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1.
Zhongguo Zhong Yao Za Zhi ; 48(10): 2781-2791, 2023 May.
Artículo en Chino | MEDLINE | ID: mdl-37282938

RESUMEN

Rosae Radix et Rhizoma is a herbal medicine in a variety of famous Chinese patent medicines, while the quality standard for this medicine remains to be developed due to the insufficient research on the quality of Rosae Radix et Rhizoma from different sources. Therefore, this study comprehensively analyzed the components in Rosae Radix et Rhizoma of different sources from the aspects of extract, component category content, identification based on thin-lay chromatography, active component content determination, and fingerprint, so as to improve the quality control. The results showed that the content of chemical components varied in the samples of different sources, while there was little difference in the chemical composition among the samples. The content of components in the roots of Rosa laevigata was higher than that in the other two species, and the content of components in the roots was higher than that in the stems. The fingerprints of triterpenoids and non-triterpenoids were established, and the content of five main triterpenoids including multiflorin, rosamultin, myrianthic acid, rosolic acid, and tormentic acid in Rosae Radix et Rhizoma was determined. The results were consistent with those of major component categories. In conclusion, the quality of Rosae Radix et Rhizoma is associated with the plant species, producing area, and medicinal parts. The method established in this study lays a foundation for improving the quality standard of Rosae Radix et Rhizoma and provides data support for the rational use of the stem.


Asunto(s)
Medicamentos Herbarios Chinos , Plantas Medicinales , Medicamentos Herbarios Chinos/química , Rizoma/química , Raíces de Plantas/química , Control de Calidad
2.
Artículo en Chino | WPRIM | ID: wpr-981381

RESUMEN

Rosae Radix et Rhizoma is a herbal medicine in a variety of famous Chinese patent medicines, while the quality standard for this medicine remains to be developed due to the insufficient research on the quality of Rosae Radix et Rhizoma from different sources. Therefore, this study comprehensively analyzed the components in Rosae Radix et Rhizoma of different sources from the aspects of extract, component category content, identification based on thin-lay chromatography, active component content determination, and fingerprint, so as to improve the quality control. The results showed that the content of chemical components varied in the samples of different sources, while there was little difference in the chemical composition among the samples. The content of components in the roots of Rosa laevigata was higher than that in the other two species, and the content of components in the roots was higher than that in the stems. The fingerprints of triterpenoids and non-triterpenoids were established, and the content of five main triterpenoids including multiflorin, rosamultin, myrianthic acid, rosolic acid, and tormentic acid in Rosae Radix et Rhizoma was determined. The results were consistent with those of major component categories. In conclusion, the quality of Rosae Radix et Rhizoma is associated with the plant species, producing area, and medicinal parts. The method established in this study lays a foundation for improving the quality standard of Rosae Radix et Rhizoma and provides data support for the rational use of the stem.


Asunto(s)
Medicamentos Herbarios Chinos/química , Rizoma/química , Raíces de Plantas/química , Plantas Medicinales , Control de Calidad
3.
Zhen Ci Yan Jiu ; 47(10): 896-901, 2022 Oct 25.
Artículo en Chino | MEDLINE | ID: mdl-36301167

RESUMEN

OBJECTIVE: To observe the effect of electroacupuncture on sexual development and ovarian estrogen receptor ß(ER-ß) expression in female adolescent obese rats induced by high-fat diet, so as to explore its underlying mechanisms of improving adolescent obesity. METHODS: Female SD rats (age of 21 days) were randomly divided into control, model and acupuncture groups, with 6 rats in each group. The obese model was established by feeding high-fat diet for 6 weeks. Rats of the acupuncture group received electroacupuncture(2 Hz, 0.5-1.2 mA)stimulation at bilateral "Sanyinjiao"(SP6), "Fenglong"(ST40) and "Zusanli"(ST36) for 30 min, once a day for 14 days. The body mass and abdominal circumference of rats were measured before and after treatment. The contents of serum follicle stimulating hormone (FSH), luteinizing hormone (LH) and estradiol (E2) were detected by ELISA. The number of corpus luteum and follicle were observed by HE staining. The expression levels of ER-ß mRNA and protein in ovary were detected by fluorescence quantitative PCR and Western blot, respectively. RESULTS: Compared with the control group, the body mass and abdominal circumference, the contents of serum FSH and E2, and the expression levels of ER-ß mRNA and protein in ovary were significantly increased (P<0.05)in the model group, while the number of mature follicles and corpus luteum increased significantly. Compared with the model group, the body mass and abdominal circumference, the contents of serum FSH and E2, and the expression levels of ER-ß mRNA and protein in ovary were significantly decreased (P<0.05) in the acupuncture group, while the number of mature follicles and corpus luteum decreased significantly. CONCLUSION: Electroacupuncture can effectively improve the levels of sex hormone and the development of ovary, down-regulate the expression levels of ER-ß mRNA and protein in ovary, so as to regulate the process of sexual development of female adolescent obese rats induced by high-fat diet.


