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1.
Adv Mater ; 36(24): e2311591, 2024 Jun.
Artículo en Inglés | MEDLINE | ID: mdl-38426690

RESUMEN

2D van der Waals (vdW) magnets open landmark horizons in the development of innovative spintronic device architectures. However, their fabrication with large scale poses challenges due to high synthesis temperatures (>500 °C) and difficulties in integrating them with standard complementary metal-oxide semiconductor (CMOS) technology on amorphous substrates such as silicon oxide (SiO2) and silicon nitride (SiNx). Here, a seeded growth technique for crystallizing CrTe2 films on amorphous SiNx/Si and SiO2/Si substrates with a low thermal budget is presented. This fabrication process optimizes large-scale, granular atomic layers on amorphous substrates, yielding a substantial coercivity of 11.5 kilo-oersted, attributed to weak intergranular exchange coupling. Field-driven Néel-type stripe domain dynamics explain the amplified coercivity. Moreover, the granular CrTe2 devices on Si wafers display significantly enhanced magnetoresistance, more than doubling that of single-crystalline counterparts. Current-assisted magnetization switching, enabled by a substantial spin-orbit torque with a large spin Hall angle (85) and spin Hall conductivity (1.02 × 107 ℏ/2e Ω⁻¹ m⁻¹), is also demonstrated. These observations underscore the proficiency in manipulating crystallinity within integrated 2D magnetic films on Si wafers, paving the way for large-scale batch manufacturing of practical magnetoelectronic and spintronic devices, heralding a new era of technological innovation.

2.
Int Immunopharmacol ; 123: 110572, 2023 Oct.
Artículo en Inglés | MEDLINE | ID: mdl-37572501

RESUMEN

Postmenopausal osteoporosis, a chronic condition that predominantly affects postmenopausal women, presents a significant impediment to their overall well-being. The condition arises from estrogen deficiency, leading to enhanced osteoclast activity. Salvia miltiorrhiza, a well-established Chinese herbal medicine with a history of clinical use for osteoporosis treatment, contains diverse active constituents that have shown inhibitory effects on osteoclast formation and bone loss. Dihydrotanshinone I (DTI), a phenanthrenonequinone compound derived from the root of Salvia miltiorrhiza, has been identified as a potential therapeutic agent, although its mechanism of action on osteoclasts remains elusive. In this study, we aimed to elucidate the inhibitory potential of DTI on RANKL-induced osteoclastogenesis. We observed the ability of DTI to effectively impede the expression of key osteoclast-specific genes and proteins, as assessed by Real-time PCR and Western Blotting analyses. Mechanistically, DTI exerted its inhibitory effects on osteoclast formation by modulating critical signaling pathways including NF-κB, ERK, and calcium ion signaling. Notably, DTI intervention disrupted the nuclear translocation and subsequent transcriptional activity of the NFATc1, thus providing mechanistic insights into its inhibitory role in osteoclastogenesis. To further assess the therapeutic potential of DTI, we employed an ovariectomized osteoporosis animal model to examine its impact on bone loss. Encouragingly, DTI demonstrated efficacy in mitigating bone loss induced by estrogen deficiency. In conclusion, our investigation elucidates the ability of DTI to regulate multiple signaling pathways activated by RANKL, leading to the inhibition of osteoclast formation and prevention of estrogen-deficiency osteoporosis. Consequently, DTI emerges as a promising candidate for the treatment of osteoporosis.


Asunto(s)
Resorción Ósea , Osteoporosis , Animales , Femenino , Humanos , Resorción Ósea/prevención & control , Diferenciación Celular , Estrógenos/deficiencia , Estrógenos/metabolismo , FN-kappa B/metabolismo , Factores de Transcripción NFATC/genética , Factores de Transcripción NFATC/metabolismo , Osteoclastos , Osteogénesis , Osteoporosis/metabolismo , Ligando RANK/metabolismo , Transducción de Señal
3.
Molecules ; 28(13)2023 Jul 07.
Artículo en Inglés | MEDLINE | ID: mdl-37446941

RESUMEN

When added to mushroom growing substrates, edible and medicinal herbs affect the mushrooms' nutritional and medicinal value. In this study, polysaccharides (P0OP-I and P15OP-I) were extracted and purified from oyster mushrooms grown on substrates supplemented with 0% and 15% Astragalus roots (P0 and P15), respectively, and their chemical structure and immunobiological activities were compared. P15OP-I and P0OP-I were extracted using ultrasound-assisted hot water and deproteinized with the Sevage method, depigmented with 30% H2O2, desalted with dialysis, and purified using DEAE-52 cellulose and Sephadex G-100 dextran column chromatography. The molecular weight of P0OP-I and P15OP-I was 21,706.96 and 20,172.65 Da, respectively. Both were composed of monosaccharides D-mannose, galacturonic acid, D-glucose, D-galactose, and L-arabinose but in different molar ratios, and both were connected by a pyranoside linkage. P15OP-I consisted of higher contents of mannose, glucose, galactose and arabinose and lower content of galacturonic acid as compared to P0OP-I. Both P0OP-I and P15OP-I induced NO and TNF-α production but did not show cytotoxic effect or induce ROS generation in RAW264.7 cells. P15OP-I showed a stronger ability to promote NO and TNF-α production relative to P0OP-I. In vitro experiments showed that the immunomodulatory activity of P0OP-I and P15OP-I in RAW264.7 macrophages were mediated by the JNK/MAPK, Erk/MAPK, and NF-κB signaling pathways. The results would be helpful for elucidation of the health promoting mechanism of Astragalus oyster mushrooms as a source of neutraceuticals.


