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BACKGROUND: Observational studies have previously shown a possible link between fatty acids and aging-related diseases, raising questions about its health implications. However, the causal relationship between the two remains uncertain. METHODS: Univariable and multivariable Mendelian randomization (MR) was used to analyze the relationship between five types of fatty acids-polyunsaturated fatty acid (PUFA), monounsaturated fatty acid (MUFA), saturated fatty acid (SFA), Omega-6 fatty acid (Omega-6 FA), and Omega-3 fatty acid (Omega-3 FA) and three markers of aging: telomere length (TL), frailty index (FI), and facial aging (FclAg). The primary approach for Mendelian randomization (MR) analysis involved utilizing the inverse variance weighted (IVW) method, with additional supplementary methods employed. RESULTS: Univariate MR analysis revealed that MUFA, PUFA, SFA, and Omega-6 fatty acids were positively associated with TL (MUFA OR: 1.019, 95% CI: 1.006-1.033; PUFA OR: 1.014, 95% CI: 1.002-1.026; SFA OR: 1.016, 95% CI: 1.002-1.031; Omega-6 FAs OR=1.031, 95% CI: 1.006-1.058). PUFA was also associated with a higher FI (OR: 1.033, 95% CI: 1.009-1.057). In multivariate MR analysis, after adjusting for mutual influences among the five fatty acids, MUFA and PUFA were positively independently associated with TL (MUFA OR: 1.1508, 95% CI = 1.0724-1.2350; PUFA OR: 1.1670, 95% CI = 1.0497-1.2973, while SFA was negatively correlated (OR: 0.8005, 95% CI: 0.7045-0.9096). CONCLUSIONS: Our research presents compelling evidence of a causal association between certain fatty acids and indicators of the aging process. In particular, MUFA and PUFA may play a role in slowing down the aging process, while SFAs may contribute to accelerated aging. These findings could have significant implications for dietary recommendations aimed at promoting healthy aging.
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Ácidos Grasos Omega-3 , Ácidos Grasos , Grasas de la Dieta , Análisis de la Aleatorización Mendeliana , Ácidos Grasos Insaturados , Ácidos Grasos MonoinsaturadosRESUMEN
Objective: Although acupuncture is widely used as a complementary therapy in the treatment of Bell's palsy (BP) when to initiate acupuncture is still controversial. This study aims to determine the efficacy of the early intervention by acupuncture on BP. Methods: We retrospectively gathered clinical data from the Third Affiliated Hospital of SUN-YAT SEN University between 2016 and 2021. We selected newly diagnosed patients with BP who were diagnosed by registered neurologists or acupuncturists formally. The qualified patients were divided into two groups according to whether or not initial acupuncture treatment was given within 7 days from the onset of palsy. Cohorts were balanced using 1:1 propensity score matching (PSM). Cox proportional hazards modeling and Kaplan-Meier analysis were applied to determine the differences between the two groups. The outcome included time to complete recovery of facial function, the rate of complete recovery, and the occurrence of sequelae in 24 weeks. Results: A total of 345 patients were eligible for this study and were divided into the manual acupuncture/electroacupuncture (MA/EA) group (n = 76) and the EA group (n = 125). In the propensity score-matched cohort, the time to complete recovery was significantly shorter in the MA/EA group compared with the patients in the EA group (hazard ratio 1.505, 95% CI 1.028-2.404, p <0.05). The MA/EA group had a higher rate of favorable outcomes at 12 weeks than the EA group (93.4 vs. 80.3%, p = 0.032), and the occurrence of sequelae at 24 weeks showed a greater reducing trend in the MA/EA group than the EA group (6.6 vs. 16.4%, p = 0.088). Conclusion: Acupuncture intervention at the acute stage of BP could shorten the time to recovery and improve the outcome. Clinical trial registration: http://www.chictr.org.cn, identifier ChiCTR 2200058060.
