RESUMEN
Ampelopsis delavayana, a distinctive Yi medicine, utilized the roots as an essential medicinal substance for trauma treatment of the "Yunnan Hong Yao". A. delavayana, however, cannot be cultivated artificially presently, and it has been described with a phenomenon of mixed utilization of roots and stems, impeding pharmaceutical quality control. In response to resource scarcity and standardization issues, the research comprehensively compares the material basis and efficacy of medicinal (roots) and non-medicinal (stems) parts by using chemical profiling and pharmacological methodologies. Chemical disparity between two parts was compared by TLC and HPLC. Analgesia and anti-inflammatory capabilities of both parts were comprehensively evaluated through acetic acid writhing test, hot plate test, and xylene-induced mouse ear swelling test. Additionally, all the extracts were evaluated for anti-inflammatory activities by monitoring regulation of the levels of TNF-α, IL-1ß, IL-6, and IgE in ear tissue. Consequently, the findings of TLC and HPLC revealed substantial similarity in the material basis of the medicinal and non-medicinal parts of A. delavayana, and pharmacological activities of anti-inflammatory and analgesic between two parts were consistent. Different extracts remarkably reduced the levels of TNF-α, IL-1ß, IL-6, and IgE, demonstrating no discernible differences. Collectively, the comprehensive exploitation indicated that the medicinal and non-medicinal parts of A. delavayana exhibited identical chemical profiling and bioactivities, providing a theoretical rationale and scientific evidence for using stems as a therapeutic part, thereby holding considerable potential for ameliorating the current status of its medicinal reserves.
RESUMEN
BACKGROUND: Obese asthma is an asthma phenotype that causes more severe lung inflammation and airway hyperresponsiveness than allergic asthma and it is resistant to conventional therapy. Involucrasin B (IB) is a dihydroflavonoid isolated from Shuteria involucrata (Wall.) Wight & Arn., a traditional "Dai" and "Wa" medicine was used in southern China to treat the "phlegm and wetness of sputum" (obesity disease) as well as lung inflammation. However, whether IB can ameliorate obese asthma remains unclear, and the underlying mechanisms and molecular expression in obese asthma specifically targeted by IB are still not fully understood. METHODS: An in vivo C57BL/6 J mouse model of obese asthma was established using house dust mites (HDMs) and high-fat diet (HFD) as inducers to evaluate the therapeutic effect of IB. An in vitro cell culture of human THP-1 monocytic cell culture was used to investigate the effect of IB after the treatment with lipopolysaccharide (LPS) and palmitic acid (PA). RESULTS: In vivo, we found that intervention with IB improved airway hyperresponsiveness and lung histopathology and significantly inhibited the secretion of relevant inflammatory factors, such as interleukin (IL)-1ß, IL-17A, and IL-22 in bronchoalveolar lavage fluid, and total-IgE and HDM-IgE in serum compared with the model group (HFD+HDM). The findings indicate that IB could decrease the expression of granulocyte receptor 1 (Gr-1) and neutrophil extracellular traps (NETs) in lung tissue, as well as the expression of NLR family pyrin domain containing 3 (NLRP3) and inducible nitric oxide synthase in M1 macrophages (M1). IB also reduced the population of ILC3/Th17 cells, which are responsible for producing IL-17A, a crucial mediator of neutrophil-mediated inflammation, confirming that the therapeutic effect of IB in obesity-related asthma was related to neutrophils and M1 cells. In addition, IB regulated lipid metabolism and inhibited the production of macrophages in adipose tissue. The in vitro results revealed that IB inhibited the secretion of IL-1ß, IL-18, and tumor necrosis factor-α (TNF-α) from THP-1 cells, and the expression of NLRP3-related protein in THP-1 cells compared with the model groups (LPS, PA, and LPS+PA), confirming that the action of IB involved the TLR4-NF-κB-NLRP3 pathway. CONCLUSION: This study demonstrated the therapeutic effect of IB in obese asthma for the first time and further clarified its mechanistic pathway as the TLR4-NF-κB-NLRP3 pathway.
