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1.
Bol. latinoam. Caribe plantas med. aromát ; 22(6): 864-878, nov. 2023. tab, graf
Article in English | LILACS | ID: biblio-1554462

ABSTRACT

Triterpenes are very important secondary metabolites with wide structural diversity and significant role in pharmacy and medicine. In the present research, a comparative study of pharamacological activities of the triterpene fractions obtained from several plant species belonging to Lamiaceae family, was carried out. In - vitro anti - proliferative activity was performed using a standard proliferation assay based on tetrazolium salts. In vitro anti - inflammatory activity of triterpene fractions was determined by an assay of inhibition of albumin denaturation. In general, the triterpene fractions obtained from plant species belonging to Lam iaceae family showed a strong anti - proliferative activity and anti - inflammatory activity. The triterpene fraction of Rosmarini folium showed the strongest anti - proliferative activity (GI 50 range from 4 to 37 µg/ml) and the strongest anti - inflammatory activ ity in the range from 57.27% to 80.69%. This comparative study provides scientific evidence to support the traditional use of Lamiacae plant species for medical purposes as anti - inflammatory and anti - proliferative medicines.


Los triterpenos son metabolitos secundarios muy importantes, con una amplia diversidad estructural y un rol significativo en la farmacia y la medicina. En esta investiga ción, se realizó un estudio comparativo de las actividades farmacológicas de las fracciones de triterpenos obtenidas de varias especies de plantas pertenecientes a la familia Lamiaceae. La actividad antiproliferativa in vitro se realizó mediante un ensayo estándar de proliferación basado en sales de tetrazolio. Se determinó la actividad antinflamatoria de las fracciones de triterpeno s mediante un ensayo de inhibición de desnaturalización de la albúmina. En general, las fracciones de triterpeno s obtenidas de las plantas pertenecientes a la familia Lamiaceae mostraron una actividad antiproliferativa y antinflamatoria fuerte. La fracción de triterpeno de Folium Rosmarini mostró la actividad antiproliferativa más fuerte (rango GI 50 entre 4 y 37 µg/m L ) y la más f uerte actividad antinflamatoria en el rango de 57,27% a 80,69%. Este estudio comparativo provée evidencia científica para apoyar el uso tradicional de especies de plantas Lamiaceae para usos médicos como medicinas antinflamatorios y antiproliferativas.


Subject(s)
Triterpenes/pharmacology , Plant Extracts/pharmacology , Lamiaceae/chemistry , Triterpenes/chemistry , Lamiaceae/metabolism , Anti-Inflammatory Agents
2.
Chinese Journal of Natural Medicines (English Ed.) ; (6): 599-609, 2023.
Article in English | WPRIM | ID: wpr-1010973

ABSTRACT

Gypenosides, structurally analogous to ginsenosides and derived from a sustainable source, are recognized as the principal active compounds found in Gynostemma pentaphyllum, a Chinese medicinal plant used in the treatment of the metabolic syndrome. By bioactive tracking isolation of the plants collected from different regions across China, we obtained four new gypenosides (1-4), together with nine known gypenosides (5-13), from the methanol extract of the plant. The structures of new gypenosides were elucidated by one-dimensional (1D) and two-dimensional (2D) nuclear magnetic resonance (NMR) spectra, complemented by chemical degradation experiments. Through comprehensive evaluation involving COL1A1 promoter assays and PP2Cα activity assays, we established a definitive structure-activity relationship for these dammarane-type triterpenoids, affirming the indispensability of the C-3 saccharide chain and C-17 lactone ring in effectively impeding extracellular matrix (ECM) deposition within hepatic stellate cells. Further in vivo study on the CCl4-induced liver damage mouse model corroborated that compound 5 significantly ameliorated the process of hepatic fibrosis by oral administration. These results underscore the potential of dammarane-type triterpenoids as prospective anti-fibrotic leads and highlight their prevalence as key molecular frameworks in the therapeutic intervention of chronic hepatic disorders.


Subject(s)
Animals , Mice , Gynostemma , Liver Cirrhosis/drug therapy , Triterpenes/pharmacology , Ginsenosides , Extracellular Matrix , Dammaranes
3.
Chinese Medical Journal ; (24): 1144-1154, 2023.
Article in English | WPRIM | ID: wpr-980900

ABSTRACT

Tumor chemoprevention and treatment are two approaches aimed at improving the survival of patients with cancers. An ideal anti-tumor drug is that which not only kills tumor cells but also alleviates tumor-causing risk factors, such as precancerous lesions, and prevents tumor recurrence. Chinese herbal monomers are considered to be ideal treatment agents due to their multi-target effects. Astragaloside has been shown to possess tumor chemoprevention, direct anti-tumor, and chemotherapeutic drug sensitization effects. In this paper, we review the effects of astragaloside on tumor prevention and treatment and provide directions for further research.


