for 4 h, and the accumulation of GFP was detected by fluorescence microscope. Using Western blotting, we investigated the expression of Casp-3, PARP, S6', which is a subunit of the 19S regulatory complex of the 26S proteasome, and cellular ubiqutinated proteins. We found that Rabd-B induced growth inhibition and apoptosis of Kasumi-1 cells in a dose-dependent manner. In Kasumi-1 cells treated with 2.5 micromol/L Rabd-B for 24 h, pro-caspase-3 was processed into its active form. The substrate of Casp-3, poly ADP-ribose polymerase (PARP), was cleaved with generation of an 85 kD fragment. The increased GFP fluorescence intensity, cleavage of S6' and the accumulation of ubiquitinated proteins were found in Kasumi-1 cells treated with Rabd-B. These results suggested that Rabd-B is a potential proteasome inhibitor which induces programmed cell death of t(8;21) cells. Further study might provide evidence for employing Rabd-B in treating human t(8;21) leukemia.


Asunto(s)
Humanos , Antineoplásicos Fitogénicos , Farmacología , Apoptosis , Caspasa 3 , Metabolismo , Línea Celular Tumoral , Diterpenos , Farmacología , Isodon , Química , Leucemia Mieloide Aguda , Patología , Inhibidores de Proteasoma , Translocación Genética , Ubiquitinas , Metabolismo
20.
Acta Pharmaceutica Sinica ; (12): 35-39, 2007.
Artículo en Chino | WPRIM | ID: wpr-281930

RESUMEN

To study the mechanism of downregulation of apoptosis by autophagy induced by oridonin in HeLa cells, the cell viability was measured by MTT method. DNA fragmentation was assayed by agarose gel electrophoresis. Autophagic and apoptotic ratio was determined by flowcytometric analysis. Protein expression was detected by Western blotting analysis. Oridonin induced both apoptosis and autophagy in HeLa cells. Apoptosis was upregulated by introduction of the inhibitor of autophagy, 3-methyladenine (3-MA). Addition of oridonin increased Bax/Bcl-2 expression ratio and cytochrome c, whereas the expression of SIRT-1 was decreased, and 3-MA pre-application enhanced these changes. Oridonin-induced autophagy antagonized apoptosis in HeLa cells through mitochondrial pathway.


Asunto(s)
Humanos , Antineoplásicos Fitogénicos , Farmacología , Apoptosis , Autofagia , Western Blotting , Citocromos c , Metabolismo , Diterpenos , Farmacología , Diterpenos de Tipo Kaurano , Farmacología , Citometría de Flujo , Células HeLa , Isodon , Química , Hojas de la Planta , Química , Plantas Medicinales , Química , Proteínas Proto-Oncogénicas c-bcl-2 , Metabolismo , Sirtuina 1 , Sirtuinas , Metabolismo , Proteína X Asociada a bcl-2 , Metabolismo
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