Asunto(s)
Planta del Astrágalo , Pleurotus , Pleurotus/química , Factor de Necrosis Tumoral alfa , Peróxido de Hidrógeno , Diálisis Renal , Polisacáridos/farmacología , Polisacáridos/química , Planta del Astrágalo/química
4.
Phytother Res ; 37(9): 3898-3912, 2023 Sep.
Artículo en Inglés | MEDLINE | ID: mdl-37132081

RESUMEN

Liver fibrosis is a key global health care burden. Sclareol, isolated from Salvia sclarea, possesses various biological activities. Its effect on liver fibrosis remains unknown. This study was proposed to evaluate the antifibrotic activity of sclareol (SCL) and explore its underlying mechanisms. Stimulated hepatic stellate cells served as an in vitro liver fibrosis model. The expression of fibrotic markers was assessed by western blot and real-time PCR. Two classical animal models, bile duct-ligated rats and carbon tetrachloride-treated mice, were utilized for the in vivo experiments. The liver function and fibrosis degree were determined by serum biochemical and histopathological analyses. VEGFR2 SUMOylation was analyzed using coimmunoprecipitation assay. Our results indicated that SCL treatment restricted the profibrotic propensity of activated HSCs. In fibrotic rodents, SCL administration alleviated hepatic injury and reduced collagen accumulation. Mechanistic studies indicated that SCL downregulated the protein level of SENP1 and enhanced VEGFR2 SUMOylation in LX-2 cells, which affected its intracellular trafficking. Blockade of the interaction between VEGFR2 and STAT3 was observed, resulting in the suppression of downstream STAT3 phosphorylation. Our findings demonstrated that SCL has therapeutic efficacy against liver fibrosis through mediating VEGFR2 SUMOylation, suggesting that SCL may be a potential candidate compound for its treatment.


Asunto(s)
Cirrosis Hepática , Sumoilación , Ratas , Ratones , Animales , Cirrosis Hepática/tratamiento farmacológico , Hígado , Transducción de Señal , Fibrosis , Células Estrelladas Hepáticas
5.
J Pharm Anal ; 12(4): 664-682, 2022 Aug.
Artículo en Inglés | MEDLINE | ID: mdl-36105162

RESUMEN

XueBiJing is an intravenous five-herb injection used to treat sepsis in China. The study aimed to develop a liquid chromatography-tandem mass spectrometry (LC-MS/MS)- or liquid chromatography-ultraviolet (LC-UV)-based assay for quality evaluation of XueBiJing. Assay development involved identifying marker constituents to make the assay therapeutically relevant and building a reliable one-point calibrator for monitoring the various analytes in parallel. Nine marker constituents from the five herbs were selected based on XueBiJing's chemical composition, pharmacokinetics, and pharmacodynamics. A selectivity test (for "similarity of response") was developed to identify and minimize interference by non-target constituents. Then, an intercept test was developed to fulfill "linearity through zero" for each analyte (absolute ratio of intercept to C response, <2%). Using the newly developed assays, we analyzed samples from 33 batches of XueBiJing, manufactured over three years, and found small batch-to-batch variability in contents of the marker constituents (4.1%-14.8%), except for senkyunolide I (26.5%).

6.
Zhongguo Zhong Yao Za Zhi ; 47(8): 2134-2147, 2022 Apr.
Artículo en Chino | MEDLINE | ID: mdl-35531729

RESUMEN

An UPLC-Q-TOF-MS method was employed to characterize and classify the chemical components of the standard decoction of Yiguanjian, a classical famous recipe. Chromatographic separation was performed on an Acquity HSS T3(2.1 mm ×100 mm, 1.8 µm) column with a mobile phase of 0.1% formic acid water-0.1% formic acid acetonitrile using gradient elution. The flow rate was 0.4 mL·min~(-1) and the column temperature was 40 ℃. Mass spectrometry was performed on electrospray ionization source(ESI) with positive and negative ion scanning modes. The potential compounds were identified by comparing the reference compounds, analyzing the mass spectrometry data and matching the published articles on Masslynx 4.1 software and SciFinder database. Finally, a total of 113 compounds, including 11 amino acids, 19 terpenoids, 13 phthalides, 11 steroidal saponins, 10 coumarins, 9 alkaloids, 7 flavonoids, 8 phenylethanoid glycosides, 8 organic acids and 17 other categories were identified. The established method systematically and accurately characterized the chemical components in Yiguanjian, which could provide experimental evidences for the subsequent studies on the pharmacodynamical material basis and quality control of Yiguanjian.