Subject(s)
Humans , Chemoprevention , Antineoplastic Agents , Neoplasms/prevention & control , Saponins/pharmacology , Triterpenes/pharmacology
4.
China Journal of Chinese Materia Medica ; (24): 6676-6681, 2023.
Article in Chinese | WPRIM | ID: wpr-1008865

ABSTRACT

Nine compounds were isolated from the 90% ethanol extract of Salacia polysperma by silica gel, Sephadex LH-20 column chromatography, together with preparative HPLC methods. Based on HR-ESI-MS, MS, 1D and 2D NMR spectral analyses, the structures of the nine compounds were identified as 28-hydroxy wilforlide B(1), wilforlide A(2), 1β,3β-dihydroxyurs-9(11),12-diene(3),(-)-epicatechin(4),(+)-catechin(5),(-)-4'-O-methyl-ent-galloepicatechin(6), 3-hydroxy-1-(4-hydroxy-3-methoxy-phenyl)propan-1-one(7),(-)-(7S,8R)-4-hydroxy-3,3',5'-trimethoxy-8',9'-dinor-8,4'-oxyneoligna-7,9-diol-7'-aldehyde(8), and vanillic acid(9). Compound 1 is a new oleanane-type triterpene lactone. Compounds 1, 3, 4, 7-9 were isolated from the Salacia genus for the first time. All compounds were assayed for their α-glucosidase inhibitory activity. The results suggested that compound 8 exhibited moderate α-glucosidase inhibitory activity, with an IC_(50) value of 37.2 μmol·L~(-1), and the other compounds showed no α-glucosidase inhibitory activity.


Subject(s)
Salacia/chemistry , alpha-Glucosidases , Triterpenes/pharmacology , Magnetic Resonance Spectroscopy , Ethanol , Molecular Structure
5.
China Journal of Chinese Materia Medica ; (24): 4834-4842, 2023.
Article in Chinese | WPRIM | ID: wpr-1008653

ABSTRACT

This study aims to investigate the effect and mechanism of total triterpenes of Euphorbium in treating rheumatoid arthritis(RA). The rat model of RA was established with Freund's complete adjuvant(FCA). Male rats were randomly assigned into control, model, Tripterygium glycosides(7.5 mg·kg~(-1)), and low-, medium-, and high-dose total triterpenes of Euphorbium(32, 64, and 128 mg·kg~(-1), respectively) groups, with 10 rats in each group. In other groups except the control group, 0.2 mL FCA was injected into the right hind toe. Rats in the intervention groups were administrated with corresponding drugs by gavage, and the control group and the model group with the same volume of 0.5% CMC-Na solution once a day. During the treatment period, the swelling degree of the hind paw was measured and the arthritis was scored until day 30. At the end of drug administration, the pathological changes of the joint tissue were observed by hematoxylin-eosin staining. The content of malondialdehyde(MDA), glutathione(GSH), and Fe~(2+) and the activity of superoxide dismutase(SOD) in the joint tissue were measured by biochemical colorimetry. RT-PCR was performed to determine the mRNA levels of nuclear factor erythroid 2-related factor 2(Nrf2), glutathione peroxidase 4(GPX4), and acyl-CoA synthetase long chain family member 4(ACSL4) in the joint tissue. Western blot was employed to determine the protein levels of Nrf2, Kelch-like ECH-associated protein 1(Keap1), heme oxygenase-1(HO-1), NAD(P)H quinone oxidoreductase 1(NQO1), SOD2, GPX4, and ACSL4 in the joint tissue. The results showed that the treatment with Tripterygium glycosides(7.5 mg·kg~(-1)) and total triterpenes of Euphorbium(32, 64, and 128 mg·kg~(-1)) alleviated the swelling degree of bilateral hind limbs, decreased the arthritis score, reduced joint tissue lesions and the content of MDA and Fe~(2+) in the joint tissue, and increased GSH content and SOD activity. Furthermore, the interventions up-regulated the protein and mRNA levels of Nrf2 and GPX4, down-regulated the protein and mRNA levels of ACSL4, and up-regulated the protein levels of Keap1, NQO1, HO-1, and SOD2 in the Nrf2/HO-1/GPX4. In summary, the total triterpenes of Euphorbium can treat RA by inhibiting lipid peroxidation and abnormal ferroptosis, which may involve the Nrf2/HO-1/GPX4 signaling pathway.


Subject(s)
Rats , Male , Animals , Rats, Sprague-Dawley , NF-E2-Related Factor 2/metabolism , Kelch-Like ECH-Associated Protein 1/metabolism , Triterpenes/pharmacology , Oxidative Stress , Arthritis, Rheumatoid/genetics , Glutathione , Superoxide Dismutase/metabolism , Glycosides/pharmacology , RNA, Messenger/metabolism
6.
China Journal of Chinese Materia Medica ; (24): 1642-1651, 2023.
Article in Chinese | WPRIM | ID: wpr-970636