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Elsberg syndrome (ES) is an infectious syndrome presenting with variable signs of acute lumbosacral radiculomyelitis. Its low recognition rate leads to misdiagnosis and incorrect treatment. Thus, some ES patients may develop neurological sequelae. This case described a 74-year-old woman complained of urinary retention, constipation, and sacral numbness after herpes zoster in the perianal area. She was diagnosed with ES and accepted conventional drug treatments and urethral catheterization. The treatment was ineffective; therefore, she accepted electroacupuncture six times and her symptoms completely disappeared, with no recurrence of neurological disorders during 1-year follow-up. This shows that acupuncture is a safe and effective alternative therapy for ES. Nonetheless, further prospective studies are necessary to prove its efficacy in ES.
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Terapia por Acupuntura , Herpes Zóster , Retención Urinaria , Terapia por Acupuntura/efectos adversos , Anciano , Femenino , Herpes Zóster/complicaciones , Herpes Zóster/diagnóstico , Herpes Zóster/terapia , Herpesvirus Humano 3 , Humanos , Estudios Prospectivos , Retención Urinaria/complicaciones , Retención Urinaria/terapiaRESUMEN
@#Objective - ( ) To analyze the current situation of work related musculoskeletal disorders WMSDs in neck and low , Methods back of acupuncturists and to explore its influencing factors. A total of 272 acupuncturists from 21 hospitals above grade B level in Guangdong Province were selected as study subjects using convenient sampling method. The revised Chinese , version of Musculoskeletal Disorders Questionnaire was used to investigate the prevalence of WMSDs in the past one year and Results the influencing factors of WMSDs in the high incidence areas such as neck and low back were analyzed. The annual ( ), ( ) prevalence of WMSDs among acupuncturists was 94.9%. The prevalence of WMSDs in the neck 81.6% low back 81.6% ( ) , and shoulder 63.2% was the highest and the prevalence of WMSDs in both the neck and low back was 73.5%. The prevalence - - ( vs ,P ) of multi site WMSDs was higher than that of single site WMSDs 86.0% 8.8% <0.01 . Multivariate logistic regression , - , , analysis showed that acupuncturists who were female long time sitting work repeated operations within one minute and work ( P ) changing every day were common risk factors for neck or low back WMSDs or both neck and low back all <0.05 . Keeping the , , same posture for a long time driving to work and personnel shortage were risk factors for low back WMSDs in acupuncturists ( P ) (P )Conclusion all <0.05 . Uncomfortable working posture was a risk factor for WMSDs in both neck and low back <0.05 . - , - Acupuncturists are the high risk population of WMSDs and the neck and low back are the high risk sites of WMSDs. The influencing factors of WMSDs in acupuncturists include individual factors and occupational factors such as poor ergonomics and work organization.
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Lung cancer is one of the most malignant tumors with the highest mortality and morbidity. The tubers of Bletilla striata are known as "an excellent medicine for lung diseases" in traditional Chinese medicine. This study performed a targeted study to explore compounds with anti-lung cancer activity and the molecular mechanisms using A549 cells. Eighteen bibenzyl derivatives, including four new compounds (13, 14, 16, and 18), were isolated from the tubers of B. striata. Analysis of the structure-activity relationship indicated that the cytotoxicity of the bibenzyls against A549 cells increased gradually as the number of the benzyl groups in the structures increased. Bletillain (18), an unusual benzyl polymer, was found to be the most active compound. Further flow cytometric analysis, dual-luciferase assays, real-time PCR assays, and western blot assays revealed that bletillain induced autophagy in A549 cells by regulating the Akt/GSK-3ß/ß-catenin signaling pathway. Beclin 1, LC3, and p62 are downstream autophagy factors of Akt, and Beclin 1 was the key autophagy factor. These results suggested that bibenzyls of B. striata play important roles in the treatment of lung cancer and provided scientific evidence illustrating why the tubers of B. striata are a suitable medicine for the treatment of lung cancer in traditional Chinese medicine.