Asunto(s)
Medicamentos Herbarios Chinos , Cromatografía Líquida de Alta Presión , Medicamentos Herbarios Chinos/química , Flavonoides/análisis , Formiatos , Glicósidos/análisis , Prescripciones
7.
Artículo en Chino | WPRIM | ID: wpr-955479

RESUMEN

XueBiJing is an intravenous five-herb injection used to treat sepsis in China.The study aimed to develop a liquid chromatography-tandem mass spectrometry(LC-MS/MS)-or liquid chromatography-ultraviolet(LC-UV)-based assay for quality evaluation of XueBiJing.Assay development involved identifying marker constituents to make the assay therapeutically relevant and building a reliable one-point cali-brator for monitoring the various analytes in parallel.Nine marker constituents from the five herbs were selected based on XueBiJing's chemical composition,pharmacokinetics,and pharmacodynamics.A selectivity test(for"similarity of response")was developed to identify and minimize interference by non-target constituents.Then,an intercept test was developed to fulfill"linearity through zero"for each analyte(absolute ratio of intercept to C response,<2%).Using the newly developed assays,we analyzed samples from 33 batches of XueBiJing,manufactured over three years,and found small batch-to-batch variability in contents of the marker constituents(4.1%-14.8%),except for senkyunolide I(26.5%).

8.
Carbohydr Polym ; 254: 117189, 2021 Feb 15.
Artículo en Inglés | MEDLINE | ID: mdl-33357839

RESUMEN

The incidence of ulcerative colitis (UC) is high. Despite the availability of various therapeutic agents for the treatment of UC, the routine treatment has limitations and serious side effects. Therefore, a new drug that safely and effectively treats UC is urgently needed. Polysaccharides from natural resources have recently become a hot topic of study for their therapeutic effects on UC. These effects are associated with the regulation of inflammatory cytokines, intestinal flora, and immune system and protection of the intestinal mucosa. This review focuses on the recent advances of polysaccharides from natural resources in the treatment of UC. The mechanisms and practicability of polysaccharides, including pectin, guar gum, rhamnogalacturonan, chitosan, fructan, psyllium, glycosaminoglycan, algal polysaccharides, polysaccharides from fungi and traditional Chinese medicine, and polysaccharide derivatives, are discussed in detail. The good efficacy and safety of polysaccharides make them promising drugs for treating UC.


Asunto(s)
Colitis Ulcerosa/tratamiento farmacológico , Medicina Tradicional China , Polisacáridos/uso terapéutico , Productos Biológicos/química , Productos Biológicos/aislamiento & purificación , Productos Biológicos/uso terapéutico , Colitis Ulcerosa/inmunología , Colitis Ulcerosa/microbiología , Medicamentos Herbarios Chinos/química , Medicamentos Herbarios Chinos/aislamiento & purificación , Medicamentos Herbarios Chinos/uso terapéutico , Microbioma Gastrointestinal , Humanos , Estructura Molecular , Polisacáridos/química , Polisacáridos/aislamiento & purificación
9.
Front Pharmacol ; 11: 1036, 2020.
Artículo en Inglés | MEDLINE | ID: mdl-32848725

RESUMEN

ETHNOPHARMACOLOGICAL RELEVANCE: In Traditional Chinese medicine (TCM) theory, ulcerative colitis (UC) is associated with damp-heat, blood stasis, and intestinal vascular ischemia. Kuijieyuan decoction (KD) is a traditional Chinese medicine based on the above theory and used clinically to alleviate UC injury. METHODS: The main components of KD were analyzed by using high-pressure liquid chromatography (HPLC) and confirmed by UPLC-MS/MS. A UC model was established in rats by using dextran sulfate sodium (DSS) and dead rats (caused by DSS) were excluded from the study. Forty-eight rats were divided into 6 groups, health control (CG), UC model (UG), sulfasalazine (SG), low-dose KD (LG), middle-dose KD (MG), and high-dose KD (HG) groups. UC damage was assessed by hematoxylin and eosin staining and scan electron microscopy. We measured Toll-like receptor 4 (TLR4), p-phosphatidylinositol 3-kinase (PI3K), PI3K, p-Protein kinase B (AKT), AKT, p-nuclear factor kappa B (NF-κB), NF-κB, oxidative stress marker (superoxidase dismutase (SOD), catalase (CAT), glutathione peroxidases (GPx), and malondialdehyde) and inflammatory markers (tumor necrosis factor α (TNFα), interleukin (IL)-1, IL-6 and IL-10) in UC tissues. Gut microbiota was analyzed through16S rRNA sequencing. RESULTS: The main components of KD consist of gallic acid, paeoniflorin, emodin, berberine, coptisine, palmatine, jatrorrhizine, baicalein and baicalin. The UC model was successfully established by causing intestinal barrier injury with the loss of intestinal villi and destructed mitochondria of intestinal epithelial cells. Both sulfasalazine and KD treatment repaired UC injury, reduced the levels of malondialdehyde, TNFα, IL-1, IL-6, TLR4, p-PI3K, p-AKT, and p-NF-κB, and increased the levels of SOD, GPx, CAT, and IL-10. KD showed a protective function for the UC model in a dose-dependent way. The serum levels of paeoniflorin and baicalin had a strong relationship with the levels of inflammatory and oxidative stress biomarkers. KD treatment increased the proportion of Alloprevotella, Treponema, Prevotellaceae, and Prevotella, and reduced the proportion of Escherichia_Shigella and Desulfovibrio in gut microbiota. CONCLUSIONS: KD improved intestinal barrier injury of ulcerative colitis, antioxidant and anti-inflammatory properties by affecting TLR4-dependent PI3K/AKT/NF-κB signaling possibly through the combination of its main compounds, and improving gut microbiota.

