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1.
China Journal of Chinese Materia Medica ; (24): 2419-2425, 2023.
Article in Chinese | WPRIM | ID: wpr-981318

ABSTRACT

This study combined the herbal pair Platycodonis Radix-Curcumae Rhizoma(PR-CR) possessing an inhibitory effect on tumor cell proliferation and metastasis with the active component of traditional Chinese medicine(TCM) silibinin-loaded nanoparticles(NPs) with a regulatory effect on tumor microenvironment based on the joint effect on tumor cells and tumor microenvironment to inhi-bit cell metastasis. The effects of PR-CR on the cellular uptake of NPs and in vitro inhibition against breast cancer proliferation and metastasis were investigated to provide an experimental basis for improving nanoparticle absorption and enhancing therapeutic effects. Silibinin-loaded lipid-polymer nanoparticles(LPNs) were prepared by the nanoprecipitation method and characterized by transmission electron microscopy. The NPs were spherical or quasi-spherical in shape with obvious core-shell structure. The mean particle size was 107.4 nm, Zeta potential was-27.53 mV. The cellular uptake assay was performed by in vitro Caco-2/E12 coculture cell model and confocal laser scanning microscopy(CLSM), and the results indicated that PR-CR could promote the uptake of NPs. Further, in situ intestinal absorption assay by the CLSM vertical scanning approach showed that PR-CR could promote the absorption of NPs in the enterocytes of mice. The inhibitory effect of NPs on the proliferation and migration of 4T1 cells was analyzed using 4T1 breast cancer cells and co-cultured 4T1/WML2 cells, respectively. The results of the CCK8 assay showed that PR-CR-containing NPs could enhance the inhibition against the proliferation of 4T1 breast cancer cells. The wound healing assay indicated that PR-CR-containing NPs enhanced the inhibition against the migration of 4T1 breast cancer cells. This study enriches the research on oral absorption of TCM NPs and also provides a new idea for utilizing the advantages of TCM to inhibit breast cancer metastasis.


Subject(s)
Humans , Mice , Animals , Female , Silymarin/therapeutic use , Caco-2 Cells , Polymers/chemistry , Nanoparticles/chemistry , Cell Line, Tumor , Breast Neoplasms/pathology , Tumor Microenvironment
2.
Arq. bras. med. vet. zootec. (Online) ; 72(4): 1248-1257, July-Aug. 2020. tab, ilus
Article in English | LILACS, VETINDEX | ID: biblio-1131497

ABSTRACT

Bidens pilosa L. is a medicinal plant popularly used for treatment of liver diseases. In this study, the dry extract of aerial parts of Bidens pilosa and Silymarin, a phytocomplex obtained from the Silybum marianum fruits and marketed as hepatoprotective, were tested in dogs experimentally acutely intoxicated with carbon tetrachloride. The liver activity was evaluated by hematological and biochemical profiles, and histological and ultrasound analyzes. It was observed that the lowest serum activities of ALT and serum concentrations of total bilirubin occurred in the groups treated with the dry extract of Bidens pilosa, while only decreased serum concentrations of total bilirubin occurred in the group treated with Silymarin. Best liver recovery was also observed for the dry extract of B. pilosa at a 400mg/Kg dose by ultrasonography. This study showed that the dry extract of Bidens pilosa acted more efficiently in the treatment of acute toxic hepatitis induced in dogs than Silymarin.(AU)


Bidens pilosa L. é uma planta medicinal utilizada popularmente para tratamento de doenças hepáticas. Neste trabalho, o extrato seco das partes aéreas da Bidens pilosa e a silimarina, um fitocomplexo obtido dos frutos da Silybum marianum e comercializado como hepatoprotetor, foram testados em cães intoxicados experimentalmente de forma aguda com tetracloreto de carbono. A atividade hepática foi avaliada por meio dos perfis hematológico e bioquímico, análises histológica e ultrassonográfica. Observou-se que, nos grupos tratados com o extrato seco da Bidens pilosa, ocorreram as menores atividades séricas da ALT e de concentrações séricas de bilirrubina total, enquanto no grupo tratado com silimarina, ocorreu apenas diminuição de concentrações séricas de bilirrubina total. Melhor recuperação hepática também foi verificada para o extrato seco de B. pilosa na dose de 400mg/kg por ultrassonografia. Este estudo evidenciou que o extrato seco da Bidens pilosa atuou de forma mais eficiente no tratamento da hepatite aguda tóxica induzida em cães do que a silimarina.(AU)


