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Introduction: Persistent infections caused by certain viruses and parasites have been associated with multiple diseases and substantial mortality. Heavy metals are ubiquitous environmental pollutants with immunosuppressive properties. This study aimed to determine whether heavy metals exposure suppress the immune system, thereby increasing the susceptibility to persistent infections. Methods: Using data from NHANES 1999-2016, we explored the associations between heavy metals exposure and persistent infections: Cytomegalovirus (CMV), Epstein-Barr Virus (EBV), Hepatitis C Virus (HCV), Herpes Simplex Virus Type-1 (HSV-1), Toxoplasma gondii (T. gondii), and Toxocara canis and Toxocara cati (Toxocara spp.) by performing logistic regression, weighted quantile sum (WQS) and Bayesian kernel machine regression (BKMR) models. Mediation analysis was used to determine the mediating role of host immune function in these associations. Results: Logistic regression analysis revealed positive associations between multiple heavy metals and the increased risk of persistent infections. In WQS models, the heavy metals mixture was associated with increased risks of several persistent infections: CMV (OR: 1.58; 95% CI: 1.17, 2.14), HCV (OR: 2.94; 95% CI: 1.68, 5.16), HSV-1 (OR: 1.25; 95% CI: 1.11, 1.42), T. gondii (OR: 1.97; 95% CI: 1.41, 2.76), and Toxocara spp. (OR: 1.76; 95% CI: 1.16, 2.66). BKMR models further confirmed the combined effects of heavy metals mixture and also identified the individual effect of arsenic, cadmium, and lead. On mediation analysis, the systemic immune inflammation index, which reflects the host's immune status, mediated 12.14% of the association of mixed heavy metals exposure with HSV-1 infection. Discussion: The findings of this study revealed that heavy metals exposure may increase susceptibility to persistent infections, with the host's immune status potentially mediating this relationship. Reducing exposure to heavy metals may have preventive implications for persistent infections, and further prospective studies are needed to confirm these findings.
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Exposición a Riesgos Ambientales , Metales Pesados , Humanos , Femenino , Masculino , Exposición a Riesgos Ambientales/efectos adversos , Adulto , Persona de Mediana Edad , Modelos Logísticos , Contaminantes Ambientales/toxicidad , Teorema de Bayes , Virosis/inmunología , AnimalesRESUMEN
ETHNOPHARMACOLOGICAL RELEVANCE: Plants in the genus Hypericum (Hypericaceae), include more than 500 species worldwide, and many are valued for their medicinal properties, and are used as traditional herbal medicines. However, only H. perforatum is officially recognized as herbal drug in several pharmacopoeias, and used as an antidepressant clinically. Hypericum perforatum had been used as an herbal medicine since the Han Dynasty (206 B.C. -220 A.D.) in China. It taxonomically belongs to the section Hypericum in the genus Hypericum. There are about 42 species in the section Hypericum, with six species occurring in China. All six are recorded as traditional herbal medicines for treating aliments, including hepatitis, malaria, traumatic hemorrhage, irregular menstruation, wounds, and bruises. AIM OF THE STUDY: The study aimed to characterize the chemical profiles of five phylogenetically related Hypericum species, and compare their metabolites with three H. perforatum products. Informed by ethnobotanical use, the extracts prepared from the five species were further investigated into anticancer, anti-inflammatory and antiplasmodial activity. This study tested the hypothesis that systematic metabolomic and bioactivity characterization of species in section Hypericum will help to validate their phytotherapeutic use and reveal potential drug lead compounds. MATERIALS AND METHODS: Targeted and non-targeted metabolic analyses coupled with chemometrics were conducted on H. perforatum and four medicinal species, H. attenuatum, H. enshiense, H. erectum, and H. faberi, native to China from section Hypericum. UPLC-QTOF-MS/MS and UPLC-TQD-MS/MS were used for non-targeted and targeted metabolic analyses, respectively. Cytotoxicity bioassays on four cancer cell lines, anti-inflammation tests and anti-plasmodial activity on Plasmodium falciparum 3D7, selected based on traditional medicinal use, were evaluated on extracts from Hypericum species. Progenesis QI and EZinfo were used for chemometrics analysis to link the chemical profile and bioassay activity to aid in the identification of bioactive compounds. RESULTS: In total, 58 compounds were identified from the five species, including compounds with well-characterized bioactivity. Hypericum attenuatum, H. erectum, and H. perforatum, displayed the highest cytotoxicity, and contain the cytotoxic compounds petiolin A, prolificin A, and hypercohin G, respectively. Hypericum faberi and H. perforatum showed the highest anti-inflammatory activity, with pseudohypericin, quercetin and chlorogenic acid being observed at higher concentrations. Hypericum perforatum and H. erectum showed anti-plasmodial activity, with higher hyperforin and xanthones in these species that may account for the anti-plasmodial activity. CONCLUSIONS: This study characterized the chemical differences among five Hypericum species using metabolomics. These ethnomedically important species were tested for their biological activities in three distinct in vitro assays. The ethnobotanical data were useful for identifying bioactive Hypericum species. Hypericum attenuatum, H. erectum and H. faberi are promising phytotherapeutic species, although they are much less studied than H. perforatum, St. John's wort. Combining ethnobotanical surveys with chemometric analyses and bioactivity screening can greatly enhance the discovery of promising active constituents.