10.
Int J Phytoremediation ; 22(11): 1156-1167, 2020.
Artículo en Inglés | MEDLINE | ID: mdl-32202138

RESUMEN

The seed germination plant growth parameters and level of heavy metal accumulation were investigated in pakchoi cultured in four contaminated soils with different levels of heavy metals supplemented with citric acid (CA) or calcium phosphate (CP). Results showed that the seed germination energy, germination percentage and germination index parameters were similar, while the seed vigor (SV) significantly (p < 0.05) decreased as the soil pollution level increased. The lengths of the shoots and roots presented the same trend as SV. All the seedlings grew in heavily polluted soil without any amendments before harvesting; therefore, no plant material was available for subsequent analyses. The photosynthesis parameters of pakchoi cultured in lightly polluted soil without amendment (LPS), lightly polluted soil with CA (LPSA) and moderately polluted soil with CP (MPSP) were similar. The concentrations of Pb, Zn, Mn, Cu and Cd in the shoots, roots and whole plants were in the order of MPSP > LPSA > LPS. Pakchoi cultured in MPSP showed the most promising results in terms of plant height, biomass and heavy metal accumulation. Pakchoi presented the highest translocation and bioaccumulation factors for Cd and the lowest for Pb.HighlightsSoil pollution and the type of chemical amendment had no effect on the seed germination of pakchoi.Citric acid addition in lightly polluted soil improved pakchoi growth and heavy metal extraction.Pakchoi cultured in moderately polluted soil with calcium phosphate amendment presented the highest biomass and heavy metal concentration.


Asunto(s)
Metales Pesados/análisis , Contaminantes del Suelo/análisis , Biodegradación Ambiental , Germinación , Semillas , Suelo
11.
J Ethnopharmacol ; 253: 112658, 2020 May 10.
Artículo en Inglés | MEDLINE | ID: mdl-32035876

RESUMEN

ETHNOPHARMACOLOGICAL RELEVANCE: Many bioactive constituents of Chinese herbal medicines have poor oral bioavailability. Besides oral administration, herbal medicines in China are also prepared for parenteral administration. Unlike for intravenous route, little is known about the intramuscular pharmacokinetics of herbal compounds. To facilitate rational use of herbal medicine, it is important to better understand such intramuscular pharmacokinetics. AIM OF THE STUDY: Bioactive constituents of XueShuanTong (a lyophilized extract of Panax notoginseng roots, extensively used in treatment of ischemic heart and cerebrovascular diseases) predominantly comprise ginsenosides Rb1 and Rd of 20(S)-protopanaxadiol-type and ginsenosides Rg1, and Re, and notoginsenoside R1 of 20(S)-protopanaxatriol-type; these saponins are poorly absorbed from the gastrointestinal tract. This study aimed to compare intramuscular and intravenous pharmacokinetics of these ginsenosides after dosing XueShuanTong. METHODS: Pharmacokinetics of ginsenosides was assessed in human volunteers receiving an intramuscular injection or 1.5-h intravenous infusion of XueShuanTong, both at 150 mg/person, and the plasma and urine samples were analyzed by liquid chromatography/mass spectrometry. RESULTS: Like after intravenous administration, the unchanged saponins were the major circulating forms after intramuscular administration, while their metabolites were poorly detected. These ginsenosides exhibited intramuscular bioavailability of 100%-112%, relative to the respective intravenous data. Similar to that after intravenous infusion, the 20(S)-protopanaxadiol-type ginsenosides after the intramuscular injection exhibited notably longer terminal half-lives (46-106 h) than the 20(S)-protopanaxatriol-type ginsenosides (1.1-1.4 h). CONCLUSIONS: Intramuscular route might be an effective alternative to intravenous route for XueShuanTong, from the pharmacokinetic perspective.