Subject(s)
Animals , Dogs , Carbon Tetrachloride Poisoning/therapy , Carbon Tetrachloride Poisoning/veterinary , Bidens/chemistry , Hepatitis, Animal/therapy , Plants, Medicinal , Silymarin/therapeutic use
3.
Acta cir. bras ; 32(6): 407-417, June 2017. tab, graf
Article in English | LILACS | ID: biblio-886210

ABSTRACT

Abstract Purpose: To investigate the hepatoprotective and antioxidant effeicacies of Silybum marianum's (silymarin, S) on University of Wisconsin (UW) and histidinetryptophan-ketoglutarate (HTK) preservation solutions. Methods: Thirty two Wistar albino adult male rats were used. Group 1: UW group, Group 2: UW + Silymarin group(S), Group 3: HTK group, Group 4: HTK + silymarin group (S), respectively. Silymarin was enforced intraperitoneally before the surgery. Biopsies were enforced in 0, 6 and 12.hours to investigate. Results: Biochemical parameters examined in alanine aminotransferase (ALT), furthermore superoxide dismutase (SOD), catalase (CAT), and malondialdehyde (MDA) in rats were also evaluated. Detected histopathological changings were substantially declining in the groups that received silymarin, cellular damage was decreased significantly in HTK + Silymarin group, according to other groups. It has been identified as the most effective group was HTK + silymarin group in evaluation of ALT, electron microscopic results, also decreased MDA and elevated in SOD, and CAT activity. Caspase 3 analysis showed a substantial lower apoptosis ratio in the silymarin groups than in the non-performed groups (p<0.05). Conclusion: Histidinetryptophan-ketoglutarate+silymarin group provides better hepatoprotection than other groups, by decreasing the hepatic pathologic damage, delayed changes that arise under cold ischemic terms.


Subject(s)
Animals , Male , Rats , Silymarin/therapeutic use , Organ Preservation Solutions , Protective Agents/therapeutic use , Chemical and Drug Induced Liver Injury/drug therapy , Antioxidants/therapeutic use , Potassium Chloride , Procaine , Raffinose , Immunohistochemistry , Adenosine , Allopurinol , Rats, Wistar , Disease Models, Animal , Glucose , Glutathione , Insulin , Mannitol
4.
Pakistan Journal of Pharmaceutical Sciences. 2017; 30 (4): 1203-1211
in English | IMEMR | ID: emr-189683

ABSTRACT

This study was designed to evaluate the effects of sylimarin supplementation on different biochemical parameters in thioacetamide induced cirrhotic rats. For this purpose 24 male Albino wistar rats were divided into four groups [n=6]. Group I, remained healthy control rats, Group II, received thioacetamide [at a dose of 200mg/kg b.w, i.p, for 12 weeks, twice a week] in first phase and saline in second phase, Group III, received thioacetamide [200mg/kg b.w, i.p for 12 weeks, twice a week] in first phase and silymarin [orally at a dosage of 200mg/kg b.w, twice a week, for 8 weeks] in second phase and Group IV, received silymarin [orally at a dosage of 200mg/kg b.w, twice a week, for 8 weeks] in first phase and saline in second phase. Biochemical analysis was evaluated by total and direct bilirubin [Retiman and Franhel, 1957, Sherlock, 1951], liver specific enzymes, antioxidant enzymes [SOD [Kono et a/., 1978], Catalase [Sinha et al, 1979], Glutathione reductase [Calberg and Mannervik, 1985] and MDA [Okhawa et al, 1979]] and plasma and intraerythrocyte sodium and potassium [Tabssum et #/., 1996]. Marked increase in total and direct bilirubin and ALT activity was the indicative markers of liver cirrhosis while reduced antioxidant activity [SOD and GSH] and increased MDA and Catalase levels and disturbed electrolyte homeostasis were observed in cirrhotic group. Silymarin supplementation markedly reduced total bilirubin and ALT activity and restored the antioxidant enzymes [SOD and GSH], MDA and catalase activity and electrolyte homeostasis. These results indicate that silymarin successively attenuates the thioacetamide induced liver cirrhosis