Asunto(s)
Electroacupuntura , Obesidad Infantil , Ratas , Femenino , Animales , Ovario/metabolismo , Puntos de Acupuntura , Receptor beta de Estrógeno/genética , Receptor beta de Estrógeno/metabolismo , Ratas Sprague-Dawley , Obesidad Infantil/metabolismo , Hormona Folículo Estimulante , Desarrollo Sexual , ARN Mensajero/metabolismo
4.
Sheng Li Xue Bao ; 74(4): 563-573, 2022 Aug 25.
Artículo en Chino | MEDLINE | ID: mdl-35993208

RESUMEN

The classical auditory oddball paradigm is a commonly used experimental paradigm for evoking event related potentials (ERPs). The present study was aimed to explore the auditory cognitive processing mechanism of space perception of human brain. We employed an auditory oddball paradigm of binaural unbiased and biased sound intensity to compare and analyze the response characteristics of ERP. By focusing on the spatial lateralization characteristics of P300 and mismatch negativity (MMN) components, we analyzed their lateralization trends according to the laterality index. We found that both P300 and MMN components showed right-hemisphere lateralization phenomenon under the stimulation of asymmetric intensity of auditory acoustic. The results suggested that the right hemisphere of human brain played a key role in spatial information processing. The results also indicated that the hemispherical characteristics of the brain were not related to the actual spatial direction of the auditory stimulus, but were determined by the hemispherical functions of the brain. Furthermore, the results suggested that the MMN components induced by spatial differences were stronger in females than those in males.


Asunto(s)
Mapeo Encefálico , Potenciales Evocados Auditivos , Estimulación Acústica , Percepción Auditiva/fisiología , Electroencefalografía , Potenciales Evocados , Potenciales Evocados Auditivos/fisiología , Femenino , Humanos , Masculino
5.
Front Pharmacol ; 12: 658092, 2021.
Artículo en Inglés | MEDLINE | ID: mdl-33935779

RESUMEN

Clear cell renal cell carcinoma (ccRCC) is characterized by abnormal lipid accumulation. Celastrol is a pentacyclic triterpene extracted from Tripterygium wilfordii Hook F with anti-cancer activity. In the present study, the anticancer effects of celastrol on ccRCC and the underlying mechanisms were studied. Patients with reduced high density lipoprotein (HDL) and elevated levels of triglyceride (TG), total cholesterol (TC), low density lipoprotein (LDL) was found to have higher risk of ccRCC. In ccRCC clinical samples and cell lines, caveolin-1 (CAV-1) was highly expressed. CAV-1 was identified as a potential prognostic biomarker for ccRCC. Celastrol inhibited tumor growth and decreased lipid deposition promoted by high-fat diet in vivo. Celastrol reduced lipid accumulation and caveolae abundance, inhibited the binding of CAV-1 and lectin-like oxidized low-density lipoprotein receptor-1 (LOX-1) in ccRCC cells. Furthermore, celastrol attenuated stemness through blocking Wnt/ß-catenin pathway after knockdown of CAV-1 and LOX-1. Therefore, the findings suggest that celastrol may be a promising active ingredient from traditional Chinese medicine for anti-cancer therapy.