Asunto(s)
Medicamentos Herbarios Chinos/farmacocinética , Ginsenósidos/metabolismo , Administración Intravenosa , Adulto , Medicamentos Herbarios Chinos/administración & dosificación , Liofilización , Humanos , Inyecciones Intramusculares , Masculino , Panax notoginseng , Raíces de Plantas , Adulto Joven
12.
Acta Pharmacol Sin ; 40(10): 1351-1363, 2019 Oct.
Artículo en Inglés | MEDLINE | ID: mdl-31358899

RESUMEN

XueShuanTong, a lyophilized extract of Panax notoginseng roots (Sanqi) for intravenous administration, is extensively used as add-on therapy in the treatment of ischemic heart and cerebrovascular diseases and comprises therapeutically active ginsenosides. Potential for XueShuanTong-drug interactions was determined; the investigation focused on cytochrome P450 (CYP)3A induction and organic anion-transporting polypeptide (OATP)1B inhibition. Ginsenosides considerably bioavailable for drug interactions were identified by dosing XueShuanTong in human subjects and their interaction-related pharmacokinetics were determined. The CYP3A induction potential was determined by repeatedly dosing XueShuanTong for 15 days in human subjects and by treating cryopreserved human hepatocytes with circulating ginsenosides; midazolam served as a probe substrate. Joint inhibition of OATP1B by XueShuanTong ginsenosides was assessed in vitro, and the data were processed using the Chou-Talalay method. Samples were analyzed by liquid chromatography/mass spectrometry. Ginsenosides Rb1, Rd, and Rg1 and notoginsenoside R1 were the major circulating XueShuanTong compounds; their interaction-related pharmacokinetics comprised compound dose-dependent levels of systemic exposure and, for ginsenosides Rb1 and Rd, long terminal half-lives (32‒57 and 58‒307 h, respectively) and low unbound fractions in plasma (0.8%‒2.9% and 0.4%‒3.0%, respectively). Dosing XueShuanTong did not induce CYP3A. Based on the pharmacokinetics and inhibitory potency of the ginsenosides, XueShuanTong was predicted to have high potential for OATP1B3-mediated drug interactions (attributed chiefly to ginsenoside Rb1) suggesting the need for further model-based determination of the interaction potential for XueShuanTong and, if necessary, a clinical drug interaction study. Increased awareness of ginsenosides' pharmacokinetics and XueShuanTong-drug interaction potential will help ensure the safe use of XueShuanTong and coadministered synthetic drugs.


Asunto(s)
Citocromo P-450 CYP3A/biosíntesis , Medicamentos Herbarios Chinos/farmacocinética , Ginsenósidos/farmacocinética , Transportador 1 de Anión Orgánico Específico del Hígado/antagonistas & inhibidores , Raíces de Plantas/química , Administración Intravenosa , Adulto , Cromatografía Liquida , Composición de Medicamentos , Interacciones Farmacológicas , Medicamentos Herbarios Chinos/administración & dosificación , Medicamentos Herbarios Chinos/química , Femenino , Ginsenósidos/administración & dosificación , Ginsenósidos/química , Voluntarios Sanos , Hepatocitos/efectos de los fármacos , Hepatocitos/metabolismo , Humanos , Transportador 1 de Anión Orgánico Específico del Hígado/metabolismo , Masculino , Espectrometría de Masas , Conformación Molecular , Adulto Joven
13.
Acta Pharmacol Sin ; 40(6): 833-849, 2019 Jun.
Artículo en Inglés | MEDLINE | ID: mdl-30327544

RESUMEN

ShenMai, an intravenous injection prepared from steamed Panax ginseng roots (Hongshen) and Ophiopogon japonicus roots (Maidong), is used as an add-on therapy for coronary artery disease and cancer; saponins are its bioactive constituents. Since many saponins inhibit human organic anion-transporting polypeptides (OATP)1B, this investigation determined the inhibition potencies of circulating ShenMai saponins on the transporters and the joint potential of these compounds for ShenMai-drug interaction. Circulating saponins and their pharmacokinetics were characterized in rats receiving a 30-min infusion of ShenMai at 10 mL/kg. Inhibition of human OATP1B1/1B3 and rat Oatp1b2 by the individual saponins was investigated in vitro; the compounds' joint inhibition was also assessed in vitro and the data was processed using the Chou-Talalay method. Plasma protein binding was assessed by equilibrium dialysis. Altogether, 49 saponins in ShenMai were characterized and graded into: 10-100 µmol/day (compound doses from ShenMai; 7 compounds), 1-10 µmol/day (17 compounds), and <1 µmol/day (25 compounds, including Maidong ophiopogonins). After dosing, circulating saponins were protopanaxadiol-type ginsenosides Rb1, Rb2, Rc, Rd, Ra1, Rg3, Ra2, and Ra3, protopanaxatriol-type ginsenosides Rg1, Re, Rg2, and Rf, and ginsenoside Ro. The protopanaxadiol-type ginsenosides exhibited maximum plasma concentrations of 2.1-46.6 µmol/L, plasma unbound fractions of 0.4-1.0% and terminal half-lives of 15.6-28.5 h (ginsenoside Rg3, 1.9 h), while the other ginsenosides exhibited 0.1-7.7 µmol/L, 20.8-99.2%, and 0.2-0.5 h, respectively. The protopanaxadiol-type ginsenosides, ginsenosides without any sugar attachment at C-20 (except ginsenoside Rf), and ginsenoside Ro inhibited OATP1B3 more potently (IC50, 0.2-3.5 µmol/L) than the other ginsenosides (≥22.6 µmol/L). Inhibition of OATP1B1 by ginsenosides was less potent than OATP1B3 inhibition. Ginsenosides Rb1, Rb2, Rc, Rd, Ro, Ra1, Re, and Rg2 likely contribute the major part of OATP1B3-mediated ShenMai-drug interaction potential, in an additive and time-related manner.