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Autofagia/efectos de los fármacos , Descubrimiento de Drogas , Células A549 , Relación Dosis-Respuesta a Droga , Glucógeno Sintasa Quinasa 3 beta/antagonistas & inhibidores , Glucógeno Sintasa Quinasa 3 beta/metabolismo , Humanos , Estructura Molecular , Proteínas Proto-Oncogénicas c-akt/antagonistas & inhibidores , Proteínas Proto-Oncogénicas c-akt/metabolismo , Transducción de Señal/efectos de los fármacos , Relación Estructura-Actividad , Células Tumorales Cultivadas , beta Catenina/antagonistas & inhibidores , beta Catenina/metabolismoRESUMEN
Reverse prediction and molecular docking techniques were employed to evaluate the feasibility of reniformin A(RA) as an anti-tumor leading compound. Based on the reverse prediction, network pharmacology was used to construct a "disease-compound-target-pathway" network. Thirty-nine tumor-related targets of RA were predicted, which participated in the regulation of multiple cellular activities such as apoptosis, cell cycle, and tumor metastasis, and regulated estrogen signal transduction and inflammatory response. Discovery Studio 2020 was adopted for molecular docking and toxicity prediction(TOPKAT). As revealed by the results, the binding affinity of RA with the tumor-related targets ABL1, ESR1, SRC and BCL-XL was stronger than that of oridonin(OD), while its mutagenicity, rodent carcinogenesis, and oral LD_(50) in rats were all inferior to that of OD. Furthermore, in vitro experiments were performed to confirm the anti-tumor activity of RA, and the mechanism was preliminarily discussed. The results demonstrated that RA was superior to OD in cytotoxicity, inhibition of cell colony formation, and induction of apoptosis. RA, possessing potent anti-tumor activity, is expected to be a new anti-tumor leading compound.
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Medicamentos Herbarios Chinos , Neoplasias , Animales , Medicamentos Herbarios Chinos/farmacología , Plomo , Simulación del Acoplamiento Molecular , Neoplasias/tratamiento farmacológico , Neoplasias/genética , Ratas , Transducción de SeñalRESUMEN
Polygonatum cyrtonema is a known tonic herb in Chinese Materia Medica, extensively consumed in China, but the structure and activity of its polysaccharide components remain to be clarified. Herein, two new polysaccharides (a fructan and a galactan) were purified from the dried and the processed P. cyrtonema rhizome, respectively. Structural analysis suggested that the fructan consisted of a (2 â 6) linked ß-d-Fruf residues backbone with an internal α-d-Glcp residue and two (2 â 1) linked ß-d-Fruf residues branches, and that the galactan was a (1 â 4)-ß-d-galactan branched with a single ß-d-galactose at C-6 at about every nine residues in its main chain. The bioactive assay showed that the fructan and the galactan remarkably promoted growth of Bifidobacterium and Lactobacillus strains, indicating that they possess prebiotic activity. These findings may help expand the application of the polysaccharides from the tonic herb P. cyrtonema as functional ingredients in food products.