6.
Zhongguo Zhong Yao Za Zhi ; 46(7): 1813-1821, 2021 Apr.
Artículo en Chino | MEDLINE | ID: mdl-33982486

RESUMEN

Prunella vulgaris(PV) is an edible and traditional medicinal herb which has a wide range application in fighting inflammation and oxidative stress, and protecting liver. Now it has been used to treat various types of liver diseases and has significant clinical efficacy. This study aims to investigate the effects of PV on ethanol-induced oxidative stress injury in rats and its metabolic mechanism. The rats were divided into control group, model group, PV group, and VC group. The liver protection of PV was identified by measuring pharmacological indexes such as antioxidant and anti-inflammatory activity. The metabolic mechanism of long-term ethanol exposure and the metabolic regulation mechanism of PV treatment were studied by LS-MS metabonomics. The pharmacological investigation indicated that ethanol could significantly decrease the contents of SOD, GSH-Px, CAT and other antioxidant enzymes in liver and increase the content of MDA. At the same time, PV could significantly reduce the contents of inflammatory factors(TNF-α, IL-6 and IL-1ß) and liver function markers(ALT, AST, ALP) in serum. What's more, long-term ethanol exposure could significantly cause liver injury, while PV could protect liver. Metabolomics based on multiple statistical analyses showed that long-term ethanol exposure could cause significant metabolic disorder, and fatty acids, phospholipids, carnitines and sterols were the main biomarkers. Meanwhile, pathway analysis and enrichment analysis showed that the ß oxidation of branched fatty acids was the main influencing pathway. Also, PV could improve metabolic disorder of liver injury induced by ethanol, and amino acids, fatty acids, and phospholi-pids were the main biomarkers in PV treatment. Metabolic pathway analysis showed that PV mainly regulated metabolic disorder of ethanol-induced liver injury through phenylalanine, tyrosine and tryptophan biosynthetic pathways. This study could provide a new perspective on the hepatoprotective effect of natural medicines, such as PV.


Asunto(s)
Prunella , Animales , Antioxidantes/metabolismo , Etanol/toxicidad , Hígado/metabolismo , Metabolómica , Estrés Oxidativo , Ratas
7.
BMC Complement Med Ther ; 21(1): 120, 2021 Apr 12.
Artículo en Inglés | MEDLINE | ID: mdl-33845816

RESUMEN

BACKGROUND: The idiosyncratic hepatotoxicity of Polygonum multiflorum (PM) has attracted considerable interest, but the idiosyncratically hepatotoxic components and endogenous metabolite changes resulting from idiosyncratic hepatotoxicity of PM are not well understood. The aim of this study was to identify the idiosyncratically hepatotoxic components and potential endogenous metabolic biomarkers for PM-induced liver injury. METHODS: Serum biochemical indicators and hematoxylin and eosin (H&E) staining were evaluated to identify pathological changes. Gas chromatography/mass spectrometry (GC-MS) was performed to identify changes in metabolic biomarkers. Orthogonal projection to latent structures discriminant analysis (OPLS-DA) was applied to determine group clustering trends and differential metabolites. RESULTS: The results for the liver index, the liver function index and liver pathology showed that Polygonum multiflorum ethanol extract (PME), 50% ethanol elution fractions and tetrahydroxystilbene glucoside (TSG) from PME can induce idiosyncratic hepatotoxicity. TSG was the main idiosyncratically hepatotoxic component. Forty endogenous metabolites were identified in the rat liver. Six biomarkers, including lower levels of L-valine and higher levels of 3-hydroxybutyric acid, hexadecanoic acid, ribose, phosphoric acid and oxalic acid, were related to PM-induced liver injury. These differential biomarkers led to disruptions in amino acid, fatty acid, oxalate, energy and glucose metabolism. A total of 32 types of endogenous metabolites were identified in rat serum. Ten biomarkers were related to the liver injury induced by TSG, including lower levels of L-valine and L-proline and higher levels of urea, caproic acid, DL-malic acid, D-mannose, 3-hydroxybutyric acid, D-galactose, octadecane and hexadecanoic acid. These differential biomarkers led to disruptions in amino acid, glucose and fat metabolism. The mechanism of idiosyncratic hepatotoxicity in PM involves TSG-induced disruptions in amino acid metabolism, lipid metabolism, energy metabolism and glucose metabolism. CONCLUSIONS: These findings reflect the material basis and metabolic mechanism of idiosyncratic PM hepatotoxicity.


Asunto(s)
Medicamentos Herbarios Chinos/farmacología , Polygonum , Animales , Biomarcadores/metabolismo , Enfermedad Hepática Inducida por Sustancias y Drogas , Medicamentos Herbarios Chinos/química , Cromatografía de Gases y Espectrometría de Masas , Hígado/efectos de los fármacos , Masculino , Extractos Vegetales/química , Extractos Vegetales/farmacología , Raíces de Plantas , Ratas , Organismos Libres de Patógenos Específicos
8.
Zhongguo Zhong Yao Za Zhi ; 46(24): 6353-6365, 2021 Dec.
Artículo en Chino | MEDLINE | ID: mdl-34994127