Asunto(s)
Medicamentos Herbarios Chinos/farmacocinética , Ginsenósidos/farmacocinética , Transportador 1 de Anión Orgánico Específico del Hígado/antagonistas & inhibidores , Miembro 1B3 de la Familia de los Transportadores de Solutos de Aniones Orgánicos/antagonistas & inhibidores , Administración Intravenosa , Animales , Combinación de Medicamentos , Interacciones Farmacológicas , Medicamentos Herbarios Chinos/administración & dosificación , Medicamentos Herbarios Chinos/química , Medicamentos Herbarios Chinos/metabolismo , Ginsenósidos/administración & dosificación , Ginsenósidos/sangre , Ginsenósidos/metabolismo , Humanos , Transportador 1 de Anión Orgánico Específico del Hígado/metabolismo , Masculino , Ophiopogon/química , Panax/química , Unión Proteica , Ratas Sprague-Dawley , Miembro 1B3 de la Familia de los Transportadores de Solutos de Aniones Orgánicos/metabolismo
14.
Acta Pharmacol Sin ; 39(12): 1935-1946, 2018 Dec.
Artículo en Inglés | MEDLINE | ID: mdl-30054600

RESUMEN

Terpene lactones are a class of bioactive constituents of standardized preparations of Ginkgo biloba leaf extract, extensively used as add-on therapies in patients with ischemic cardiovascular and cerebrovascular diseases. This investigation evaluated human pharmacokinetics of ginkgo terpene lactones and impact of their carboxylation in blood. Human subjects received oral YinXing-TongZhi tablet or intravenous ShuXueNing, two standardized ginkgo preparations. Their plasma protein-binding and platelet-activating factor antagonistic activity were assessed in vitro. Their carboxylation was assessed in phosphate-buffered saline (pH 7.4) and in human plasma. After dosing YinXing-TongZhi tablet, ginkgolides A and B and bilobalide exhibited significantly higher systemic exposure levels than ginkgolides C and J; after dosing ShuXueNing, ginkgolides A, B, C, and J exhibited high exposure levels. The compounds' unbound fractions in plasma were 45-92%. Apparent oral bioavailability of ginkgolides A and B was mostly >100%, while that of ginkgolides C and J was 6-15%. Bilobalide's bioavailability was probably high but lower than that of ginkgolides A/B. Terminal half-lives of ginkgolides A, B, and C (4-7 h) after dosing ShuXueNing were shorter than their respective values (6-13 h) after dosing YinXing-TongZhi tablet. Half-life of bilobalide after dosing the tablet was around 5 h. Terpene lactones were roughly evenly distributed in various body fluids and tissues; glomerular-filtration-based renal excretion was the predominant elimination route for the ginkgolides and a major route for bilobalide. Terpene lactones circulated as trilactones and monocarboxylates. Carboxylation reduced platelet-activating factor antagonistic activity of ginkgolides A, B, and C. Ginkgolide J, bilobalide, and ginkgo flavonoids exhibited no such bioactivity. Collectively, differences in terpene lactones' exposure between the two preparations and influence of their carboxylation in blood should be considered in investigating the relative contributions of terpene lactones to ginkgo preparations' therapeutic effects. The results here will inform rational clinical use of ginkgo preparations.


Asunto(s)
Medicamentos Herbarios Chinos/farmacocinética , Ginkgólidos/farmacocinética , Lactonas/farmacocinética , Factor de Activación Plaquetaria/antagonistas & inhibidores , Adulto , Animales , Fenómenos Bioquímicos/efectos de los fármacos , Medicamentos Herbarios Chinos/química , Femenino , Ginkgo biloba/química , Ginkgólidos/sangre , Ginkgólidos/química , Ginkgólidos/orina , Células HEK293 , Humanos , Lactonas/sangre , Lactonas/química , Lactonas/orina , Masculino , Conejos , Adulto Joven
15.
Zhongguo Zhong Yao Za Zhi ; 42(5): 875-881, 2017 Mar.
Artículo en Chino | MEDLINE | ID: mdl-28994529