Subject(s)
Animals, Laboratory , Silymarin/therapeutic use , Rats, Wistar , Thioacetamide , Glutathione Reductase , Antioxidants
5.
Indian J Exp Biol ; 2014 Jul; 52(7): 705-711
Article in English | IMSEAR | ID: sea-153750

ABSTRACT

Justicia adhatoda (vasaka) leaves have long been used in Indian Ayurvedic system of medicine as antitussive. Its crude extract has been previously reported to have hepatoprotective activity. Vasicinone was isolated from leaves of J. adhatoda, column purified and characterized using, TLC UV, FT-IR and 1H NMR. The isolated vasicinone was evaluated for hepatoprotective activity using (CCl4)-induced acute hepatotoxicity model in mice. CCl4 treatments lead to significant increase in SGOT, SGPT, ALP levels. Pre-treatment with vasicinone and silymarin (25 mg/kg/day for 7 days) significantly decreased these enzyme levels. Histopathology of the livers from vasicinone and silymarin pre-treated animals showed normal hepatic cords and absence of necrotic changes suggesting pronounced recovery from CCl4 induced liver damage. Both vasicinone and silymarin significantly decrease the CCl4 mediated increase in pentobarbital indiced sleeping time in experimental animals, thus indicating recovery of liver function. Based on the above results it can be concluded that vasicinone may act as hepatoprotective in mice and warrants further investigation on human volunteers.


Subject(s)
Justicia/chemistry , Alkaloids/therapeutic use , Animals , Carbon Tetrachloride Poisoning , Chemical and Drug Induced Liver Injury/prevention & control , Humans , Male , Mice , Phytotherapy , Plant Extracts/therapeutic use , Plant Leaves/chemistry , Protective Agents/therapeutic use , Silymarin/therapeutic use , Spectroscopy, Fourier Transform Infrared
6.
Article in English | IMSEAR | ID: sea-157400

ABSTRACT

Objective: To study the protective effect of ethyl acetate extract of Acacia catechu in carbon tetrachloride induced hepatotoxicity in albino rats. Methods: The liver damage in albino rat was induced by a subcutaneous injection of 50%v/ v carbon tetrachloride in olive oil at the dose of 2ml/kg twice a week for 14days. The hepatoprotective activity was monitored biochemically by estimating serum transaminases, serum alkaline phosphatase, serum bilirubin and serum protein after intraperitoneal injection of ethyl acetate extract of Katha(250mg/kg). Silymarin(5mg/kg.I.P) was given as a reference drug. The histopathological changes of liver samples were compared with that of control. Results: Ethyl acetate extract of Acacia catechu inhibited carbon tetrachloride induced liver toxicity in albino rats at 250mg/kg body weight as assessed by the biochemical and histological examination. Conclusion: Ethyl acetate extract of “Katha” exhibited significant hepatoprotective activity.


Subject(s)
Acacia/classification , Acacia/therapeutic use , Acetates , Adult , Animals , Carbon Tetrachloride/toxicity , Chemical and Drug Induced Liver Injury/chemically induced , Chemical and Drug Induced Liver Injury/drug therapy , Chemical and Drug Induced Liver Injury/etiology , Chemical and Drug Induced Liver Injury/prevention & control , Liver/toxicity , Plant Extracts/therapeutic use , Rats , Silymarin/therapeutic use
7.
Diagn. tratamento ; 17(1)mar. 2012.
Article in Portuguese | LILACS | ID: lil-621172

ABSTRACT

Introduction: Silymarin is a plant known for decades and with varied medicinal properties targeted to the liver.Objective: To investigate evidence of the use of silymarin in alcoholic liver disease and on hepatitis B and C.Methods: Review of the literature through electronic search, including studies of good methodological quality assessing the effects of silymarin on liver.Results: A systematic review of 13 studies and only 3 of them with good methodological quality showed unsatisfactory results in chronic liver diseases most common evolutionary disease as alcoholic and viral hepatitis B and C. Were demonstrated statistically significant changes in the decrease of transaminases and gamma-GT (gamma-glutamyl transpeptidase) in alcoholic liver disease, but did not change the mortality and other clinical and biochemical parameters in both alcoholic liver disease and in liver viral.Conclusion: Experimental studies have shown beneficial effects of silymarin in the liver by various drugs. However, there is insufficient evidence of its efficacy and safety in the treatment of chronic alcoholic liver disease and viral in its outcome greater mortality.