RESUMEN

In this paper, the newly isolated tannins were sorted after a review of the literature concerning tannins in recent 10 years, and their research progress was summarized in terms of extraction, isolation, pharmacological activity and metabolism. Hydrolysable tannins and condensed tannins are the main structural types. Modern research shows that tannins have many pharmacological effects, such as bacteriostasis, antioxidation, antitumor, antivirus and blood glucose reduction, and have broad development prospects. They are usually extracted by water, ethanol and acetone and isolated and purified by macroporous resin and gel column chromatography. The packings commonly adopted for the column chromatography mainly included Sephadex LH-20, Diaion HP-20, MCI-gel CHP-20 and Toyopearl HW-40. Modern analytical techniques such as nuclear magnetic resonance spectroscopy(NMR), fast atom bombardment mass spectrometry(FAB-MS) and circular dichroism(CD) are generally used for the structural identification of tannins. Howe-ver, their isolation, purification and structural identification are still challenging. It is necessary to use a variety of high-throughput screening methods to explore their pharmacological activities and to explore the material basis responsible for their functions through experiments in vivo.


Asunto(s)
Proantocianidinas , Taninos , China , Taninos Hidrolizables , Medicina Tradicional China
9.
Artículo en Chino | WPRIM | ID: wpr-921794

RESUMEN

In this paper, the newly isolated tannins were sorted after a review of the literature concerning tannins in recent 10 years, and their research progress was summarized in terms of extraction, isolation, pharmacological activity and metabolism. Hydrolysable tannins and condensed tannins are the main structural types. Modern research shows that tannins have many pharmacological effects, such as bacteriostasis, antioxidation, antitumor, antivirus and blood glucose reduction, and have broad development prospects. They are usually extracted by water, ethanol and acetone and isolated and purified by macroporous resin and gel column chromatography. The packings commonly adopted for the column chromatography mainly included Sephadex LH-20, Diaion HP-20, MCI-gel CHP-20 and Toyopearl HW-40. Modern analytical techniques such as nuclear magnetic resonance spectroscopy(NMR), fast atom bombardment mass spectrometry(FAB-MS) and circular dichroism(CD) are generally used for the structural identification of tannins. Howe-ver, their isolation, purification and structural identification are still challenging. It is necessary to use a variety of high-throughput screening methods to explore their pharmacological activities and to explore the material basis responsible for their functions through experiments in vivo.


Asunto(s)
China , Taninos Hidrolizables , Medicina Tradicional China , Proantocianidinas , Taninos
10.
Artículo en Chino | WPRIM | ID: wpr-879096

RESUMEN

Prunella vulgaris(PV) is an edible and traditional medicinal herb which has a wide range application in fighting inflammation and oxidative stress, and protecting liver. Now it has been used to treat various types of liver diseases and has significant clinical efficacy. This study aims to investigate the effects of PV on ethanol-induced oxidative stress injury in rats and its metabolic mechanism. The rats were divided into control group, model group, PV group, and VC group. The liver protection of PV was identified by measuring pharmacological indexes such as antioxidant and anti-inflammatory activity. The metabolic mechanism of long-term ethanol exposure and the metabolic regulation mechanism of PV treatment were studied by LS-MS metabonomics. The pharmacological investigation indicated that ethanol could significantly decrease the contents of SOD, GSH-Px, CAT and other antioxidant enzymes in liver and increase the content of MDA. At the same time, PV could significantly reduce the contents of inflammatory factors(TNF-α, IL-6 and IL-1β) and liver function markers(ALT, AST, ALP) in serum. What's more, long-term ethanol exposure could significantly cause liver injury, while PV could protect liver. Metabolomics based on multiple statistical analyses showed that long-term ethanol exposure could cause significant metabolic disorder, and fatty acids, phospholipids, carnitines and sterols were the main biomarkers. Meanwhile, pathway analysis and enrichment analysis showed that the β oxidation of branched fatty acids was the main influencing pathway. Also, PV could improve metabolic disorder of liver injury induced by ethanol, and amino acids, fatty acids, and phospholi-pids were the main biomarkers in PV treatment. Metabolic pathway analysis showed that PV mainly regulated metabolic disorder of ethanol-induced liver injury through phenylalanine, tyrosine and tryptophan biosynthetic pathways. This study could provide a new perspective on the hepatoprotective effect of natural medicines, such as PV.