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Hypericum , Metabolómica , Extractos Vegetales , Hypericum/química , Humanos , Extractos Vegetales/farmacología , Extractos Vegetales/química , Antiinflamatorios/farmacología , Antimaláricos/farmacología , Antimaláricos/aislamiento & purificación , Antineoplásicos Fitogénicos/farmacología , Antineoplásicos Fitogénicos/aislamiento & purificación , Línea Celular Tumoral , Plasmodium falciparum/efectos de los fármacos , AnimalesRESUMEN
Locating and stratifying the submucosal tumor of the digestive tract from endoscopy ultrasound (EUS) images are of vital significance to the preliminary diagnosis of tumors. However, the above problems are challenging, due to the poor appearance contrast between different layers of the digestive tract wall (DTW) and the narrowness of each layer. Few of existing deep-learning based diagnosis algorithms are devised to tackle this issue. In this article, we build a multi-task framework for simultaneously locating and stratifying the submucosal tumor. And considering the awareness of the DTW is critical to the localization and stratification of the tumor, we integrate the DTW segmentation task into the proposed multi-task framework. Except for sharing a common backbone model, the three tasks are explicitly directed with a hierarchical guidance module, in which the probability map of DTW itself is used to locally enhance the feature representation for tumor localization, and the probability maps of DTW and tumor are jointly employed to locally enhance the feature representation for tumor stratification. Moreover, by means of the dynamic class activation map, probability maps of DTW and tumor are reused to enforce the stratification inference process to pay more attention to DTW and tumor regions, contributing to a reliable and interpretable submucosal tumor stratification model. Additionally, considering the relation with respect to other structures is beneficial for stratifying tumors, we devise a graph reasoning module to replenish non-local relation knowledge for the stratification branch. Experiments on a Stomach-Esophagus and an Intestinal EUS dataset prove that our method achieves very appealing performance on both tumor localization and stratification, significantly outperforming state-of-the-art object detection approaches.
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Neoplasias Gástricas , Humanos , AlgoritmosRESUMEN
Introduction: A. truncatum Bunge (Sapindaceae or formerly Aceraceae) is a tall deciduous tree native to China. Traditionally, the leaves of A. truncatum are decocted and used by Chinese Mongolians, Koreans, and Tibetans to treat skin itching, dry cracks, and other skin ailments, which indicates A. truncatum leaves may have a potential inhibitory effect on various skin inflammations. Methods: To examine the protective effect against skin inflammations of A. truncatum leaf extract (ATLE), an in vitro dermatitis model was established using sodium dodecyl sulfate (SLS)-induced HaCaT cells. The anti-inflammatory effect of ATLE was evaluated by analyzing cell viability, apoptosis, reactive oxygen species (ROS), interleukin 6 (IL-6), and prostaglandin E2 (PGE2) levels. Results: Orthogonal experiments showed that the pretreatment with ATLE can reduce the IL-6 levels, PGE2 levels, and apoptosis increased in SLS-stimulated HaCaT cells, which indicates that ATLE has positive efficacy for dermatitis. Furthermore, three flavonoid compounds kaempferol-3-O-α-L-rhamnoside, quercetin-3-O-α-L-rhamnopyranoside, kaempferol-3,7-di-O-α-L-rhamnoside, and 1,2,3,4,6-Penta-O-galloyl-ß-D-glucopyranose (PGG) were isolated and identified. Among them, kaempferol-3,7-di-O-α-L-rhamnoside was isolated from this plant for the first time. These compounds have been proven to have an anti-inflammatory effect. They may contribute to the efficacy of A. truncatumin treating skin inflammation. Discussion: The results revealed that ATLE has the potential to be used as an additive in various skin care products to prevent skin inflammations and may be incorporated in formulations for topical application as a therapeutic approach against dermatitis.
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The chemical constituents in the ethanol extract of Hypericum wightianum(Hypericaceae) were purified by column chromatography and identified via magnetic resonance imaging(NMR), high-resolution mass spectrum, and circular dichroism. A total of 22 compounds were identified, including eight polyprenylated phloroglucinols(1-8), three chromones(9-11), and three terpenoids(14-16) and so on. Among them, compounds 16 and 17 were first reported in the genus Hypericum, and compounds 1-11, 14, 15, and 19 were first isolated from H. wightianum. Compounds 1-4 were previously reported as two pairs of enantiomers. This study reported the chiral resolutions and absolute configurations of compounds 1-4 for the first time.