ABSTRACT

The UPLC-MS/MS was established for the determination of acetyl-11-keto-beta-boswellic acid(AKBA) and β-boswellic acid(β-BA), the main active components of Olibanum and Myrrha extracts in Xihuang Formula, in rat plasma and urine. The effects of compatibility on the pharmacokinetic behaviors of AKBA and β-BA in rats were investigated, and the differences in pharmacokinetic behaviors between healthy rats and rats with precancerous lesions of breast cancer were compared. The results showed that compared with RM-NH and RM-SH groups, the AUC_(0-t) and AUC_(0-∞) of β-BA increased(P<0.05 or P<0.01), T_(max) decreased(P<0.05 or P<0.01), and C_(max) increased(P<0.01) after compatibility. The trends of AKBA and β-BA were the same. Compared with RM-SH group, the T_(max) decreased(P<0.05), C_(max) increased(P<0.01), and the absorption rate increased in the normal group of Xihuang Formula. The results of urinary excretion showed that there was a decreasing trend in the urinary excretion rate and total urinary excretion of β-BA and AKBA after compatibility, but there was no statistical difference. Compared with normal group of Xihuang Formula, the AUC_(0-t) and AUC_(0-∞) of β-BA increased(P<0.05), T_(max) increased(P<0.05), and the clearance rate decreased in the breast precancerous lesion group. AUC_(0-t) and AUC_(0-∞) of AKBA showed an increasing trend, the in vivo retention time was prolonged, and the clearance rate was reduced, but there was no significant difference compared with the normal group. The cumulative urinary excretion and urinary excretion rate of β-BA and AKBA decreased under pathological conditions, indicating that pathological conditions could affect the in vivo process of β-BA and AKBA, and reduce their excretion in the form of prototype drugs, showing different pharmacokine-tic characteristics from normal physiological conditions. In this study, UPLC-MS/MS analysis method was established, which was sui-table for in vivo pharmacokinetic analysis of β-BA and AKBA. This study laid a foundation for the development of new dosage forms of Xihuang Formula.


Subject(s)
Rats , Animals , Chromatography, Liquid , Tandem Mass Spectrometry , Drugs, Chinese Herbal , Precancerous Conditions , Triterpenes/pharmacology
7.
China Journal of Chinese Materia Medica ; (24): 469-475, 2022.
Article in Chinese | WPRIM | ID: wpr-927991

ABSTRACT

This study aimed to investigate the anti-inflammatory effect of astragaloside Ⅳ in mice with ulcerative colitis(UC) and its effect on the percentage of peripheral blood T helper(Th17) cells. Following the establishment of UC mouse model with 2% sodium dextran sulfate(DSS), mice in the positive control group and low-and high-dose astragaloside Ⅳ groups were treated with corresponding drugs by gavage. Disease activity index(DAI) was calculated, and serum interleukin-17(IL-17), tumor necrosis factor-α(TNF-α), and transforming growth factor-β(TGF-β) levels were assayed by ELISA. The pathological changes in colon tissue were observed by HE staining, and Th17/regulatory T cells(Treg) ratio in the peripheral blood was determined by flow cytometry. Western blot was conducted for detecting the relative protein expression levels of forkhead box protein P3(Foxp3) and retinoic acid-related orphan nuclear receptor γT(ROR-γt). The findings demonstrated that in normal mice, the colonic structure was intact. The goblet cells were not reduced and the glands were neatly arranged, with no mucosal erosion, bleeding, or positive cell infiltration. In the model group, the colonic mucosal structure was seriously damaged, manifested as disordered arrangement or missing of glands, vascular dilatation, congestion, and massive inflammatory cell infiltration. The pathological injury of colon tissue was alleviated to varying degrees in drug treatment groups. Compared with the normal group, the model group exhibited elevated percentage of Th17 cells, increased IL-17 and TNF-α content, up-regulated relative ROR-γt protein expression, lowered TGF-β, reduced percentage of Treg cells, and down-regulated relative Foxp3 protein expression. The comparison with the model group showed that DAI score, pathological score, percentage of Th17 cells, IL-17 and TNF-α content, and relative ROR-γt protein expression in the positive control group, low-dose astragaloside Ⅳ group, and high-dose astragaloside Ⅳ group were decreased, while TGF-β content, percentage of Treg cells, and relative Foxp3 protein expression were increased. The DAI score, pathological score, percentage of Th17 cells, IL-17 and TNF-α content, and relative ROR-γt protein expression in the low-dose astragaloside Ⅳ group were higher than those in the positive control group, whereas the content of TGF-β, percentage of Treg cells, and relative Foxp3 protein expression were lower. DAI score, pathological score, percentage of Th17 cells, IL-17 and TNF-α content, relative ROR-γt protein expression in the high-dose astragaloside Ⅳ group declined in contrast to those in the low-dose astragaloside Ⅳ group, while the TGF-β content, percentage of Treg cells, and relative Foxp3 protein expression rose. There was no significant difference between the positive control group and the high-dose astragaloside Ⅳ group. Astragaloside Ⅳ is able to inhibit inflammatory response and diminish the percentage of Th17 cells in mice with UC.


Subject(s)
Animals , Mice , Colitis, Ulcerative/metabolism , Saponins/pharmacology , T-Lymphocytes, Regulatory , Th17 Cells , Triterpenes/pharmacology
8.
China Journal of Chinese Materia Medica ; (24): 6114-6129, 2021.
Article in Chinese | WPRIM | ID: wpr-921770

ABSTRACT

At present, 141 compounds have been isolated from Picrorhiza scrophulariiflora and P. kurroa of the Scrophulariaceae plants, including 46 iridoid glycosides, 29 tetracyclic triterpenoids, 25 phenylpropanoids, and 11 phenylethanoid glycosides. Pharmacological studies have demonstrated that they have liver-, heart-, brain-, kidney-, and nerve cells-protecting effects as well as anti-tumor, anti-inflammatory, anti-bacterial, anti-asthma, anti-diabetic, immunomodulatory, and blood lipid-lowering activities. This article reviews the chemical components and pharmacological activities of P. scrophulariiflora and P. kurroa, aiming to provide a basis for the in-depth research, development, and utilization of the two plants.