Asunto(s)
Animales , Ratas , Antioxidantes/metabolismo , Etanol/toxicidad , Hígado/metabolismo , Metabolómica , Estrés Oxidativo , Prunella
11.
Nutrition ; 83: 111058, 2021 03.
Artículo en Inglés | MEDLINE | ID: mdl-33360033

RESUMEN

Substance abuse is a chronic relapsing disorder that results in serious health and socioeconomic issues worldwide. Addictive drugs induce long-lasting morphologic and functional changes in brain circuits and account for the formation of compulsive drug-seeking and drug-taking behaviors. Yet, there remains a lack of reliable therapy. In recent years, accumulating evidence indicated that neuroinflammation was implicated in the development of drug addiction. Findings from both our and other laboratories suggest that ω-3 polyunsaturated fatty acids (PUFAs) are effective in treating neuroinflammation-related mental diseases, and indicate that they could exert positive effects in treating drug addiction. Thus, in the present review, we summarized and evaluated recently published articles reporting the neuroinflammation mechanism in drug addiction and the immune regulatory ability of ω-3 PUFAs. We also sought to identify some of the challenges ahead in the translation of ω-3 PUFAs into addiction treatment.


Asunto(s)
Conducta Adictiva , Ácidos Grasos Omega-3 , Trastornos Relacionados con Sustancias , Humanos , Trastornos Relacionados con Sustancias/tratamiento farmacológico
12.
Acta Pharmacol Sin ; 42(9): 1472-1485, 2021 Sep.
Artículo en Inglés | MEDLINE | ID: mdl-33303989

RESUMEN

Celastrol is a triterpene derived from the traditional Chinese medicine Tripterygium wilfordii Hook f, which displays potential anticancer activity. In the present study, we investigated the anticancer effects of celastrol against clear cell renal cell carcinoma (ccRCC) and the underlying mechanisms. Using Cancer Genome Atlas (TCGA) database and genotype-tissue expression (GTEx) database we conducted a bioinformatics analysis, which showed that the mRNA levels of liver-X receptors α (LXRα) and ATP-binding cassette transporter A1 (ABCA1) in ccRCC tissues were significantly lower than those in adjacent normal tissues. This result was confirmed by immunoblotting analysis of 4 ccRCC clinical specimens, which showed that the protein expression of LXRα and ABCA1 was downregulated. Similar results were obtained in a panel of ccRCC cell lines (786-O, A498, SN12C, and OS-RC-2). In 786-O and SN12C cells, treatment with celastrol (0.25-2.0 µM) concentration-dependently inhibited the cell proliferation, migration, and invasion as well as the epithelial-mesenchymal transition (EMT) process. Furthermore, we demonstrated that celastrol inhibited the invasion of 786-O cells through reducing lipid accumulation; celastrol concentration-dependently promoted autophagy to reduce lipid storage. Moreover, we revealed that celastrol dramatically activated LXRα signaling, and degraded lipid droplets by inducing lipophagy in 786-O cells. Finally, celastrol promoted cholesterol efflux from 786-O cells via ABCA1. In high-fat diet-promoted ccRCC cell line 786-O xenograft model, administration of celastrol (0.25, 0.5, 1.0 mg·kg-1·d-1, for 4 weeks, i.p.) dose-dependently inhibited the tumor growth with upregulated LXRα and ABCA1 protein in tumor tissue. In conclusion, this study reveals that celastrol triggers lipophagy in ccRCC by activating LXRα, promotes ABCA1-mediated cholesterol efflux, suppresses EMT progress, and ultimately inhibits cell proliferation, migration, and invasion as well as tumor growth. Thus, our study provides evidence that celastrol can be used as a lipid metabolism-based anticancer therapeutic approach.


Asunto(s)
Transportador 1 de Casete de Unión a ATP/metabolismo , Autofagia/efectos de los fármacos , Carcinoma de Células Renales/metabolismo , Receptores X del Hígado/metabolismo , Triterpenos Pentacíclicos/farmacología , Transportador 1 de Casete de Unión a ATP/genética , Animales , Línea Celular Tumoral , Movimiento Celular/efectos de los fármacos , Humanos , Metabolismo de los Lípidos/efectos de los fármacos , Ratones Endogámicos BALB C , Ratones Desnudos , Transducción de Señal/efectos de los fármacos
13.
BMC Complement Med Ther ; 20(1): 189, 2020 Jun 18.
Artículo en Inglés | MEDLINE | ID: mdl-32552673