Asunto(s)
Asma , Ratones Endogámicos C57BL , FN-kappa B , Proteína con Dominio Pirina 3 de la Familia NLR , Obesidad , Receptor Toll-Like 4 , Animales , Asma/tratamiento farmacológico , Proteína con Dominio Pirina 3 de la Familia NLR/metabolismo , Humanos , Obesidad/tratamiento farmacológico , FN-kappa B/metabolismo , Receptor Toll-Like 4/metabolismo , Ratones , Modelos Animales de Enfermedad , Masculino , Células THP-1 , Lipopolisacáridos , Dieta Alta en Grasa , Transducción de Señal/efectos de los fármacos , Pulmón/efectos de los fármacos , Pyroglyphidae , Inflamación/tratamiento farmacológicoRESUMEN
Background: As one of the most common gynecological disorders, PD significantly impacts the quality of life for women. TSD, a well-known traditional Chinese medical prescription, has gained popularity for its use in treating gynecological cold coagulation and blood stasis syndromes such as PD. However, the lack of comprehensive data hinders our understanding of its molecular mechanism. Purpose: The objective of the present study is to investigate the therapeutic effects of TSD on PD and elucidate its plausible mechanism. Methods: HPLC was employed to confirm the presence of the principal metabolites of TSD. The rat model of PD was induced by OT exposure following IWM and EB pretreatment, and subsequently treated with TSD via gastric gavage. The effects and potential mechanisms of TSD on PD rats were explored, encompassing general behavior, morphological alterations in the uterus and ovaries, biochemical indicators in the uterus and serum, and levels of proteins related to the PI3K/AKT signaling pathway. Results: Gallic acid, hydroxysafflower yellow A, albiflorin, paeoniflorin, and ferulic acid were determined to be the primary active metabolites of TSD. The pharmacological studies yielded results indicating the successful establishment of the PD model in rats. Additionally, TSD demonstrated its ability to protect PD rats by ameliorating general behavior, mitigating pathological damage to uterine and ovarian tissues, and modulating the expression levels of correlated factors (PGE2, PGF2α, Ca2+, TXB2, IL-6, TNF-α, NO, and COX-2) as well as p-PI3K/PI3K and p-AKT/AKT proteins. Conclusion: TSD exhibited protective effects against PD in rats through its interaction with multiple targets including P13K/AKT signaling pathway, indicating that TSD holds therapeutic potential for PD treatment and providing evidence supporting the rational utilization of TSD.
RESUMEN
The strategies or drugs for preventing and treating Hyperuricemia (HUA) are still lacking. As a traditional Chinese medicine (TCM) with a profound history, Ampelopsis grossedentata has been shown to play diverse biological roles. The purpose of the present study was to evaluate hypouricemic effect of A. grossedentata, and investigate its involved material basis and mechanism. A HUA mice model was established to evaluate the therapeutic effects of A. grossedentata. And then some extracts from A. grossedentata were prepared, isolated and analyzed. Furthermore, network pharmacology, based on the above results, was used to discover potential active ingredients and therapeutic targets, and they were further verified and explored by molecular docking and in vitro experiments. In vivo experiments showed that A. grossedentata exerted hypouricemic effect on mice of HUA. The core active ingredients (quercetin, myricetin and dihydromyricetin etc.) and core targets (PTGS2, XOD and ABCG2 etc.) for A. grossedentata to treat HUA were predicted by network pharmacology. And molecular docking showed that the spontaneous binding activities of above components and targets were marvelous. In vitro experiments further demonstrated that A. grossedentata exerted hypouricemic effect by decreasing the levels of UA, XOD, antioxidant factors, inflammatory factors, GLUT9 and URAT1 in HK-2 cells of HUA. Taken together, this study integrates multi-level interaction network with in vivo/vitro experiments to systematically reveal the material basis and mechanism of A. grossedentata in treating HUA, which provides a scientific basis for further study of A. grossedentata and HUA.
Asunto(s)
Ampelopsis , Hiperuricemia , Ratones , Animales , Hiperuricemia/tratamiento farmacológico , Ampelopsis/química , Simulación del Acoplamiento Molecular , Estructura Molecular , Antioxidantes/farmacologíaRESUMEN
The bark of Streblus indicus, a Dai medicine in China, has been listed in the Chinese Materia Medica as possessing hemostatic and analgesic properties. Ethnic medicine books record that its bark or leaves for the treatment of mumps and lymphoma. However, according to the literature survey, anti-inflammatory and analgesic studies available for leaves and branches of S. indicus have been seldom reported so far. The current study focuses on the metabolites of S. indicus bark and leaves responsible for anti-inflammatory and analgesic effects on the basis of bioactive-included acetic acid writhing, hot-plate, and xylene-induced ear swelling. The secretion of inflammatory mediators, TNF-α, IL-6, IL-1ß, IL-4, and IL-10, were evaluated for their anti-inflammatory by xylene-induced in mouse ear cells. Histological examination was used to assess the anti-inflammatory and analgesic effects of the branches and leaves of S. indicus, and Western blot analysis determined the mechanism of the methanolic extract of branches and leaves. Different metabolites of S. indicus significantly alleviated analgesic and anti-inflammatory effects, with no discernable differences among them. All metabolites decreased the levels of TNF-α, IL-1ß, and IL-6 and increased the levels of IL-4 and IL-10. The analgesic and anti-inflammatory mechanism of the methanolic extract was related to the NF-kB signaling pathway. These results not only would account for scientific knowledge for the traditional application of S. indicus, but also provide a credible theoretical foundation for the further development of anti-inflammatory and analgesic agents.