Subject(s)
Iridoid Glycosides , Picrorhiza , Triterpenes/pharmacology
9.
China Journal of Chinese Materia Medica ; (24): 1783-1789, 2021.
Article in Chinese | WPRIM | ID: wpr-879092

ABSTRACT

Chemical constituents were isolated and purified from fruiting bodies of Ganoderma calidophilum by various column chromatographic techniques, and their chemical structures were identified through combined analysis of physicochemical properties and spectral data. As a result, 11 compounds were isolated and identified as(24E)-lanosta-8,24-dien-3,11-dione-26-al(1), ganoderone A(2), 3-oxo-15α-acetoxy-lanosta-7,9(11), 24-trien-26-oleic acid(3),(23E)-27-nor-lanosta-8,23-diene-3,7,25-trione(4), ganodecanone B(5), ganoderic aldehyde A(6), 11β-hydroxy-lucidadiol(7), 3,4-dihydroxyacetophenone(8), methyl gentiate(9), ganoleucin C(10), ganotheaecolumol H(11). Among them, compound 1 is a new triterpenoid. The cytotoxic activities of all of the compounds against tumor cell lines were evaluated. The results showed that compounds 1, 3, 4 and 6 showed cytotoxic activity against BEL-7402, with IC_(50) values of 26.55, 11.35, 23.23, 18.66 μmol·L~(-1); compounds 1 and 3-6 showed cytotoxic activity against K562, with IC_(50) values of 5.79, 22.16, 12.16, 35.32, and 5.59 μmol·L~(-1), and compound 4 showed cytotoxic activity against A549, with IC_(50) value of 42.50 μmol·L~(-1).


Subject(s)
Cell Line, Tumor , Fruiting Bodies, Fungal , Ganoderma , Molecular Structure , Triterpenes/pharmacology
10.
China Journal of Chinese Materia Medica ; (24): 380-387, 2021.
Article in Chinese | WPRIM | ID: wpr-878984

ABSTRACT

One new and two known dammarane-type saponins were isolated from the leaves of Gynostemma pentaphyllum using various chromatographic methods. Their structures were identified by HR-ESI-MS,~( 1)H-NMR, ~(13)C-NMR, 2 D-NMR spectra as 2α,3β,12β,20,24(S)-tetrahdroxydammar-25-en-3-O-[β-D-glucopyranosyl(1→2)-β-D-glucopyranosyl]-20-O-β-D-xylopyranosyl(1→6)-β-D-glucopyranoside(1, a new compound, namely gypenoside J5) and 2α,3β,12β,20,24(R)-tetrahdroxydammar-25-en-3-O-[β-D-glucopyranosyl(1→2)-β-D-glucopyranosyl]-20-O-β-D-xylopyranosyl(1→6)-β-D-glucopyranoside(2) and 2α,3β,12β,20-tetrahydroxy-25-hydroperoxy-dammar-23-en-3-O-[β-D-glucopyranosyl(1→2)][β-D-glucopyranosyl]-20-O-[β-D-xylopyranosyl(1→6)]-β-D-glucopy-ranoside(3), respectively. Compounds 1 and 2 were a pair of C-24 epimers. All compounds showed weak cytotoxicity agxinst H1299, HepG2, PC-3, SH-SY5 Y cancer cell lines. However, they exerted protective effect against SH-SY5 Y cellular damage induced by H_2O_2 dose-dependently, of which compound 1 displayed the strongest antioxidant effect. The present study suggested that G. pentaphyllum has antioxidative potential and the saponins from G. pentaphyllum are considered as the active compounds with neuroprotecitve effect.


Subject(s)
Gynostemma , Molecular Structure , Neuroprotective Agents/pharmacology , Saponins/pharmacology , Triterpenes/pharmacology
11.
Frontiers of Medicine ; (4): 79-90, 2021.
Article in English | WPRIM | ID: wpr-880969

ABSTRACT

Natural killer (NK) cells, a type of cytotoxic lymphocytes, can infiltrate into ischemic brain and exacerbate neuronal cell death. Astragaloside IV (ASIV) is the major bioactive ingredient of Astragalus membranaceus, a Chinese herbal medicine, and possesses potent immunomodulatory and neuroprotective properties. This study investigated the effects of ASIV on post-ischemic brain infiltration and activation of NK cells. ASIV reduced brain infarction and alleviated functional deficits in MCAO rats, and these beneficial effects persisted for at least 7 days. Abundant NK cells infiltrated into the ischemic hemisphere on day 1 after brain ischemia, and this infiltration was suppressed by ASIV. Strikingly, ASIV reversed NK cell deficiency in the spleen and blood after brain ischemia. ASIV inhibited astrocyte-derived CCL2 upregulation and reduced CCR2


Subject(s)
Animals , Rats , Brain , Histone Deacetylases , Killer Cells, Natural , Saponins/pharmacology , Triterpenes/pharmacology
12.
Bol. latinoam. Caribe plantas med. aromát ; 18(4): 347-358, jul. 2019. ilus
Article in English | LILACS | ID: biblio-1008172

ABSTRACT

Manilkara zapota (Sapotaceae), commonly known as Sapodilla, is widely known for its delicious fruit. Various parts of this plant are also used in folk medicine to treat a number of conditions including fever, pain, diarrhoea, dysentery, haemorrhage and ulcers. Scientific studies have demonstrated analgesic, anti-inflammatory, antioxidant, cytotoxic, antimicrobial, antidiarrheal, anti-hypercholesteremic, antihyperglycemic and hepatoprotective activities in several parts of the plant. Phytochemical studies have revealed the presence of phenolic compounds including protocatechuic acid quercitrin, myricitrin, catechin, gallic acid, vanillic acid, caffeic acid, syringic acid, coumaric acid, ferulic acid, etc. as main constituents of the plant. Several fatty acids, carotenoids, triterpenes, sterols, hydrocarbons and phenylethanoid compounds have also been isolated from M. zapota. The present review is a comprehensive description focused on pharmacological activities and phytochemical constituents of M. zapota.