RESUMEN

BACKGROUND: The flowers and dried fruit spikes of Prunella vulgaris L. (P. vulgaris L.) have been widely used in traditional Chinese medicine and food. P. vulgaris L. is regarded as a good option for treating uterine myoma (UM). However, scientific evidence of anti-UM activity of the extract of P. vulgaris L. (PVE) is lacking. The present study aimed to characterize the chemical composition of PVE and evaluate the pharmacodynamics and mechanism of PVE against UM. METHODS: The chemical composition of PVE was analyzed by GC-MS. MTT was used to screen and evaluate cell proliferation and toxicity. Double fluorescence flow cytometry method were used to determine the apoptosis and cell cycle progression of UM cells under PVE treatment. The anti-UM activity of PVE was investigated by using a specific-pathogen-free (SPF) rat model of UM. TUNEL staining was used to detect the apoptosis of UM cells. The concentrations of estrogen and progesterone in the serum of SPF rats were detected by ELISA. The expression levels of PCNA, estrogen receptor alpha, estrogen receptor beta, progesterone receptor, survivin, caspase-3, Bax and Bcl-2 in the uterus of SPF rats was detected by immunohistochemistry (IHC). RESULTS: The extraction rate of PVE was 8.1%. The main components were squalene (28.3%), linoleic acid (9.96%), linolenic acid (9.95%), stearic acid (6.26%) and oleic acid (5.51%). In vitro, PVE had significant anti-human UM cell activity, exhibited no drug toxicity, promoted the apoptosis of human UM cells, and inhibited the transition of UM cells from the G0/G1 stage into the G2 stage, in which DNA replication occurs. In vivo, PVE had significant anti-UM activity. PVE decreased the concentrations of estrogen and progesterone and downregulated the expression levels of the estrogen and progesterone receptors through the estrogen signaling pathway. PVE also promoted the apoptosis of UM cells by downregulating the expression levels of the survivin and Bcl-2 proteins and upregulating the expression levels of caspase-3 and Bax through the mitochondria-mediated apoptotic pathway. CONCLUSION: PVE has marked anti-UM activity. PVE can be used as an ideal candidate drug to treat UM.


Asunto(s)
Antineoplásicos/farmacología , Apoptosis/efectos de los fármacos , Extractos Vegetales/farmacología , Prunella/química , Neoplasias Uterinas/tratamiento farmacológico , Animales , Antineoplásicos/química , Línea Celular Tumoral , Modelos Animales de Enfermedad , Evaluación Preclínica de Medicamentos , Femenino , Flores/química , Frutas/química , Humanos , Extractos Vegetales/química , Ratas , Organismos Libres de Patógenos Específicos
14.
Am J Chin Med ; 48(3): 559-577, 2020.
Artículo en Inglés | MEDLINE | ID: mdl-32345030

RESUMEN

Depression is partially caused by inflammation in the central nervous system. Early study demonstrated that musk, glandular secretion from male musk deer, exerted an antidepressant-like effect. The aim of this study was to investigate if muscone, a bioactive ingredient in musk, could ameliorate neuroinflammation and depressive-like behaviors as well as explore the potential action mechanism. Mice were intraperitoneally (i.p.) injected with muscone for 2 weeks prior to administration of lipopolysaccharides (LPS, 1mg/kg, i.p.). Pre-treatment with muscone reversed the LPS-induced decrease in body weight within 24h and ameliorated depressive-like behaviors shown by sucrose preference, tail suspension test, and forced swimming test. LPS-induced activation of microglial cells and elevation in expression of inflammatory cytokines including IL-1ß, RANTES, and MCP-1 in the prefrontal cortex of mice were effectively abrogated by muscone, which significantly down-regulated expression of TLR4, MyD88, Caspase-1, NLRP3, renin, and Ang II. In addition, treatment of BV2 microglia cells with muscone markedly attenuated the LPS-induced rise in protein expression of TLR4, Ang II, and IL-1ß. This study revealed that muscone could ameliorate LPS-induced depressive-like behaviors by repressing neuroinflammation in the prefrontal cortex of mice caused by its suppression on microglia activation and production of inflammatory cytokines via acting on TLR4 pathway and RAS cascade.


Asunto(s)
Cicloparafinas/administración & dosificación , Cicloparafinas/farmacología , Depresión/tratamiento farmacológico , Lipopolisacáridos/efectos adversos , Animales , Peso Corporal/efectos de los fármacos , Citocinas/metabolismo , Ciervos , Depresión/inducido químicamente , Mediadores de Inflamación/metabolismo , Inyecciones Intraperitoneales , Masculino , Ratones , Microglía/citología , Microglía/efectos de los fármacos , Corteza Prefrontal/metabolismo , Corteza Prefrontal/patología , Transducción de Señal/efectos de los fármacos , Receptor Toll-Like 4/metabolismo
15.
Medicine (Baltimore) ; 99(2): e18467, 2020 Jan.
Artículo en Inglés | MEDLINE | ID: mdl-31914018