Introdução: A silimarina é uma planta conhecida há décadas e com propriedades medicinais variadas direcionadas para o fígado.Objetivo: Verificar evidências do uso da silimarina na doença alcóolica do fígado e nas hepatites B e C.Métodos: Revisão sistematizada da literatura por meio de busca eletrônica, incluindo estudos com boa qualidade metodológica que avaliem os efeitos da silimarina em hepatopatias.Resultados: Uma revisão sistemática com 13 estudos e somente 3 deles com boa qualidade metodológica mostraram resultados não satisfatórios nas hepatopatias crônicas evolutivas mais comuns como por doença alcóolica e hepatites virais B e C. Foram demonstradas alterações estatisticamente significantes na diminuição das transaminases e gama-GT (gama-glutamil transpeptidase) na doença hepática alcoólica, porém, sem alterar a mortalidade e outros parâmetros clínicos e bioquímicos tanto na hepatopatia alcoólica como nas hepatopatias virais.Conclusão: Estudos experimentais mostraram efeitos benéficos da silimarina nas hepatopatias por diversas drogas. No entanto, não há evidências suficientes de sua eficácia e segurança no tratamento de hepatopatias crônicas alcoólicas e virais no seu desfecho maior, a mortalidade.


Subject(s)
Humans , Alcoholism/therapy , Liver Cirrhosis/therapy , Hepatitis B/therapy , Hepatitis C/therapy , Silymarin/analysis , Silymarin/therapeutic use
8.
Braz. j. med. biol. res ; 44(7): 652-659, July 2011. ilus, tab
Article in English | LILACS | ID: lil-595696

ABSTRACT

Silybin, a natural antioxidant, has been traditionally used against a variety of liver ailments. To investigate its effect and the underlying mechanisms of action on non-alcoholic fatty liver in rats, we used 60 4-6-week-old male Sprague-Dawley rats to establish fatty liver models by feeding a high-fat diet for 6 weeks. Hepatic enzyme, serum lipid levels, oxidative production, mitochondrial membrane fluidity, homeostasis model assessment-insulin resistance index (HOMA-IR), gene and protein expression of adiponectin, and resistin were evaluated by biochemical, reverse transcription polymerase chain reaction (RT-PCR) and Western blot analysis. Compared with the model group, silybin treatment (26.25 mg·kg-1·day-1, started at the beginning of the protocol) significantly protected against high-fat-induced fatty liver by stabilizing mitochondrial membrane fluidity, reducing serum content of alanine aminotransferase (ALT) from 450 to 304 U/L, decreasing hepatic malondialdehyde (MDA) from 1.24 to 0.93 nmol/mg protein, but increasing superoxide dismutase (SOD) and glutathione (GSH) levels from 8.03 to 9.31 U/mg protein and from 3.65 to 4.52 nmol/mg protein, respectively. Moreover, silybin enhanced the gene and protein expression of adiponectin from 215.95 to 552.40, but inhibited that of resistin from 0.118 to 0.018. Compared to rosiglitazone (0.5 mg·kg-1·day-1, started at the beginning of the protocol), silybin was effective in stabilizing mitochondrial membrane fluidity, reducing SOD as well as ALT, and regulating gene and protein expression of adiponectin (P < 0.05). These results suggest that mitochondrial membrane stabilization, oxidative stress inhibition, as well as improved insulin resistance, may be the essential mechanisms for the hepatoprotective effect of silybin on non-alcoholic fatty liver disease in rats. Silybin was more effective than rosiglitazone in terms of maintaining mitochondrial membrane fluidity and reducing oxidative stress.


Subject(s)
Animals , Male , Rats , Antioxidants/therapeutic use , Fatty Liver/drug therapy , Hypoglycemic Agents/therapeutic use , Oxidative Stress/drug effects , Silymarin/therapeutic use , Thiazolidinediones/therapeutic use , Antioxidants/administration & dosage , Dietary Fats , Disease Models, Animal , Drug Evaluation, Preclinical , Fatty Liver/chemically induced , Fatty Liver/prevention & control , Homeostasis , Hypoglycemic Agents/administration & dosage , Insulin Resistance/physiology , Lipid Peroxidation/drug effects , Lipids/blood , Liver/drug effects , Random Allocation , Rats, Sprague-Dawley , Silymarin/administration & dosage , Thiazolidinediones/administration & dosage
9.
Rev. chil. dermatol ; 25(1): 8-20, 2009.
Article in Spanish | LILACS | ID: lil-525460