Manilkara zapota (Sapotaceae), comúnmente conocida como Sapodilla, es ampliamente conocida por su delicioso fruto. Variadas partes de esta planta se usan en medicina popular para tratar una serie de afecciones, como fiebre, dolor, diarrea, disentería, hemorragia y úlceras. Estudios científicos han demostrado actividad analgésica, antiinflamatoria, antioxidante, citotóxica, antimicrobiana, antidiarreica, antihipercolesterolémica, antihiperglucémica y hepatoprotectora en diferentes partes de la planta. Los estudios fitoquímicos han revelado la presencia de compuestos fenólicos que incluyen ácido protocatechúico, quercitrina, miricitrina, catequina, ácido galico, ácido vanílico, ácido cafeico, ácido sirínico, ácido cumárico, ácido fúnico y ácido ferúlico como componentes principales de la planta. Varios ácidos grasos, carotenoides, triterpenos, esteroles, hidrocarburos y compuestos feniletanoides también han sido aislados de M. zapota. La presente revisión es una descripción exhaustiva centrada en las actividades farmacológicas y los constituyentes fitoquímicos de M. zapota.


Subject(s)
Plant Extracts/pharmacology , Manilkara/chemistry , Phenols/isolation & purification , Phenols/pharmacology , Saponins/isolation & purification , Saponins/pharmacology , Sterols/isolation & purification , Sterols/pharmacology , Triterpenes/isolation & purification , Triterpenes/pharmacology , Carotenoids/isolation & purification , Carotenoids/pharmacology , Sapotaceae/chemistry , Phenolic Compounds/analysis , Medicine, Traditional
13.
Braz. oral res. (Online) ; 33: e032, 2019. tab, graf
Article in English | LILACS | ID: biblio-1001608

ABSTRACT

Abstract: This study aimed to investigate the effects of astragaloside IV (AsIV) on inflammation and immunity in rats with experimental periodontitis. Periodontitis was established in 48 Wistar rats, which were then randomly divided into model and 10, 20 and 40 mg/kg AsIV groups, with 12 rats in each group. The latter 3 groups were treated with AsIV at doses of 10, 20 and 40 mg/kg, respectively. The control group (12 rats, without periodontitis) and model group were given the same amount of 5% sodium carboxymethyl cellulose. The treatment was performed once per day for 8 weeks. Before and after treatment, the tooth mobility scores of the rats were determined. After treatment, the salivary occult blood index (SOBI), plaque index (PLI), peripheral blood T lymphocyte subsets, and serum inflammatory factor and immunoglobulin levels were determined. The results showed that, after treatment, compared with that in model group, in 40 mg/kg AsIV group, the general state of rats was improved, while the tooth mobility score, SOBI and PLI were significantly decreased (p < 0.05); the peripheral blood CD4+ T cell percentage and CD4+/CD8+ ratio were significantly increased (p < 0.05), while the CD8+ T cell percentage was significantly decreased (p < 0.05); the serum tumor necrosis factor-α, interleukin-1β and interleukin-2 levels were significantly decreased (p < 0.05); the serum immunoglobulin A and immunoglobulin G levels were significantly decreased (p < 0.05). In conclusion, AsIV can alleviate inflammation and enhance immunity in rats with experimental periodontitis.


Subject(s)
Animals , Male , Female , Periodontitis/drug therapy , Saponins/pharmacology , Triterpenes/pharmacology , Immune System/drug effects , Periodontitis/immunology , Periodontitis/pathology , Reference Values , Tooth Mobility , Immunoglobulins/blood , Random Allocation , Reproducibility of Results , T-Lymphocyte Subsets , Interleukin-2/blood , Tumor Necrosis Factor-alpha/blood , Treatment Outcome , Rats, Wistar , Interleukin-1beta/blood
14.
Acta cir. bras ; 34(7): e201900708, 2019. tab, graf
Article in English | LILACS | ID: biblio-1038121

ABSTRACT

Abstract Purpose: To investigate the effect of astragaloside IV (As-IV) on myocardial ischemia-reperfusion (I/R) injury in rats and reltaed mechanisms. Methods: Sixty rats were randomly divided into sham-operated, control I/R and 2.5, 5 and 10 mg/kg As-IV groups, 12 rats in each group. The later three groups were intragastrically administered with As-IV for 7 days, with a dose of 2.5, 5 and 10 mg/kg, respectively. The myocardial I/R injury model was constructed in later four groups. At the end of reperfusion, the cardiac function indexes, serum lactate dehydrogenase (LDH) and creatine kinase (CK) levels, heart weight (HW)/body weight (BW) ratio and infarct size, and expressions of phosphatidylinositol-3 kinase/serine-threonine protein kinase (PI3K/AKT) and glycogen synthase kinase-3β (GSK-3β) proteins and the phosphorylated forms (p-AKT, p-GSK-3β) were determined. Results: Compared with control I/R group, in 5 and 10 mg/kg As-IV groups the left ventricular systolic pressure, fractional shortening and ejection fraction were increased, the left ventricular end-diastolic pressure was decreased, the serum LDH and CK levels were decreased, the HW/BW ratio and myocardial infarct size were decreased, and the p-Akt/Akt ratio and p-GSK-3β/GSK-3β ratio were increased (all P < 0.05). Conclusion: As-IV can alleviate the myocardial I/R injury in rats through regulating PI3K/AKT/GSK-3β signaling pathways.