RESUMEN
Objective: Swertiamarin (STM) belongs to iridoid class of compounds, and the heat-transformed products (HTPS) are produced by STM in the process of drug processing. The purpose of this study was to explore the protective effect and mechanism of STM or HTPS on acetaminophen (APAP)-induced hepatotoxicity. Methods: Mice and L-O2 cells were given APAP to establish the hepatotoxicity model in vivo and in vitro. The effects of STM or HTPS on oxidative stress, inflammation, and apoptosis induced by APAP were evaluated, with N-acetylcysteine (NAC) as a positive control. Results: STM or HTPS reduced the APAP-induced apoptosis of L-O2 cells and significantly alleviated the liver injury index induced by APAP (p < 0.01, 0.005) Interestingly, HTPS had better protective effect against APAP-induced hepatotoxicity than STM (p < 0.05). In addition STM or HTPS improved the histological abnormalities; inhibited lipid peroxidation and reduced the level of inflammatory mediators. They also activated the defense system of nuclear factor erythroid 2 related factor 2 (Nrf-2) and inhibited nuclear factor-κ B (NF-κB).
RESUMEN
PURPOSE: Music and animation are the most common and affordable distraction strategies to reduce preoperative anxiety in children; however, their effects are inconsistent. This study aimed to examine the effectiveness of two distraction strategies (music or animation) in reducing preoperative anxiety in children. DESIGN AND METHODS: In this randomized controlled trial, 183 children who underwent surgery were divided into music, animation, and control groups using a single-blind block randomized design. Children in the control group underwent routine preoperative visits. Meanwhile, the children in the intervention groups could choose their favorite music and cartoons as intervention content. Study outcomes included anxiety levels, degree of cooperation, heart rate, and blood pressure. Data were collected before entering the operating room, entering the operating room, and before the induction of anesthesia; only the degree of cooperation was collected before the induction of anesthesia. RESULTS: Only animation significantly reduced preoperative anxiety in the children (P < 0.05) upon entering the operating room. Both music and animation reduced the level of preoperative anxiety before induction of anesthesia; however, there was no significant difference between them (P > 0.05). The induction compliance score was significantly lower in the music and animation groups than in the control group (P < 0.05). Heart rates differed significantly between the three groups from before entering the operating room to before induction of anesthesia. Children in the control group had the highest systolic blood pressure upon entering the operating room (P < 0.05). CONCLUSIONS: Music and animation strategies can significantly reduce preoperative anxiety in children and improve surgical cooperation during anesthesia induction. TRIAL REGISTRATION: Clinical. TRIALS: gov NCT05285995.
Asunto(s)
Música , Cuidados Preoperatorios , Niño , Humanos , Método Simple Ciego , Ansiedad/prevención & control , Anestesia GeneralRESUMEN
(±)-Involucrasin C (1), a pair of new 2,3-dihydro-1H-indene enantiomers, along with an enantiomeric analog (2), were isolated from Shuteria involucrata. Their structures were established by the basis of comprehensive spectroscopic data analysis and X-ray crystallographic diffraction. Both 1 and 2 significantly inhibited the secretion of pro-inflammatory cytokines IL-6, TNF-α, and IL-1ß, suggesting that these two natural 2,3-dihydro-1H-indene derivatives may be active components of S.â involucrata and may block inflammation in the initial stage.