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Fructanos/química , Fructanos/metabolismo , Galactanos/química , Galactanos/metabolismo , Polygonatum/química , Bifidobacterium/metabolismo , Secuencia de Carbohidratos , Fructanos/aislamiento & purificación , Galactanos/aislamiento & purificación , Lactobacillus/metabolismo , Peso Molecular , PrebióticosRESUMEN
Chinese materia medica (CMM) has been applied for the prevention and treatment of diseases for thousands of years. However, arrhythmia, myocardial ischemia, heart failure, and other cardiac adverse reactions during CMM application were gradually reported. CMM-induced cardiotoxicity has aroused widespread attention. Our review aimed to summarize the risk compounds, preclinical toxicity evaluation, and potential mechanisms of CMM-induced cardiotoxicity. All relevant articles published on the PubMed, Embase, and China National Knowledge Infrastructure (CNKI) databases for the latest twenty years were searched and manually extracted. The risk substances of CMM-induced cardiotoxicity are relatively complex. A single CMM usually contains various risk compounds, and the same risk substance may exist in various CMM. The active and risk substances in CMM may be transformed into each other under different conditions, such as drug dosage, medication methods, and body status. Generally, the risk compounds of CMM-induced cardiotoxicity can be classified into alkaloids, terpenoids, steroids, heavy metals, organic acids, toxic proteins, and peptides. Traditional evaluation methods of chemical drug-induced cardiotoxicity primarily include cardiac function monitoring, endomyocardial biopsy, myocardial zymogram, and biomarker determination. In the preclinical stage, CMM-induced cardiotoxicity should be systematically evaluated at the overall, tissue, cellular, and molecular levels, including cardiac function, histopathology, cytology, myocardial zymogram, and biomarkers. Thanks to the development of systematic biology, the higher specificity and sensitivity of biomarkers, such as genes, proteins, and metabolic small molecules, are gradually applied for evaluating CMM-induced cardiotoxicity. Previous studies on the mechanisms of CMM-induced cardiotoxicity focused on a single drug, monomer or components of CMM. The interaction among ion homeostasis (sodium, potassium, and calcium ions), oxidative damage, mitochondrial injury, apoptosis and autophagy, and metabolic disturbance is involved in CMM-induced cardiotoxicity. Clarification on the risk compounds, preclinical toxicity evaluation, and potential mechanisms of CMM-induced cardiotoxicity must be beneficial to guide new CMM development and post-marketed CMM reevaluation.
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Liver fibrosis resulting from continuous long-term hepatic damage represents a heavy burden worldwide. Liver fibrosis is recognized as a complicated pathogenic mechanism with extracellular matrix (ECM) accumulation and hepatic stellate cell (HSC) activation. A series of drugs demonstrate significant antifibrotic activity in vitro and in vivo. No specific agents with ideally clinical efficacy for liver fibrosis treatment have been developed. In this review, we summarized the antifibrotic effects and molecular mechanisms of 29 kinds of common natural products. The mechanism of these compounds is correlated with anti-inflammatory, antiapoptotic, and antifibrotic activities. Moreover, parenchymal hepatic cell survival, HSC deactivation, and ECM degradation by interfering with multiple targets and signaling pathways are also involved in the antifibrotic effects of these compounds. However, there remain two bottlenecks for clinical breakthroughs. The low bioavailability of natural products should be improved, and the combined application of two or more compounds should be investigated for more prominent pharmacological effects. In summary, exploration on natural products against liver fibrosis is becoming increasingly extensive. Therefore, natural products are potential resources for the development of agents to treat liver fibrosis.
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The fight against the novel coronavirus pneumonia (namely COVID-19) that seriously harms human health is a common task for all mankind. Currently, development of drugs against the novel coronavirus (namely SARS-CoV-2) is quite urgent. Chinese medical workers and scientific researchers have found some drugs to play potential therapeutic effects on COVID-19 at the cellular level or in preliminary clinical trials. However, more fundamental studies and large sample clinical trials need to be done to ensure the efficacy and safety of these drugs. The adoption of these drugs without further testing must be careful. The relevant articles, news, and government reports published on the official and Preprint websites, PubMed and China National Knowledge Infrastructure (CNKI) databases from December 2019 to April 2020 were searched and manually filtered. The general pharmacological characteristics, indications, adverse reactions, general usage, and especially current status of the treatment of COVID-19 of those potentially effective drugs, including chemical drugs, traditional Chinese medicines (TCMs), and biological products in China were summarized in this review to guide reasonable medication and the development of specific drugs for the treatment of COVID-19.