ABSTRACT

Nuestra piel está constantemente expuesta al estrés oxidativo endógeno y exógeno, el cual juega un papel fundamental tanto en el envejecimiento intrínseco como extrínseco. El estrés oxidativo se debe a la producción de especies reactivas de oxígeno, también conocidas como radicales libres. Las estructuras vitales que se ven afectadas por este proceso son el ADN, elementos del citoesqueleto, proteínas celulares y membranas celulares. El cuerpo posee mecanismos de defensa contra los radicales libres, denominados antioxidantes, los cuales son capaces de reducirlos y neutralizarlos. Sin embargo, como parte natural del proceso de envejecimiento, no sólo la producción de especies reactivas de oxígeno aumenta, sino que los mecanismos endógenos de defensa disminuyen, resultando en un desbalance con predominio de radicales libres no neutralizados que dañan las estructuras del organismo. Aunque el cuerpo posee antioxidantes endógenos y ciertos alimentos son ricos en antioxidantes, muchos creen que niveles más altos de estas sustancias pueden obtenerse con suplementos alimentarios. En consecuencia, ha llegado a ser muy popular el uso de antioxidantes en suplementos orales o en forma tópica, los cuales podrían potencialmente aminorar los efectos adversos de las especies reactivas de oxígeno. En esta revisión se analizan los antioxidantes más conocidos que se encuentran incorporados en los productos cosméticos o que son administrados por vía oral en los pacientes interesados en la cosmética personal.


Our skin is constantly exposed to endogenous and exogenous oxidative stress, which plays a pivotal role in intrinsic and extrinsic aging. Oxidative stress is delivered by the creation of reactive oxygen species also known as free radicals. Vital structures that can be adversely affected by this process are DNA, cytoskeletal elements, cellular proteins, and cellular membranes. The body possesses defense mechanisms against free radicals, which are called antioxidants, and are able to reduce and neutralize them. However, as part of the natural aging process, not only does the production of reactive oxygen species increase, but our endogenous defense mechanisms decrease resulting in an imbalance and increased number of unchecked free radicals damaging vital structures of the body. Although the body possesses endogenous antioxidants and certain foods are rich in antioxidants, many believe that higher levels can be achieved by supplementation. Consequently, the use of antioxidants as oral supplements or topical formulation should be able to lessen the harmful adverse effects induced by reactive oxygen species and has thus become popular. This review discusses the most popular types of antioxidants found in cosmetic products or taken orally by cosmetic patients.


Subject(s)
Humans , Antioxidants/therapeutic use , Skin Aging , Ascorbic Acid/therapeutic use , Coffee/chemistry , Carotenoids/therapeutic use , Curcumin/therapeutic use , Stilbenes/therapeutic use , Plant Extracts/therapeutic use , Polypodium/chemistry , Silymarin/therapeutic use , Tea , Ubiquinone/analogs & derivatives , Ubiquinone/therapeutic use , Vitamin E/therapeutic use
10.
Indian J Exp Biol ; 2008 Jun; 46(6): 447-52
Article in English | IMSEAR | ID: sea-57552

ABSTRACT

Ethanol extract and its ethanol fraction from aerial parts of P. daemia exhibited significant hepatoprotective effect against CCl4 induced hepatotoxicity in rats. Glutamic oxaloacetic transaminase, glutamic pyruvic transaminase, alkaline phosphatase, total bilirubin, total cholesterol, total protein and albumin in serum indicated hepatoprotective effect of the ethanol extract and its ethanol fraction. Histopathological examination of liver sections confirmed that, pre-treatment with ethanol extract and its ethanol fraction prevented hepatic damage induced by CCl4. The results were comparable with the standard hepatoprotective drug silymarin. The extract and its fraction showed no signs of toxicity up to a dose level of 2000 mg/kg. It is suggested that, the presence of flavonoids in ethanol extract and its ethanol fraction may be responsible for hepatoprotective properties. High Performance Thin Layer Chromatography profile of flavonoids of bio-active extracts was developed using quercetin-3-glucoside as a marker. Results indicate hepatoprotective properties of ethanol extract of P. daemia.