Asunto(s)
Indenos , Factor de Necrosis Tumoral alfa , Antiinflamatorios/química , Antiinflamatorios/farmacología , China , Citocinas , Indenos/química , Interleucina-6RESUMEN
This study aims to explore whether selenium (Se) concentration correlates with arseniasis in a high-arsenic coal area in the southern Shaanxi Province, China. Herein, an epidemiological investigation was conducted among 100 arsenic (As)-poisoned patients in Ziyang County, an area with high soil As and Se levels. Fifty healthy subjects were selected from areas without endemic As poisoning. The subjects in the high-As coal area were diagnosed with either normal, suspicious, mild, moderate, or severe As poisoning. Local coal, water, soil, corn, and pepper samples, as well as hair, blood, and urine samples of subjects and patients were collected and analyzed for their As and Se contents. The contents of As and Se in coal, soil, corn, pepper, and hair samples from Ziyang County were significantly higher than those in the control area. The As content of hair in Ziyang County positively correlated with As poisoning, whereas the Se content of hair and urine negatively correlated with As poisoning. The Se content in the body was negatively correlated with the degree of As poisoning, indicating that Se may accelerate the metabolism and decumulation of As and antagonize As toxicity.
RESUMEN
Renifolin F is a prenylated chalcone isolated from Shuteria involucrata, a traditional minority ethnic medicine used to treat the respiratory diseases and asthma. Based on the effects of the original medicine plant, we established an in vivo mouse model of allergic asthma using ovalbumin (OVA) as an inducer to evaluate the therapeutic effects of Renifolin F. In the research, mice were sensitized and challenged with OVA to establish an allergic asthma model to evaluate the effects of Renifolin F on allergic asthma. The airway hyper-reactivity (AHR) to methacholine, cytokine levels, ILC2s quantity and mircoRNA-155 expression were assessed. We discovered that Renifolin F attenuated AHR and airway inflammation in the OVA-induced asthmatic mouse model by inhibiting the regulation of ILC2s in the lung, thereby, reducing the upstream inflammatory cytokines IL-25, IL-33 and TSLP; the downstream inflammatory cytokines IL-4, IL-5, IL-9 and IL-13 of ILC2s; and the co-stimulatory factors IL-2 and IL-7; as well as the expression of microRNA-155 in the lung. The findings suggest a therapeutic potential of Renifolin F on OVA-induced airway inflammation.
Asunto(s)
Asma , Hipersensibilidad , MicroARNs , Animales , Asma/inducido químicamente , Asma/tratamiento farmacológico , Asma/metabolismo , Líquido del Lavado Bronquioalveolar , Chalcona/farmacología , Chalcona/uso terapéutico , Citocinas/metabolismo , Modelos Animales de Enfermedad , Inmunidad Innata , Inflamación , Pulmón/metabolismo , Linfocitos/metabolismo , Ratones , MicroARNs/genética , MicroARNs/uso terapéutico , Ovalbúmina/efectos adversosRESUMEN
(±)-Involucrasins A (1) and B (2), two pairs of flavanone enantiomers were isolated from Shuteria involucrata. Structurally, both 1 and 2 are rare representatives of 5-dehydroxy/5-demethoxy 2',3',4'-trisubstituted flavanones. Their structures were elucidated on the basis of comprehensive spectroscopic data analysis and comparison with the literature data. Involucrasin B (2) exhibited moderate anti-proliferative activity against Caco-2, MCF-7, MDA-MB-468, and HCT116 cell lines with IC50 values ranging from 7.9-22.7 µM. Involucrasin A (1) exhibited weak inhibitory activity against Caco-2 and MCF-7 cell lines with IC50 values of 25.8 and 26.5 µM, respectively.
Asunto(s)
Flavanonas , Neoplasias , Células CACO-2 , Línea Celular Tumoral , Proliferación Celular , Flavanonas/química , Flavanonas/farmacología , Humanos , Concentración 50 Inhibidora , Estructura MolecularRESUMEN
Swertia mileensis, known as Qing-Ye-Dan (QYD), has been documented in Chinese Pharmacopoeia to cure hepatitis. Interestingly, its announced main active component, swertiamarin, could not be detected in the decoction, which indicated that the efficacy of QYD might be attributed to heat-transformed products of swertiamarin (HTPS). Further investigation on HTPS led to the isolation of sweritranslactone D (1), a novel secoiridoid dimer possessing a tetracyclic lactone skeleton, with better hepatoprotective activity than N-acetyl-L-cysteine in vitro.
Asunto(s)
Enfermedad Hepática Inducida por Sustancias y Drogas/tratamiento farmacológico , Calor , Glucósidos Iridoides/química , Lactonas/química , Sustancias Protectoras/farmacología , Pironas/química , Animales , Línea Celular , Medicamentos Herbarios Chinos , Humanos , Ratones , Estructura Molecular , Sustancias Protectoras/aislamiento & purificación , Swertia/químicaRESUMEN
Skeleton-diversity-oriented chemical conversion from pure natural products is a valuable method to obtain natural product-like compounds, especially those with novel architecture. The application of phytochemical methods to iridoids yielded three novel secoiridoid dimers: sweritranslactones A-C (1-3). These molecules possess a 6/6/6/6/6/6-fused hexacyclic skeleton and were obtained from swertiamarin, one of the major constituents of the genus Swertia, via a [4 + 2] cycloaddition and intramolecular nucleophilic addition under aqueous conditions. The structures were established based on extensive spectroscopic characterization and X-ray crystallographic diffraction analysis.