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Antivirales/uso terapéutico , Betacoronavirus/efectos de los fármacos , Infecciones por Coronavirus/tratamiento farmacológico , Infecciones por Coronavirus/epidemiología , Medicamentos Herbarios Chinos/uso terapéutico , Pandemias , Neumonía Viral/tratamiento farmacológico , Neumonía Viral/epidemiología , Adenosina Monofosfato/análogos & derivados , Adenosina Monofosfato/uso terapéutico , Alanina/análogos & derivados , Alanina/uso terapéutico , Amidas/uso terapéutico , Betacoronavirus/inmunología , COVID-19 , China/epidemiología , Cloroquina/uso terapéutico , Infecciones por Coronavirus/mortalidad , Infecciones por Coronavirus/virología , Combinación de Medicamentos , Humanos , Indoles/uso terapéutico , Interferones/uso terapéutico , Lopinavir/uso terapéutico , Pulmón/efectos de los fármacos , Pulmón/patología , Pulmón/virología , Neumonía Viral/mortalidad , Neumonía Viral/virología , Pirazinas/uso terapéutico , Ribavirina/uso terapéutico , Ritonavir/uso terapéutico , SARS-CoV-2 , Análisis de SupervivenciaRESUMEN
Stress urinary incontinence (SUI) is a public health issue attributed to weakened pelvic supporting tissues. Electrical stimulation (ES) is one of the first-line conservative treatments for SUI. However, the underlying mechanism of ES in the treatment of SUI is not clear. Here, we show that ES suppresses cell apoptosis and upregulates collagen expression by functioning as a cell growth inducer to activate the calpain 2/talin 1/integrin ß1/transforming growth factor (TGF)-ß1 axis. Specifically, ES promoted Ca2+ to flow into the cytoplasm through the calcium channel, Cav 3.2, thereby activating calpain 2. Then, the activated calpain 2 cleaved talin 1, which induced the activation of integrin ß1 and upregulated the TGF-ß1-mediated transcription of collagen I and III. Notably, blocking Cav 3.2 suppressed calcium influx and inhibited the activation of downstream proteins. Furthermore, the knockdown of calpain 2 resulted in the reduction of cleaved talin 1, and the shRNA-integrin ß1 treatment downregulated the level of activated integrin ß1 and the expression of TGF-ß1-induced collagen I and III. An association of the ES-modulated collagen I and III upregulation with the therapeutic effect of the ES-Ca2+/calpain 2/talin 1/integrin ß1/TGF-ß1 axis was demonstrated in mouse fibroblast and mouse SUI models established through vaginal distension (VD). This outcome provides insight into clinical diagnosis and treatment.
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Calpaína/metabolismo , Colágeno/metabolismo , Terapia por Estimulación Eléctrica/métodos , Fibroblastos/metabolismo , Integrina beta1/metabolismo , Incontinencia Urinaria/terapia , Animales , Apoptosis , Calcio/metabolismo , Línea Celular , Femenino , Fibroblastos/citología , Ratones , Ratones Endogámicos C57BL , Vagina/metabolismoRESUMEN
Recent research progress in the impact of abiotic stress on florets sterility was summarized in this review to reveal key processes in determining the floret sterility resulted from abiotic stress and their coherent connections. The spikelet fertility was mainly determined by four key processes, including behavior of tapetum, anther dehiscence and pollen release, pollen germination and fertilization. Abiotic stress affected these processes and led to the spikelet sterility. Abnormal changes at the early-stage of anther growth could impact the development of germ cell and fertilization. Damages of floret fertility caused by abiotic stress could be mitigated via some practices such as spraying exogenous plant growth substances or silicon fertilizer. Some research topics were suggested for future investigation, including the interactions of multiple stress factors on fertility, morphological and physiological effects on floral organ formation, differential responses of rice varieties to abiotic stress, and molecular mechanism of abiotic stress on floral organ development.
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Oryza , Polinización , Fertilidad , Flores , PolenRESUMEN
Astrocytes, the most numerous cells in the human brain, play a central role in the metabolic homeostasis following hypoxic injury. Caveolin-1 (Cav-1), a transmembrane scaffolding protein, has been shown to converge prosurvival signaling in the central nerve system. The present study aimed to investigate the role of Cav-1 in the hypoxia-induced astrocyte injury. We also examined how Cav-1 alleviates apoptotic astrocyte death. To this end, primary astrocytes were exposed to oxygen-glucose deprivation (OGD) for 6 h and a subsequent 24-h reoxygenation to mimic hypoxic injury. OGD significantly reduced Cav-1 expression. Downregulation of Cav-1 using Cav-1 small interfering RNA dramatically worsened astrocyte cell damage and impaired cellular glutamate uptake after OGD, whereas overexpression of Cav-1 with Cav-1 scaffolding domain peptide attenuated OGD-induced cell apoptosis. Mechanistically, the expressions of Ras-GTP, phospho-Raf, and phospho-ERK were sequestered in Cav-1 small interfering RNA-treated astrocytes, yet were stimulated after supplementation with caveolin peptide. MEK/ERK inhibitor U0126 remarkably blocked the Cav-1-induced counteraction against apoptosis following hypoxia, indicating Ras/Raf/ERK pathway is required for the Cav-1's prosurvival role. Together, these findings support Cav-1 as a checkpoint for the in hypoxia-induced astrocyte apoptosis and warrant further studies targeting Cav-1 to treat hypoxic-ischemic brain injury.