Subject(s)
Animals , Apocynaceae , Dose-Response Relationship, Drug , Female , Chemical and Drug Induced Liver Injury/pathology , Male , Phytotherapy , Plant Extracts/administration & dosage , Plant Leaves , Plant Stems , Rats , Silymarin/therapeutic use
11.
Indian J Exp Biol ; 2005 Jan; 43(1): 68-75
Article in English | IMSEAR | ID: sea-60600

ABSTRACT

Significant recovery after treatment with the whole plant slurry of A.longifolia Nees. was observed in plasma AST, ALT and cholesterol levels in CCl4 induced hepatotoxic rats. This was amply supported by electron micrographs, which indicated normalization of cytoarchitecture of mitochondria and endoplasmic reticulum. The results suggest that the slurry of the plant is useful as a liver tonic.


Subject(s)
Acanthaceae/chemistry , Animals , Carbon Tetrachloride/toxicity , Female , Liver/drug effects , Liver Diseases/chemically induced , Liver Function Tests , Male , Microscopy, Electron , Plant Extracts/therapeutic use , Plant Leaves/chemistry , Protective Agents/therapeutic use , Rats , Rats, Wistar , Seeds/chemistry , Silymarin/therapeutic use
12.
Southeast Asian J Trop Med Public Health ; 1999 Mar; 30(1): 157-60
Article in English | IMSEAR | ID: sea-32103

ABSTRACT

Consumption of toxic mushrooms belonging to the genus Amanita frequently leads to severe gastrointestinal distress followed by acute hepatic failure with a fatal outcome. In Thailand, valuable information as to the locally prevalent poisonous species, the preferred habitat and the management of suspected victims of intoxication is basically non-existent. We report here 5 cases of fatal poisoning with Amanita virosa having occurred in a family residing in the northeast of Thailand who as countless others had enjoyed mushroom gathering as a pasttime. Within 4 to 6 days after ingestion of the mushrooms, all had succumbed to acute hepatic failure with subsequent hepatoencephalopathy. Treatment modalities exist in the form of penicillin and silibinin, or thioctic acid administration followed by plasmapheresis. In cases taking a lethal course apparent from the results of liver biochemistry, liver transplantation is clearly indicated. In order to prevent mushroom poisoning altogether, educating the general population to that end certainly presents the method of choice.


Subject(s)
Adult , Amanita , Child , Combined Modality Therapy , Fatal Outcome , Female , Fluid Therapy , Health Education , Hepatic Encephalopathy/etiology , Humans , Liver Failure, Acute/etiology , Male , Mushroom Poisoning/etiology , Penicillins/therapeutic use , Plasmapheresis , Protective Agents/therapeutic use , Silymarin/therapeutic use , Thailand , Thioctic Acid/therapeutic use
13.
Arch. med. res ; 28(1): 11-7, mar. 1997. ilus, tab
Article in English | LILACS | ID: lil-225191

ABSTRACT

The comparative effects of colchicine (10 µg day-1, p.o.) and silymarin (50 mg kg-1, p.o.) each given for 5 days a week on the chronica carbon tetrachloride (CCl4) liver damage were studied. Treatment with CCl4, resulted in a marked reduction of Na+, K+, and Ca2+-ATPases in plasma liver membranes as compared to vehicles or either silymain or chochicine alone. Collagen content in livers of animals treated with CCl4 was increased about four-folds as compared to controls and histological examination of liver samples showed thad collagen incfrease distorted the normal liver architecture. Colchicine or silymarin treatment completely prevented all the changes observed in CCl4-cirrhotic rats (namely, lipid peroxidation, Na+, k+ and Ca2+-ATPases), except for livel collagen conten which was reduced only 55 percent as compared with CCl4-treated rats and for alkaline phosphatase and glutamic pyruvic transminase wich still remained above controls. In the CCl4 + silymarin group, the loss of glycogen content was completely prevented. However, when rats were treated with CCl4+colchicine, liver glycogen content could not be restored. The hepatoprotective effects of colchicine or silymarin were very similar in regard to the prevention of chronic liver damage