Subject(s)
Animals , Male , Rats , Saponins/pharmacology , Triterpenes/pharmacology , Myocardial Reperfusion Injury/prevention & control , Signal Transduction/drug effects , Phosphatidylinositol 3-Kinases/metabolism , Proto-Oncogene Proteins c-akt/metabolism , Glycogen Synthase Kinase 3 beta/metabolism , Phosphorylation , Myocardial Reperfusion Injury/drug therapy , Rats, Sprague-Dawley
15.
An. acad. bras. ciênc ; 89(3): 1369-1379, July-Sept. 2017. tab, graf
Article in English | LILACS | ID: biblio-886755

ABSTRACT

ABSTRACT Natural steroids and triterpenes such as b-sitosterol, stigmasterol, lupeol, ursolic and betulinic acids were transformed into its hexanoic and oleic esters, to evaluate the influence of chemical modification towards the cytotoxic activities against tumor cells. The derivatives were evaluated against five tumor cell lines [OVCAR-8 (ovarian carcinoma); SF-295 (glioblastoma); HCT-116 (colon adenocarcinoma); HL-60 (leukemia); and PC-3 (prostate carcinoma)] and the results showed only betulinic acid hexyl ester exhibits cytotoxic potential activity.


Subject(s)
Humans , Triterpenes/pharmacology , Lamiaceae/chemistry , Pentacyclic Triterpenes/pharmacology , Fabaceae/chemistry , Antineoplastic Agents/pharmacology , Triterpenes/isolation & purification , Triterpenes/chemistry , Drug Screening Assays, Antitumor , Lamiaceae/classification , Inhibitory Concentration 50 , Cell Line, Tumor , Esters , Pentacyclic Triterpenes/isolation & purification , Pentacyclic Triterpenes/chemistry , Fabaceae/classification , Antineoplastic Agents/isolation & purification , Antineoplastic Agents/chemistry
16.
Bol. latinoam. Caribe plantas med. aromát ; 14(5): 403-422, Sept. 2015. ilus, tab
Article in English | LILACS | ID: biblio-907502

ABSTRACT

In addition to eucalyptin the methanol extract from leaves of Eucalyptus citriodora (Myrtaceae) afforded the known compounds apigenin, chrysin, luteolin, naringenin, quercetin; together with betulinic acid, oleanolic, ursolic acid, and two remaining complex mixtures of unidentified flavonoids and triterpenes. These compounds together with triterpenes mixtures, hexane and ethyl acetate extracts showed antifeedant, insecticidal and insect growth regulatory activities against fall armyworm [Spodoptera frugiperda JE Smith (Lepidoptera: Noctuidae)] an important pest of corn, and yellow mealworm [Tenebrio molitor (Coleoptera:Tenebrionidae)] a pest of stored grains. The most active compounds were chrysin, eucalyptin, quercetin, luteolin, and betulinic and oleanolic acids and the mixtures of flavonoids and triterpenes (M1 and M2). These compounds and mixtures had IGR activity between 0.2 to 5.0 ug/mL and insecticidal effects between 5.0 and 10.0 μg/mL.The extracts were insecticidal to larvae, with lethal doses between 20-100 ug/mL. These compounds appear to have selective effects on the pre-emergence metabolism of the Lepidoptera, since in all treatments of the larvae of S. frugiperda the pupation was shortened and this process showed precociousness in relation to control. Thus, these substances may be useful as potential natural insecticidal agents.


Extracto metanolico de hojas de Eucalyptus citriodora (Myrtaceae) proporcionó además de eucalyptin, flavonoides tales como apigenina, crisina, luteolina, naringenina, quercetina; los triterpenos, ácido oleanólico, ácido ursólico betulínico, y dos mezclas complejas de flavonoides y triterpenos no identificados M1 y M2. Los flavonoides, triterpenos y mezclas de triterpenos, extractos de acetato de etilo y hexano mostraron efectos antialimentarios, insecticida y actividad reguladora de crecimiento (IGR) frente al gusano cogollero [Spodoptera frugiperda JE Smith (Lepidoptera: Noctuidae)], una plaga importante del maíz y frente al gusano de la harina [Tenebrio molitor (Coleoptera: Tenebrionidae)], una plaga de los granos almacenados. Los compuestos más activos fueron crisina, eucalyptin, quercetina, luteolina, ácido betulínico y ácido oleanólico y las mezclas de flavonoides y triterpenos (M1 y M2). Estos compuestos y mezclas mostraron actividad IGR entre 0,2 y 5,0 ug/mL y efectos insecticidas entre 5,0 y 10,0 μg/mL. Los extractos mostraron carácter insecticida para las larvas a dosis letales entre 20-100 ug/mL. Estas muestras parecen tener efectos selectivos sobre el metabolismo de pre-emergencia de los lepidópteros, ya que en todos los tratamientos de las larvas de S. frugiperda el tiempo de la pupación se acortó; este proceso muestra precocidad en relación con el control, las substancias ensayadas en este trabajo pueden ser útiles como potenciales agentes insecticidas naturales.