RESUMEN

BACKGROUND: Curcumin, a controversial "panacea," has been broadly studied. Its bioactivities including antioxidant, anti-inflammatory, and especially antineoplastic activities have been documented. However, due to its extensive bioactivities, some scientists hold a skeptical point of view toward curcumin and described curcumin as a "deceiver" to chemists. The objective of this study was to explore curcumin's another possibility as a potential supplementary leading compound to cancer treatments. METHODS: Literature searches were conducted using electronic databases. Search terms such as "curcumin," "curcumin analogues," and so on were used. The literatures were collected and summarized. In this article, reported targets of curcumin are reviewed. The limitations of a curcumin as a therapeutic anticancer product including low bioavailability and poor targeting are mentioned. Furthermore, modified curcumin analogues and antitumor mechanisms are listed and discussed in the aspects of cell death and tumor microenvironment including angiogenesis, tissue hypoxia status, and energy metabolism. RESULTS: Several possible modification strategies were presented by analyzing the relationships between the antitumor activity of curcumin analogues and their structural characteristics, including the introduction of hydrophilic group, shortening of redundant hydrocarbon chain, the introduction of extra chemical group, and so on. CONCLUSIONS: From our perspective, after structural modification curcumin could be more effective complementary product for cancer therapies by the enhancement of targeting abilities and the improvement of bioavailability.


Asunto(s)
Colorantes/metabolismo , Colorantes/farmacología , Curcumina/metabolismo , Curcumina/farmacología , Antineoplásicos , Disponibilidad Biológica , Muerte Celular/efectos de los fármacos , Terapias Complementarias , Curcumina/química , Humanos , Neoplasias/tratamiento farmacológico , Microambiente Tumoral/efectos de los fármacos
16.
Fitoterapia ; 140: 104441, 2020 Jan.
Artículo en Inglés | MEDLINE | ID: mdl-31778760

RESUMEN

In the present work, we reported the triterpenoids isolated from n-butanol fraction of Kadsura heteroclita which is a Tujia ethnomedicine with trivial name "Xuetong". This effort resulted in the isolation of six unpresented triterpenoids xuetongsu A-F (1-6), along with five known triterpenoids (7-11). The structures of the reported compounds were established on the 1D, and 2D NMR and HRESIMS spectra, along with CD spectroscopic analysis. Moreover, the absolute stereochemistry of compound 7 was determined by X-ray diffraction analysis. Antioxidant and cytotoxic activities were evaluated for all isolated compounds, compound 7 shown weak cytotoxic activity against HL-60 with IC50 value of 50.0 µM.


Asunto(s)
Kadsura/química , Tallos de la Planta/química , Triterpenos/química , China , Células HL-60 , Humanos , Estructura Molecular , Fitoquímicos/química , Fitoquímicos/aislamiento & purificación , Triterpenos/aislamiento & purificación
17.
Molecules ; 24(9)2019 Apr 28.
Artículo en Inglés | MEDLINE | ID: mdl-31035334

RESUMEN

As part of our continual efforts to exploit 'Tujia Ethnomedicine' for their pharmacophoric functionalities, we herein investigated Kadsura heteroclita collected from a deep Wulin mountain area in northern Hunan province. The current study resulted in the isolation of three new sesquiterpenes: 6α,9α,15-trihydroxycadinan-4-en-3-one (1), (+)-3,11,12-trihydroxycalamenene (2), (-)-3,10,11,12-tetrahydroxy-calamenene (3), along with four known sesquiterpenes (4-7), and a cytochalasin H (8). Their chemical structures were elucidated by 1D-, and 2D-NMR spectroscopy, and HRESI-MS, CD spectrometry. The antioxidant, and cytotoxic activities of the compounds were evaluated. Compound 8 exhibited a strong antioxidant effect with an IC50 value of 3.67 µM on isolated human polymorphonuclear cells or neutrophils.


Asunto(s)
Kadsura/química , Extractos Vegetales/química , Tallos de la Planta/química , Sesquiterpenos/química , Antioxidantes/química , Antioxidantes/aislamiento & purificación , Antioxidantes/farmacología , Línea Celular Tumoral , Supervivencia Celular/efectos de los fármacos , Humanos , Espectroscopía de Resonancia Magnética , Modelos Moleculares , Estructura Molecular , Extractos Vegetales/aislamiento & purificación , Extractos Vegetales/farmacología , Sesquiterpenos Policíclicos , Sesquiterpenos/aislamiento & purificación , Sesquiterpenos/farmacología
18.
Sheng Li Xue Bao ; 71(2): 235-247, 2019 Apr 25.
Artículo en Chino | MEDLINE | ID: mdl-31008483