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Apoptosis , Astrocitos/enzimología , Encéfalo/enzimología , Caveolina 1/metabolismo , Quinasas MAP Reguladas por Señal Extracelular/metabolismo , Hipoxia-Isquemia Encefálica/enzimología , Quinasas raf/metabolismo , Proteínas ras/metabolismo , Animales , Animales Recién Nacidos , Apoptosis/efectos de los fármacos , Astrocitos/efectos de los fármacos , Astrocitos/patología , Encéfalo/efectos de los fármacos , Encéfalo/patología , Caveolina 1/genética , Hipoxia de la Célula , Células Cultivadas , Quinasas MAP Reguladas por Señal Extracelular/antagonistas & inhibidores , Glucosa/deficiencia , Ácido Glutámico/metabolismo , Hipoxia-Isquemia Encefálica/genética , Hipoxia-Isquemia Encefálica/patología , Hipoxia-Isquemia Encefálica/prevención & control , Fosforilación , Cultivo Primario de Células , Inhibidores de Proteínas Quinasas/farmacología , Interferencia de ARN , Ratas Sprague-Dawley , Transducción de Señal , TransfecciónRESUMEN
The influence of the most important classical mono-ADP-ribosyltransferase, arginine ADP-ribosyltransferase 1 (Art1), on survival and apoptosis of colon carcinoma cells and the potential mechanisms have been partly discussed in our previous study but still need to be further studied. In this present study, Art1 of colon carcinoma CT26 cells was silenced with lentiviral vector-mediated short hairpin RNA (shRNA) or overexpressed with lentiviral vector-mediated complementary DNA (cDNA) and allograft transplant tumors are established in Balb/c mice. We verified Art1 knockdown increases apoptosis of CT26 cells transplant tumor; Art1 overexpression acts oppositely. Accordingly, growth of transplant tumors is inhibited in Art1 knockdown transplant tumors and increases in Art1 overexpression transplant tumors. Furthermore, activity of Akt and Erk cell signal pathways and expression of an apoptosis biomarker, ßIII-tubulin (Tubb3), decrease when Art1 was silenced and increase when Art1 was overexpressed. Inhibiting Akt pathway or Erk pathway both downregulates expression of Tubb3 on protein and messenger RNA (mRNA) level, indicating that Tubb3 could be regulated by both Akt and Erk pathways, and plays a role in the influence of Art1 on apoptosis of Balb/c mice allograft transplant tumor. We also demonstrated that Bcl-2 family is not the responsible downstream factor of the Erk pathway in colon carcinoma cells which is undergoing apoptosis. These findings enrich the molecular mechanism for the function of Art1 in colon carcinoma and provide a complementary support for Art1 to be a potential therapeutic target of the treatment of this kind of malignant tumor.