Subject(s)
Animals , Male , Rats , Carbon Tetrachloride Poisoning/drug therapy , Liver Cirrhosis, Experimental/pathology , Liver Cirrhosis, Experimental/prevention & control , Colchicine/pharmacology , Colchicine/therapeutic use , Free Radical Scavengers/therapeutic use , Liver , Liver/metabolism , Silymarin/pharmacology , Silymarin/therapeutic use , Rats, Wistar
14.
Indian J Exp Biol ; 1993 Apr; 31(4): 316-8
Article in English | IMSEAR | ID: sea-57257

ABSTRACT

Picroliv showed a dose (3-12 mg/kg, po for 7 days) dependent choleretic activity as evidenced by increase in bile flow and its contents (bile salts and bile acids). Significant anticholestatic activity was also observed against carbon tetrachloride induced cholestasis in conscious rat, anaesthetized guinea pig and cat. Picroliv was more active than the known hepatoprotective drug silymarin.


Subject(s)
Animals , Bile Acids and Salts/biosynthesis , Carbon Tetrachloride , Cats , Cholestasis/prevention & control , Cinnamates/therapeutic use , Dose-Response Relationship, Drug , Female , Glycosides/therapeutic use , Guinea Pigs , Male , Plant Extracts/therapeutic use , Rats , Silymarin/therapeutic use , Vanillic Acid/therapeutic use
15.
Mem. Inst. Oswaldo Cruz ; 86(supl.2): 79-85, 1991. ilus, tab, graf
Article in English | LILACS | ID: lil-623946

ABSTRACT

Silymarin is the flavonoids extracted from the seeds of Silybum marianum (L) Gearth as a mixture of three structural isomers: silybin, silydianin and silychristin, the former being the most active component. Silymarin protects liver cell membrane against hepatotoxic agents and improves liver function in experimental animals and humans. It is generally accepted that silymarin exerts a membrane-stabilizing action preventing or inhibiting membrane peroxidation. The experiments with soybean lipoxygenase showed that the three components of silymarin brought about a concentration-dependent non-competitive inhibition of the lipoxygenase. The experiments also showed an analogous interaction with animal lipoxygenase, thus showing that an inhibition of the peroxidation of the fatty acid in vivo was self-evident. Silybin almost completely suppressed the formation of PG at the highest concentration (0.3 mM) and proved to be an inhibitor of PG synthesis in vitro. In our experiments, silybin at lower dose (65 mg/Kg) decreased liver lipoperoxide content and microsomal lipoperoxidation to 84.5% and 68.55% of those of the scalded control rats respectively, and prevented the decrease of liver microsomal cytochrome p-450 content and p-nitroanisole-0-demethylase activity 24 h post-scalding. Effects of silymarin on cardiovascular systen have been studied in this university since 1980. O. O silymarin 800 mg/Kg/d or silybin 600 mg/Kg/d reduced plasma total cholesterol, LDL-C and VLDL-C. They however, enhanced HDL-C in hyperlipenic rats. Further studies showed that silymarin enhanced HDL-C in hyperlipemic rats. Further studies showed that silymarin enhanced HDL-C but didn't affect HDL-C, a property of this component which is beneficial to treatment of atherosclerosis. The results showed silymarin 80 mg or silybin 60 mg decreased in vitro platelet aggregation (porcentagem) in rats. The maximal platelet aggregation induced by ADP declined significantly, and time to reach maximal platelet aggregation and five-minute disaggregation didn't change. In our experiments, iv silybin 22,4 mg/kg lowered the amplitude and duration of diastolic blood pressure (DBP) more than those of systolic (SBP), but the descending aortic blood flow, cardiac contractility and ECG did not change significantly in anesthetized open-chest cats. The results indicated a reduction of peripheral resistance and dilatatory action on the resistant blood vessels. These effects are beneficial to coronary heart disease. We also observed the effects of silybin on morphological change, the release of glutamic oxaloacetate aminotrasferase (GOT) and lactate dehydrogenase (LDH) as well as the radioactivity of 3H-TdR incorporated into DNA in normal cardiac cells and cells infected by coxsackie B5, virus os newborn rats. The results showed that silynin did not affect the morphology of normal cell, and that the pathological change of cells infected by virus was delayed and reduced as compared to control. We have investigated the effect of silybin on synthesis and release of LTs in the cultured porcine cerebral basilar arteries (PCBA). Silybin 100 and 500 µmol/L declined the amounts of LTs released from the PCBA incubsated in the presence of A 23187, AA and indomenthacin. The result suggests that silybin can inhibit the activity of 5-lipoxygenase of cerebral blood vessel and may protect the brain from ischemia.