Subject(s)
Coleoptera , Eucalyptus/chemistry , Insecticides/pharmacology , Plant Extracts/pharmacology , Spodoptera , Coleoptera/growth & development , Flavonoids/pharmacology , Methanol , Myrtaceae/chemistry , Spodoptera/growth & development , Triterpenes/pharmacology
17.
Braz. j. microbiol ; 46(2): 613-617, Apr-Jun/2015. tab, graf
Article in English | LILACS | ID: lil-749716

ABSTRACT

In this study, we revealed that OA and UA significantly inhibited the expression of most genes related to peptidoglycan biosynthesis in S. mutans UA159. To the best of our knowledge, this is the first report to introduce the antimicrobial mechanism of OA and UA against S. mutans.


Subject(s)
Anti-Bacterial Agents/pharmacology , Biosynthetic Pathways/drug effects , Biosynthetic Pathways/genetics , Oleanolic Acid/pharmacology , Peptidoglycan/biosynthesis , Streptococcus mutans/drug effects , Triterpenes/pharmacology , Gene Expression Regulation, Bacterial/drug effects
18.
Bol. latinoam. Caribe plantas med. aromát ; 14(3): 179-189, mayo 2015. tab, ilus
Article in English | LILACS | ID: biblio-907483

ABSTRACT

Seven compounds were isolated from the methanol extract of leaves of Ziziphus mauritiana. The structures of the isolated compounds were elucidated as y-fagarine (1), beta-sitosterol (2), stigmasterol (3), alfa-amyrin (4), lupeol (5), beta-amyrin (6) and betulin (7) by extensive spectroscopic studies and by co-TLC with authentic samples. This is the first report of isolation of compounds 1-7 from this plant species. The extractives from leaves were investigated for thrombolytic, membrane stabilizing, antimicrobial, antidiarrheal and analgesic potentials along with sleep inducing property on animal model. The thrombolytic and membrane stabilizing activities were assessed by using human erythrocyte comparing with standard streptokinase and acetylsalicylic acid, respectively. The methanolic extract reduced frequency of diarrheal faeces when compared to the standard loperamide. In castor oil induced diarrhea in mice a dose dependent decrease of gastrointestinal transits were observed. In radiant heat tail-flick method the methanol extract showed moderate antinociceptive activity, compared to standard morphine.


Siete compuestos fueron aislados del extracto metanólico de hojas de Ziziphus mauritiana. Las estructuras de los compuestos aislados fueron identificadas como y-fagarina (1), beta-sitosterol (2), estigmasterol (3), alfa-amirina (4), lupeol (5), beta-amirina (6) y betulina (7 ) por medio de extensivos estudios espectroscópicos y por co-TLC con muestras auténticas. Este es el primer informe de aislamiento de los compuestos 1-7 a partir de esta especie vegetal. Los extractos de las hojas fueron investigados por efectos trombolíticos, estabilizadores de membrana, antimicrobianos, antidiarreicos y potenciales analgésicos junto a la propiedad de inducir sueño en el modelo animal. Las actividades trombolíticos y la estabilización de la membrana se evaluaron mediante el uso de eritrocitos humanos comparando con estreptoquinasa estándar y el ácido acetilsalicílico, respectivamente. El extracto metanólico redujo la frecuencia de las heces diarreicas en comparación con el estándar de loperamida. En la inducción por aceite de ricino de diarrea en ratones, se observó una disminución dosis dependiente de los tránsitos gastrointestinales. En el método del coletazo producido por calor radiante, el extracto metabólico mostró una actividad antinociceptiva moderada, en comparación con la morfina estándar.


Subject(s)
Animals , Mice , Rats , Anti-Infective Agents/pharmacology , Antidiarrheals/pharmacology , Plant Leaves/chemistry , Triterpenes/pharmacology , Ziziphus/chemistry , Fibrinolytic Agents/pharmacology , Methanol , Triterpenes/isolation & purification
19.
Electron. j. biotechnol ; 18(2): 88-95, Mar. 2015. graf, tab
Article in English | LILACS | ID: lil-745575

ABSTRACT

Background Triterpenoids are multifunctional secondary metabolites in plants. But little information is available concerning the actual yield, optimal extraction method and pharmacologic activity with regard to triterpenoids from Jatropha curcas leaves (TJL). Hence, response surface methodology (RSM) was used to optimize the extraction parameters. The effects of three independent variables, namely liquid-to-solid ratio, ethanol concentration and extraction time on TJL yield were investigated. TJL obtained by silica column chromatography was tested against bacterial and fungal species relevant to oral disease and wounds through broth microdilution. Antioxidant activity was assessed using the 2,2-diphenyl-2-picrylhydrazyl and 2,2'-azino-bis(3-ethylbenzothiazoline-6-sulfonic acid) assays. Results A second order polynomial model produced a satisfactory fitting of the experimental data with regard to TJL yield (R2 = 0.983, P < 0.01). The optimum extraction conditions were 16 mL/g (liquid-to-solid ratio), 70% (ethanol concentration) and 50 min (extraction time). Predicted values agreed well with the experimental values. TJL had extraordinarily strong antibacterial and antifungal activities (24.42 µg/mL < MIC < 195.31 µg/mL) against all the tested human pathogens except Bacteroides vulgatus (390.62 µg/mL) and Bacteroides stercoris (781.25 µg/mL). The DPPH and ABTS assays revealed a moderate antioxidant activity of TJL compared with ascorbic acid. Conclusion These results provided reliable scientific basis for further investigation of triterpenoids from J. curcas.