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ADP Ribosa Transferasas/genética , Apoptosis/genética , Neoplasias del Colon/genética , Sistema de Señalización de MAP Quinasas/genética , Proteínas Proto-Oncogénicas c-akt/genética , Transducción de Señal/genética , Tubulina (Proteína)/genética , Animales , Biomarcadores de Tumor/genética , Línea Celular Tumoral , Colon/metabolismo , Regulación hacia Abajo/genética , Femenino , Ratones , Ratones Endogámicos BALB C , ARN Interferente Pequeño/genéticaRESUMEN
Microbial natural products are some of the most important pharmaceutical agents and possess unparalleled chemical diversity. Here we present an untargeted metabolomics algorithm that builds on our validated iSNAP platform to rapidly identify families of peptide natural products. By utilizing known or in silico-dereplicated seed structures, this algorithm screens tandem mass spectrometry data to elaborate extensive molecular families within crude microbial culture extracts with high confidence and statistical significance. Analysis of peptide natural product producers revealed an abundance of unreported congeners, revealing one of the largest families of natural products described to date, as well as a novel variant with greater potency. These findings demonstrate the effectiveness of the iSNAP platform as an accurate tool for rapidly profiling large families of nonribosomal peptides.
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Algoritmos , Metabolómica/métodos , Péptidos/química , Automatización de Laboratorios , Productos Biológicos/química , Biología Computacional/métodos , Simulación por Computador , Evaluación Preclínica de MedicamentosRESUMEN
ETHNOPHARMACOLOGICAL RELEVANCE: Piper wallichii (Miq.) Hand.-Mazz. is a medicinal plant used widely for the treatment of rheumatoid arthritis, inflammatory diseases, cerebral infarction and angina in China. Previous study showed that lignans and neolignans from Piper spp. had potential inhibitory activities on platelet aggregation. In the present study, we investigated the chemical constituents of Piper wallichii and their antithrombotic activities, to support its traditional uses. MATERIALS AND METHODS: The methanolic extract of the air-dried stems of Piper wallichii was separated and purified using various chromatographic methods, including semi-preparative HPLC. The chemical structures of the isolates were determined by detailed spectroscopic analysis, and acidic hydrolysis in case of the new glycoside 2. Determination of absolute configurations of the new compound 1 was facilitated by calculated electronic circular dichroism using time-dependent density-functional theory. All compounds were tested for their inhibitory effects on platelet aggregation induced by platelet activating factor (PAF) in rabbits׳ blood model, from which the active ones were further evaluated the in vivo antithrombotic activity in zebrafish model. RESULTS: A new neolignan, piperwalliol A (1), and four new aromatic glycosides, piperwalliosides A-D (2-5) were isolated from the stems of Piper wallichii, along with 25 known compounds, including 13 lignans, six aromatic glycosides, two phenylpropyl aldehydes, and four biphenyls. Five known compounds (6-10) showed in vitro antiplatelet aggregation activities. Among them, (-)-syringaresinol (6) was the most active compound with an IC50 value of 0.52 mM. It is noted that in zebrafish model, the known lignan 6 showed good in vivo antithrombotic effect with a value of 37% at a concentration of 30 µM, compared with the positive control aspirin with the inhibitory value of 74% at a concentration of 125µM. CONCLUSION: This study demonstrated that lignans, phenylpropanoid and biphenyl found in Piper wallichii may be responsible for antithrombotic effect of the titled plant.
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Fibrinolíticos/farmacología , Glicósidos/farmacología , Lignanos/farmacología , Piper , Extractos Vegetales/farmacología , Animales , Ácido Araquidónico , Plaquetas/efectos de los fármacos , Plaquetas/fisiología , Embrión no Mamífero , Fibrinolíticos/aislamiento & purificación , Fibrinolíticos/uso terapéutico , Glicósidos/aislamiento & purificación , Glicósidos/uso terapéutico , Lignanos/aislamiento & purificación , Lignanos/uso terapéutico , Medicina Tradicional China , Piper/química , Extractos Vegetales/química , Extractos Vegetales/uso terapéutico , Tallos de la Planta/química , Agregación Plaquetaria/efectos de los fármacos , Conejos , Trombosis/inducido químicamente , Trombosis/tratamiento farmacológico , Pez CebraRESUMEN
Six bis-spirolabdane diterpenoids along with four known analogues were isolated from the aerial parts of Leonurus japonicus. Their structures and absolute configurations were elucidated by spectroscopic analyses, single-crystal X-ray diffraction, and a modified Mosher's method. The inhibitory activity of the compounds against the abnormal increase in platelet aggregation induced by adenosine diphosphate was investigated. Only the (13R)-bis-spirolabdane diterpenoids exhibited a significant effect.