RESUMEN

Vascular remodeling is a significant pathological characteristic of hypertension, which is regulated by complex regulatory networks. The vascular remodeling may be adaptive initially, however it becomes maladaptive and decompensation eventually and further compromises target organ function, leading to hypertensive cardiovascular complications. This review focuses on the role and mechanisms of vascular remodeling in the pathogenesis and progression of hypertension and its complications. Moreover, the strategies of syndrome differentiation of traditional Chinese medicine application provide clinical and theoretical evidences for hypertensive vascular remodeling therapy. A better understanding of underlying signaling pathways, therapeutic targets in vascular remodeling, as well as screening of active ingredients from traditional Chinese medicine may be able to provide some effective approaches for vascular protection in hypertensive diseases.


Asunto(s)
Hipertensión/fisiopatología , Hipertensión/terapia , Medicina Tradicional China , Remodelación Vascular , Humanos , Transducción de Señal
19.
Zhongguo Zhong Yao Za Zhi ; 44(3): 509-517, 2019 Feb.
Artículo en Chino | MEDLINE | ID: mdl-30989916

RESUMEN

Idiosyncratic hepatotoxicity of Polygonum multiflorum has attracted a great attention in the world. The most toxic part of idiosyncratic hepatotoxicity was screened by MTT assay and flow cytometry, which was the 50% ethanol elute by macroporous adsorptive resins from alcohol-extraction of P. multiflorum. The fingerprints were collected by HPLC from 50% ethanol elute of crude and processed P. multiflorum from different habitats, then 14 common peaks were determined. Spectrum-toxicity relationship was analyzed by rough set theory(RST). Two main chemical components were predicted for idiosyncratic hepatotoxicity, in which TSG was the greater contributor. Idiosyncratic hepatotoxicity of TSG was tested in vitro, and the results indicated that TSG was the most important constituent contributed to idiosyncratic hepatotoxicity of P. multiflorum. The study showed the discovery of the main chemical components for idiosyncratic hepatotoxicity, and RST was effective for analyzing the spectrum-toxicity relationship, which could be a new method used in the effective/toxic constituents field of traditional Chinese medicine.


Asunto(s)
Enfermedad Hepática Inducida por Sustancias y Drogas , Medicamentos Herbarios Chinos/efectos adversos , Fallopia multiflora/química , Fitoquímicos/efectos adversos , Cromatografía Líquida de Alta Presión , Humanos , Medicina Tradicional China
20.
Biochem Pharmacol ; 163: 1-8, 2019 05.
Artículo en Inglés | MEDLINE | ID: mdl-30703351

RESUMEN

Depression is highly prevalent in patients suffering from chronic inflammatory diseases. Dysregulated neuroinflammation and concomitant activated microglia play a pivotal role in the pathogenesis of depression. Paricalcitol (Pari), a vitamin D2 analogue, has been demonstrated to exert anti-inflammative effects on renal and cardiovascular diseases. In this study, mice were pretreated with Pari before being induced to acute depression-like behaviors by systemic lipopolysaccharide (LPS) injection. To determine the therapeutic effects of Pari, alterations in acute body weight, sucrose preference, forced swimming and tail suspension tests were assessed. Then, alterations of pro-inflammation cytokine IL1-ß level and microglia activity in the hypothalamus, which are involved in the pathophysiology of depression, were examined. The results showed that Pari significantly alleviated systemic LPS injection induced depressive-like behaviors as shown by increased sucrose preference and decreased TST and FST immobility. Pari could specifically regulate microglia-mediated neuroinflammation process and local activity of renin-angiotensin system to exert its anti-depressant effects. This study demonstrated a potential for paricalcitol in treating depressive symptoms induced by systemic inflammation, particularly in patients with chronic hypertension.


Asunto(s)
Antidepresivos/uso terapéutico , Depresión/tratamiento farmacológico , Ergocalciferoles/uso terapéutico , Hipotálamo/efectos de los fármacos , Mediadores de Inflamación/antagonistas & inhibidores , Lipopolisacáridos/toxicidad , Microglía/efectos de los fármacos , Animales , Antidepresivos/farmacología , Depresión/inducido químicamente , Depresión/metabolismo , Ergocalciferoles/farmacología , Hipotálamo/metabolismo , Inflamación/tratamiento farmacológico , Inflamación/metabolismo , Mediadores de Inflamación/metabolismo , Masculino , Ratones , Ratones Endogámicos C57BL , Microglía/metabolismo
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