Subject(s)
Triterpenes/analysis , Triterpenes/pharmacology , Jatropha/chemistry , Anti-Infective Agents/pharmacology , Anti-Inflammatory Agents/pharmacology , Time Factors , Bacteria/drug effects , Ultrasonics , Free Radical Scavengers , Ethanol/analysis , Fungi/drug effects
20.
Rev. bras. cir. cardiovasc ; 30(1): 33-39, Jan-Mar/2015. tab
Article in English | LILACS | ID: lil-742888

ABSTRACT

Introduction: The knowledge of the prevalence of risk factors and comorbidities, as well as the evolution and complications in patients undergoing coronary artery bypass graft allows comparison between institutions and evidence of changes in the profile of patients and postoperative evolution over time. Objective: To profile (risk factors and comorbidities) and clinical outcome (complications) in patients undergoing coronary artery bypass graft in a national institution of great surgical volume. Methods: A retrospective cohort study of patients undergoing coronary artery bypass graft in the hospital Beneficência Portuguesa de São Paulo, from July 2009 to July 2010. Results: We included 3,010 patients, mean age of 62.2 years and 69.9% male. 83.8% of patients were hypertensive, 36.6% diabetic, 44.5% had dyslipidemia, 15.3% were smokers, 65.7% were overweight/obese, 29.3% had a family history of coronary heart disease. The expected mortality calculated by logistic EuroSCORE was 2.7%. The isolated CABG occurred in 89.3% and 11.9% surgery was performed without cardiopulmonary bypass. The most common complication was cardiac arrhythmia (18.7%), especially acute atrial fibrillation (14.3%). Pneumonia occurred in 6.2% of patients, acute renal failure in 4.4%, mediastinites in 2.1%, stroke in 1.8% and AMI in 1.2%. The in-hospital mortality was 5.4% and in isolated coronary artery bypass graft was 3.5%. The average hospital stay was 11 days with a median of eight days (3-244 days). Conclusion: The profile of patients undergoing coronary artery bypass graft surgery in this study is similar to other published studies. .


Introdução: O conhecimento da prevalência dos fatores de risco e comorbidades, bem como a evolução com complicações nos pacientes submetidos à cirurgia de revascularização miocárdica, permite a comparação entre instituições e a comprovação de modificações no perfil de pacientes e na evolução pós-operatória ao longo do tempo. Objetivo: Conhecer o perfil (fatores de risco e comorbidades) e a evolução clínica (complicações) nos pacientes submetidos à cirurgia de revascularização miocárdica em uma instituição nacional de grande volume cirúrgico. Métodos: Estudo de coorte retrospectivo de pacientes submetidos ao procedimento de cirurgia de revascularização miocárdica no Hospital Beneficência Portuguesa de São Paulo, no período de julho de 2009 a julho de 2010. Resultados: Foram incluídos 3010 pacientes, com idade média de 62,2 anos e 69,9% do sexo masculino. 82,8% dos pacientes eram hipertensos, 36,6% diabéticos, 44,5% dislipidêmicos, 15,3% tabagistas, 65,7% com sobrepeso/obesidade e 29,3% tinham antecedentes familiares de doença coronária. A mortalidade média esperada calculada pelo EuroSCORE logístico foi de 2,7%. A cirurgia de revascularização miocárdica isolada ocorreu em 89,3% e em 11,9% foi realizada cirurgia sem circulação extracorpórea. A complicação mais comum foi arritmia cardíaca (18,7%), especialmente a fibrilação atrial aguda (14,3%). Pneumonia ocorreu em 6,2% dos pacientes, lesão renal aguda em 4,4%, mediastinite em 2,1%, acidente vascular encefálico em 1,8% e infarto agudo do miocárdio em 1,2%. A mortalidade intra-hospitalar foi de 5,4% e na cirurgia de revascularização miocárdica isolada foi de 3,5%. O tempo de permanência hospitalar médio foi de 11 dias, com mediana de oito dias (3 - 244 dias). Conclusão: O perfil dos pacientes submetidos à cirurgia de revascularização miocárdica neste estudo assemelha-se ao de outros estudos publicados. .


Subject(s)
Animals , Humans , Mice , Gene Expression Profiling , Muscle, Skeletal/pathology , Muscular Atrophy/genetics , Triterpenes/pharmacology , Cell Line , Fasting , Gene Expression Regulation , Gene Expression/drug effects , Hindlimb/innervation , Insulin-Like Growth Factor I/metabolism , Insulin/metabolism , Muscle Denervation , Muscle Fibers, Skeletal/drug effects , Muscle Fibers, Skeletal/metabolism , Muscle Strength/drug effects , Muscle, Skeletal/drug effects , Muscle, Skeletal/metabolism , Muscular Atrophy/drug therapy , Muscular Atrophy/metabolism , Oligonucleotide Array Sequence Analysis , Signal Transduction/drug effects
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