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Plaquetas/efectos de los fármacos , Diterpenos/farmacología , Leonurus/química , Agregación Plaquetaria/efectos de los fármacos , Animales , Diterpenos/aislamiento & purificación , Estructura Molecular , Componentes Aéreos de las Plantas/química , Ratas Sprague-DawleyRESUMEN
A new 8,4'-oxyneolignane glucoside 1 has been isolated from the stems of Dendrobium aurantiacum var. denneanum together with six known phenolic glucosides 2−7. The structure of the new compound, including its absolute configuration, was determined by spectroscopic and chemical methods as (−)-(7S,8R,7'E)-4-hydroxy-3,3',5,5'-tetramethoxy-8,4'-oxyneolign-7'-ene-7,9,9'-triol 7,9'-bis-O-ß-D-glucopyranoside (1). In the in vitro assays, compound 1 and (−)-syringaresinol-4,4'-bis-O-ß-D-glucopyranoside (2) showed evident activity against glutamate-induced neurotoxicity in PC12 cells. Shashenoside I (4) showed a selective cytotoxic activity with the IC50 value of 4.17 µM against the acute myeloid leukemia cell line MV4-11, while it was inactive against 10 other human tumor cell lines.
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Dendrobium/química , Glucósidos/química , Fenoles/química , Línea Celular , Supervivencia Celular/efectos de los fármacos , Glucósidos/farmacología , Glucósidos/toxicidad , Humanos , Estructura Molecular , Resonancia Magnética Nuclear Biomolecular , Fenoles/farmacología , Fenoles/toxicidad , Extractos Vegetales/química , Extractos Vegetales/farmacología , Extractos Vegetales/toxicidad , Tallos de la Planta/químicaRESUMEN
Based on the phase and composition analysis of 56 batches of samples, the present paper showed that hydrozincite, just as smithsonite, should be named as the mineralogical origin of medicinal galamina. Galamina was proved to be polymineral aggregation by electron probe micro-analysis, which was constituted by various mineral particulates, such as hydrozincite, smithsonite, zinc oxide, dolomite, etc. It is hydrozincite but not smithsonite that is the current mainstream mineral of commercial galamina. Both hydrozincite and smithsonite should be calcined to turn into zinc oxide when they were used as medicine. As a provider of medical galamina, essentially the zinc oxide, hydrozincite is appropriate.
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Minerales/análisis , Preparaciones Farmacéuticas/química , Compuestos de Zinc/análisis , Medicina Tradicional ChinaRESUMEN
OBJECTIVE: To study the effect of inactivated and un-inactivated pharmaco-serum of diabetic rats fed with Chinese herbs Qianggubao decoction on the proliferation of osteoblast cells (OB)cultured in vitro. METHODS: OB was isolated from the skull of newly born SD rats aged 1 to 2 days by means of Trypsin-collagenase digestion and identified by image analysis under inverted microscope, V-G collagen staining, ALP staining, calcification nod staining etc. After the OB was identified, in activated and un-inactivated pharmaco-serum of diabetic rats fed with Qianggubao decoction of ferent phase (rats were fed with medicine 3 days or 5 days after last fed with medicine 1 hour or 3 hours) and concentration (5%, 10%, 20%) were added to the OB and incubated. After determined times, the effects of the proliferation of osteoblasts were detected by MTT analysis. RESULTS: There was significant difference between un-inactivated pharmaco-serum and inactivated pharmaco-serum on the proliferation of osteoblasts, and un-inactivated serum had stronger effects to improve the proliferation of osteoblasts (P < 0.01 or P < 0.05). CONCLUSION: Un-inactivated and inactivation pharmaco-serum of diabetic rats fed with Chinese herbs Qianggubao decoction can influence the proliferation of, and the un-inactivated pharmaco-serum has stronger effects.