RESUMEN

This study has revealed the change of the soil micro-ecology of farmlands, which used for ginseng cultivation, brought by comprehensive soil improvement. The process of soil improvement was described as follows: soil was sterilized using trichloronitromethane, and then perilla seeds were planted. After growing up, the perillas were turned over into the field and fermented, then organic fertilizer was added. Rotary tillages were carried out during the intervals. Physical and chemical properties of treated soil were measured, as well as microbial diversity, which was illustrated using 16s high through-put sequencing. The survival rate and growth data of ginseng seedlings were recorded. The analysis showed that after improvement, the soil organic matter content was increased and soil bulk density was decreased, compare to the controls, and the fertility in 0-20 cm of soil layer was increased in the treatment. Additionally, the soil microbial diversity was changed greatly. In detail, alpha diversity of the soil decreased after soil improvement while the beta diversity increased. In order to verify the achievement of soil improvement, ginseng seedlings were planted. Compared to the untreated land blocks, the survival rate of ginseng on improved blocks was increased up to 21.4%, and the ginseng physiological index were all better than the controls. Results showed that comprehensive soil improvements including soil sterilization, green manure planting and organic fertilization application effectively improved the soil micro-ecology in farmlands. This study will pave the way for the future standardization of ginseng cultivation on farmlands.


Asunto(s)
Agricultura , Panax/crecimiento & desarrollo , Suelo , Fertilizantes , Plantas Medicinales/crecimiento & desarrollo
16.
Zhongguo Zhong Yao Za Zhi ; 42(3): 443-449, 2017 Feb.
Artículo en Chino | MEDLINE | ID: mdl-28952247

RESUMEN

Continuous cropping obstacles resulted in the yield losses of Panax ginseng, and affected the development of ginseng industry. Soil fungal communities participated in the key ecological process, and their changes of diversity and composition were related to the continuous cropping obstacles. We analyzed the changes of fungal diversity and composition in the rhizosphere of ginseng using the high-throughput sequencing method, stated the effects of ginseng cultivation on the micro-ecology, and provided effective strategies for overcoming continuous cropping obstacles. Compared to those of the forest soils, the fungal diversity of ginseng rhizosphere soils was increased, and the increasing trends were declined with an increasing years of ginseng cultivation; the relative abundance of Sordariomycetes, Alatospora, Eurotiomycetes, Leotiomycetes, Saccharomycetes, Mucorales and Pezizomycetes were increased in the rhizosphere of ginseng. Pearson's correlation index indicated that soil chemical perporties affected the relative abundance of fungal communities. pH was significantly related to the relative abundance of Dothideomycetes and Alatospora; the content of available potassium was markedly associated with the relative abundance of Dothideomycetes, Alatospora and Mucorales; the content of total nitrogen was significant correlation with the relative abundance of Sordariomycetes and Mucorales. These results indicated that fertilization was one of pivotal factors affecting the rhizosphere micro-ecology of ginseng, and optimization of fertilization system was an effective method to overcome continuous cropping obstacles.


Asunto(s)
Hongos/clasificación , Panax/microbiología , Rizosfera , Microbiología del Suelo , Agricultura , Raíces de Plantas/microbiología
17.
Molecules ; 22(8)2017 Aug 18.
Artículo en Inglés | MEDLINE | ID: mdl-28820480

RESUMEN

The objectives of this study were to characterize the antioxidant capacities and phytochemicals such as phenolics and flavonoids in four parts of Euphorbia lathyris L. HPLC was employed to detect the type and content of phenolic acids and flavonoids in the root, stem, seed, and testa of the plant. The total phenolic content (TPC) and total flavonoid content (TFC) were different among various parts of E. lathyris. The highest TPC were found in the testa (290.46 ± 15.09 mg of gallic acid equiv/100 g dry weight (DW)). However, the root contained the highest TFC (215.68 ± 3.10 mg of rutin equiv/g DW). Of the different antioxidant activities detected, DPPH free radical scavenging activity was highest in the testa (61.29 ± 0.29 mmol Trolox/100 g DW), but the highest FRAP antioxidant activity was found in the seed (1131.25 ± 58.68 mg FeSO4/100 g DW of free compounds and 1927.43 ± 52.13 mg FeSO4/100 g DW of bound compounds). There was a positive correlation between the total phenolic contents and DPPH free radical scavenging activity in different parts of E. lathyris.


Asunto(s)
Antioxidantes/farmacología , Euphorbia/química , Fenoles/química , Extractos Vegetales/farmacología , Antioxidantes/química , Flavonoides/química , Flavonoides/clasificación , Flavonoides/aislamiento & purificación , Fenoles/farmacología , Fitoquímicos/química , Fitoquímicos/aislamiento & purificación , Fitoquímicos/farmacología , Extractos Vegetales/química , Semillas/química
18.
Trials ; 17: 3, 2016 Jan 04.
Artículo en Inglés | MEDLINE | ID: mdl-26728982

RESUMEN

BACKGROUND: Knee osteoarthritis (KOA) is a major public health issue causing chronic disability as well as a burden on healthcare resources. In China, a herbal drug tablet has been used as an effective and conventional therapy to alleviate clinical symptoms caused by KOA. However, evidence gathered from systematic reviews or randomized controlled trials that validated herbal drugs for the management of osteoarthritic pain is weak. The purpose of this study is to explore the efficacy and safety of the Shaoyao Shujin tablet for the management of KOA in a short-term study. METHODS/DESIGN: This trial is a multicenter randomized, double-blind, placebo-controlled study. A total of 276 patients will be randomized into 3 groups: (1) the high-dose Shaoyao Shujin tablet group (HD group), (2) the low-dose Shaoyao Shujin tablet group (LD group), and (3) the placebo tablet group (control group). In the three groups, four tablets will be administered three times per day for 6 weeks. Follow-up will be at regular intervals during a 10-week period with the Western Ontario and McMaster Universities Index (WOMAC) score, visual analog scale (VAS) score, and rescue medication use assessed as outcome measures. DISCUSSION: This study will provide clinical evidence on the efficacy and safety of the Shaoyao Shujin tablet in treating KOA. TRIAL REGISTRATION: Chinese Cochrane Center ChiCTR-IPR- 15006194 , registered 4 April 2015.