Asunto(s)
Glucósidos Iridoides/química , Iridoides/química , Pironas/química , Cristalografía por Rayos X , Reacción de Cicloadición , Dimerización , Estructura MolecularRESUMEN
Aconitum vilmorinianum Komarov is a local medicinal plant used in many well-known clinical preparations to treat rheumatism and pains in Yunnan Province, China. Phytochemical examination of the roots of A. vilmorinianum led to the isolation of three novel imine-type norditerpenoid alkaloids named vilmorrianines E-G (1-3), and a new natural alkaloid N-desethyl-N-formyl-8-O-methyltalatisamine (4), together with 14 known alkaloids. Their structures were elucidated on the basis of spectroscopic evidence. Vilmorrianine E is the first known norditerpenoid alkaloid containing both an imine group and a three-membered ring formed by C8, C9, and C10.
Asunto(s)
Aconitum/química , Alcaloides/química , Diterpenos/química , Plantas Medicinales/químicaRESUMEN
Two new chalcones, 2',3,4,4'-tetrahydroxy-2-prenylchalcone (1) and 3-methoxy-2',4,4'-trihydroxy-2-prenylchalcone (2), together with two known compounds, munsericin (3) and 3,4-dihydroxylonchocarpin (4), were isolated from the ethanol extract of the whole plant of Shuteria sinensis. Their structures were identified by spectroscopic analysis methods, such as 1D and 2D NMR, along with HR-MS data. Glucose metabolism activity of four compounds was tested, compounds 3 and 4 showed effect on the glucose consumption of insulin-resistant HepG2 cells.
Asunto(s)
Chalconas/química , Fabaceae/química , Chalconas/aislamiento & purificación , Medios de Cultivo , Glucosa/metabolismo , Células Hep G2 , Humanos , Estructura Molecular , Extractos Vegetales/químicaRESUMEN
OBJECTIVE: To investigate the chemical constituents of the processed products of Aconitum Vilmorinian Radix. METHODS: The constituents were isolated by repeated column chromatography over silica gel, alumina and RP-C18 as well as recrystallization. The structures were elucidated on the basis of spectral analysis and physicochemical properties. RESULTS: Ten compounds were obtained from the methanol extract, and they were identified as yunaconitine (1), 8-deacetyl-yunaconitine (2), geniculatine C (3), vilmorrianine B (4), vilmorrianine C(5), vilmorrianine D (6), talatisamine (7), ß-sitosterol (8), ß-daucosterol (9) and ß-sitosterol acetate (10). CONCLUSION: All compounds are obtained from the processed products of Aconitum Vilmoriniani Radix for the first time.
Asunto(s)
Aconitum/química , Fitoquímicos/análisis , Raíces de Plantas/química , Aconitina/análogos & derivados , SitoesterolesRESUMEN
PURPOSE: To investigate the effect of resin curing system formulations of TMPT-contained trial dentin sealant on its bonding and polymerization properties. METHODS: Commercially available Hybrid Coat (HyC) and previously trial TMPT-contained dentin sealant T33 as control groups, adjusting camphorquinone (CQ) content to make CQ trial dentin sealants. Their dentin shear bond strength was tested to find the strongest group named CQn as the next test substrate. N-phenylglycine (NPG) content of original sponges was adjusted to make NC trial sponges. Bond strength and degree of conversion of CQn were tested using each NC trial sponges. The data was analyzed by SPSS13.0 software package. RESULTS: CQ3 showed the biggest bond strength in the group of CQ trial sealants of about 12.99 MPa. When CQ3 was used with every NPG trial sponges, NPG4.4 and NPG7.3 groups showed the statistically greatest bond strength of about 14.68 and 14.69 MPa (P<0.05). And NPG7.3 also showed the maximum degree of conversion of about 83.2%. CONCLUSIONS: The bonding strength and degree of conversion of trial TMPT-contained dentin sealant were the biggest when molar ratio of CQ and NPG was 1:4.4 or 7.3, but the material properties need to be tested in subsequent experiments.