Subject(s)
Animals , Silymarin/therapeutic use , Platelet Aggregation Inhibitors/pharmacology , Cardiovascular System/drug effects , Lipoxygenase Inhibitors/pharmacology , Hemodynamics/drug effects , Antioxidants/pharmacology , Lipids/blood , Liver
16.
Article in English | IMSEAR | ID: sea-23926

ABSTRACT

Silymarin, a flavolignan from the seeds of Silybum marianum, showed significant hepatoprotective activity in P. berghei-induced hepatic damage in M. natalensis, as assessed by changes in several serum and liver biochemical parameters. Changes in lipoprotein-X, GOT, GPT, alkaline phosphatase and bilirubin were found to be protected by silymarin at different doses. Maximum activity was observed at a dose of 5 mg/kg bw, po. Silymarin had no effect on parasitaemia.


Subject(s)
Animals , Disease Models, Animal , Dose-Response Relationship, Drug , Flavonoids/therapeutic use , Hepatitis, Animal/prevention & control , Liver Function Tests , Malaria/pathology , Male , Muridae , Plasmodium berghei , Silymarin/therapeutic use
17.
Arch. biol. med. exp ; 21(1): 75-83, jun. 1988. ilus
Article in Spanish | LILACS | ID: lil-65233

ABSTRACT

Este estudio presenta en forma sucinta los aspectos más relevantes de nuestro trabajo de investigación con el flavonoide silyvina. Su mecanismo de acción como citoprotector se relacionaría con una acción a tres niveles: como antioxidante, evitando la lipoperoxidación celular inducida por xenobióticos; aumentando la concentración intracelular de glutatión, permitiendo mejorar la función protectora y de desintoxicación de este tripéptido, y regulando la permeabilidad de las membranas celulares en forma relativamente específica a la entrada o salida de metabolitos. Se discuten las proyecciones terapéuticas del flavonoide, así como su efecto protector específico en la toxicidad hepática de la fenilhidrazina, el etanol y el acetaminofeno


Subject(s)
Humans , Liver/drug effects , Microsomes/drug effects , Silymarin/metabolism , Acetaminophen , Cell Membrane Permeability/drug effects , Ethanol/pharmacology , Liver/metabolism , Oxygen Consumption/drug effects , Phenylhydrazines/pharmacology , Silymarin/pharmacokinetics , Silymarin/therapeutic use
18.
Invest. med. int ; 14(3): 144-54, nov. 1987. ilus
Article in Spanish | LILACS | ID: lil-48181

ABSTRACT

Con el fin de estudiar el efecto y tolerancia terapéutica de silimarina en hepatopatías agudas de origen viral y alcohólico, se estudiaron 30 pacientes a los que se les administró el medicamento en grageas durante 30 días a razón de 140 mg, tres veces al día. Los pacientes fueron divididos en dos grupos. El grupo I fue compuesto por 15 pacientes con diagnóstico clínico, bioquímico y serológico de hepatitis viral. Doce pacientes fueron varones y tres mujeres, con edad de 18 a 38 años, edad media 25.5 ñ 5.81. El grupo II incluyó 15 pacientes con diagnóstico clínico, bioquímico e histológico de hepatitis alcohólica, 13 varones y dos mujeres con edad de 32 a 67 años, edad media 48.8 ñ 8.93. Cada semana fue valorada la eficacia y tolerancia al fármaco tomando como referencia da evolución clínica y exámenes de laboratorio practicados, los cuales fueron: pruebas funcionales hepáticas completas, biometría hepática, química sanguínea y examen general de orina. Los resultados demonstraron que silimarina fue bien tolerada en ambos grupos. En cuanto a la eficacia, los pacientes del grupo I presentaron respuesta terapéutica excelente en 40%, buena en 20%, regular en 6.67% y nula en 33.33%. En el grupo II la respuesta fue excelente en 33.33%m buena en 13.33%, regular en 40% y nula 13.33%. Silimarina fue útil en ambos grupos de pacientes, con respuesta eficaz clínica y bioquímica de 86.67% en el grupo II y de 66.67% en el grupo I


Subject(s)
Adult , Humans , Male , Female , Hepatitis, Alcoholic/drug therapy , Hepatitis, Viral, Human/drug therapy , Silymarin/therapeutic use
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