Asunto(s)
Protocolos Clínicos , Medicamentos Herbarios Chinos/uso terapéutico , Osteoartritis de la Rodilla/tratamiento farmacológico , Interpretación Estadística de Datos , Método Doble Ciego , Medicamentos Herbarios Chinos/efectos adversos , Humanos , Evaluación de Resultado en la Atención de Salud , Tamaño de la Muestra , Comprimidos
19.
Zhongguo Zhong Yao Za Zhi ; 41(23): 4334-4339, 2016 Dec.
Artículo en Chino | MEDLINE | ID: mdl-28933108

RESUMEN

This study analysed the changes of the soil micro-ecology in the process of soil sterilization, green manure returning farmlands and fertilization. The methods of soil improvement was initially built which ensured the successful proceed of ginseng cultivation in farmlands. The soil chemical properties were analysed, the diversity and composition of bacterial community after soil sterilization, sterilization+green manure returning farmlands and sterilization+green manure returning farmlands+fertilization. The results exhibited that measures of soil improvement decreased the pH, increased soil fertility, declined the diversity of bacterial community and changed the composition of soil bacterial community. The comprehensive measures of sterilization+green manure returning farmlands+fertilization decreased the ginseng death rate compared to the control. Our data indicated that soil micro-ecological environment was changed by the treatments of soil sterilization, sterilization+green manure returning farmlands and sterilization+green manure returning farmlands+fertilization, and comprehensive measures improved the survival rate and guaranteed the development of ginseng cultivation in farmlands.


Asunto(s)
Agricultura , Panax/crecimiento & desarrollo , Microbiología del Suelo , Suelo/química , Fertilizantes , Estiércol
20.
Trials ; 16: 124, 2015 Mar 28.
Artículo en Inglés | MEDLINE | ID: mdl-25872665

RESUMEN

BACKGROUND: Knee osteoarthritis is a major cause of disability in the aging population. Based on pathological, magnetic resonance imaging (MRI) and arthroscopy studies, progressive osteoarthritis involves all tissues of the joint and includes bone marrow lesions, synovial proliferation, fat pad inflammation, and high subchondral bone turnover. Recent research suggests that abnormal perfusion in bone marrow lesions, fat pads, and subchondral bone is associated with pain in knee osteoarthritis, and that dynamic contrast-enhanced MRI is a promising method for studying micro-perfusion alteration in knee osteoarthritis. Traditional Chinese Medicine approaches have been employed for thousands of years to relieve knee osteoarthritis pain. Among herbal medicines, the Jingui external lotion is the preferred and most commonly used method in China to reduce pain in patients with knee osteoarthritis; however, there is a lack of validated evidence for its effectiveness. The purpose of this study is to explore the effectiveness of Jingui external lotion for the management of painful knee osteoarthritis in a short-term study. In addition, we will assess micro-perfusion alteration in the patellar fat pad as well as the femur and tibia subchondral bone via dynamic contrast-enhanced MRI. METHODS/DESIGN: This trial is a randomized, controlled study. A total of 168 patients will be randomized into the following two groups: 1) the Jingui external lotion group (treatment group); and 2) the placebo lotion group (control group). In both groups, lotion fumigation and external washing of the patients' knees will be administered twice a day for 14 consecutive days. Follow-up will be at regular intervals during a 4-week period with a visual analog scale to assess pain, and additional characterization with the Western Ontario and McMaster Universities Index score; rescue medication will be recorded as the extent and time pattern. In addition, micro-perfusion alteration in the patellar fat pad, femur and tibia subchondral bone will be assessed via dynamic contrast-enhanced MRI. DISCUSSION: This study will provide clinical evidence of the efficacy of Jingui external lotion in treating knee osteoarthritis, and it will be the first randomized controlled trial to investigate micro-perfusion alteration of knee osteoarthritis with Traditional Chinese Medicine external lotion via dynamic contrast-enhanced MRI. TRIAL REGISTRATION: ClinicalTrials.gov identifier: ChiCTR-TRC-14004727 ; 31 May 2014.


Asunto(s)
Medicina Tradicional China , Osteoartritis de la Rodilla/terapia , Fitoterapia , Preparaciones de Plantas/uso terapéutico , Crema para la Piel/uso terapéutico , Protocolos Clínicos , Humanos , Proyectos de Investigación
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