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Medicamentos Herbarios Chinos , Hypericum , Floroglucinol , Hypericum/química , Estructura Molecular , Espectroscopía de Resonancia Magnética , Medicamentos Herbarios Chinos/químicaRESUMEN
Hypericum species (Hypericaceae) are a group of important plants with medicinal, edible, and ornamental values. A phytochemical study on the whole plants of H. hengshanense W. T. Wang, a species endemic to China, led to the isolation and elucidation of 25 monoterpenoid acylphloroglucinols (MAPs). Among them, 10 are undescribed compounds, namely hyphengshanols A-D, (+)-empetrilatinol A, (-)-empetrilatinol B, (-)-hyperjovinol A, (9S,2'S)-dauphinol F, and (8R,2'S)-empetrikathiforin. In addition, the absolute configurations of other six compounds were firstly determined in the current study. The structures were established by ultraviolet (UV), high resolution electrospray ionization mass spectrum (HR-ESI-MS), and nuclear magnetic resonance spectroscopy (NMR) data. The absolute configurations were determined by experimental and calculated electronic circular dichroism (ECD) data analyses. Cytotoxicity assays on five human cell lines HL-60, A549, SMMC-7721, MDA-MB-231, and SW480 revealed that 16 compounds exhibited broad-spectrum antiproliferative activities with IC50 ranging from 7.54 to 45.70 µM.
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Hypericum , Humanos , China , Monoterpenos/farmacologíaRESUMEN
A bioactivity-guided fractionation on the phenolic fractions from the peeled stems of Syringa pinnatifolia Hemsl., one of representative Mongolian folk medicine in China, led to the isolation and structural determination of 11 undescribed lignans and 12 known ones. These lignans cover diverse types, among them syringanones A and B represent an unprecedented carbon skeleton (proposed syringanane) and alashanenol A possesses a rare bicyclo [3.3.1]nonadienemethanol core. Their structures were established by extensive spectroscopic data analysis, X-ray diffraction, and quantum chemical calculations. All isolates were evaluated for their cardioprotective activities on H9c2 cardiomyocytes in vitro. The results showed that five lignans exhibited the protective effects against hypoxia-induced injury at the concentrations of 1.2-40 µM and six lignans exhibited anti-oxidative stress injury at 10-40 µM. These findings account to some extend for the traditional therapeutic effects of S. pinnatifolia for the treatment of ischemic heart diseases in clinic.
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Lignanos , Syringa , Lignanos/farmacología , Lignanos/química , Syringa/química , Hipoxia/tratamiento farmacológico , Miocitos Cardíacos , Estrés OxidativoRESUMEN
As a part of systematic studies on Syringa pinnatifolia, a continued phytochemical investigation guided by 1 H-NMR and LC/MS data on the ethanol extract afforded five new dimeric eremophilane sesquiterpenoids, namely syringenes M-Q (1-5). These structures were elucidated by extensive analysis of spectroscopic data, including infrared (IR), high-resolution electrospray ionization mass spectrometry (HR-ESI-MS), nuclear magnetic resonance (NMR), quantum-mechanics-based computational analysis of NMR chemical shifts, and single-crystal X-ray diffraction. Compounds 4 and 5 showed inhibitory activities against NO production induced by lipopolysaccharide in RAW264.7 macrophage cells, with IC50 values of 5.1 and 9.3â µM, compared to positive control indomethacin (IC50 33.6â µM). These dimeric eremophilane sesquiterpenoids may be potential markers for discriminating this species from the genus Syringa and the Oleaceae family.
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Sesquiterpenos , Syringa , Estructura Molecular , Sesquiterpenos Policíclicos , Sesquiterpenos/química , Sesquiterpenos/farmacología , Espectrometría de Masa por Ionización de Electrospray , Syringa/químicaRESUMEN
A phytochemical investigation guided by 1H NMR and LC-MS data on the ethanol extract of Syringa pinnatifolia stems led to the isolation of 11 new dimeric eremophilane sesquiterpenoids, namely, syringenes A-K (1-11) and one known analog (12, syringene L). These structures were elucidated by extensive analysis of spectroscopic data, single-crystal X-ray diffraction, and computational methods. Biological assays revealed that 1-12 exhibited different degrees of anti-inflammatory effects, and 5 and 6 showed significant cytotoxicity against human hepatoma HepG2 cells with IC50 values of 12.3 and 12.9 µM, respectively. Furthermore, flow cytometry assays and western blot analysis revealed that 5 and 6 promoted the apoptosis of HepG2 cells by activating ERK. Finally, the molecular docking analysis implied that the carbonyl and hydroxy groups at the C-11/C-6' of 5 and 6 had a good binding affinity with ERK.
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Sesquiterpenos , Syringa , Humanos , Simulación del Acoplamiento Molecular , Estructura Molecular , Sesquiterpenos Policíclicos , Sesquiterpenos/química , Syringa/químicaRESUMEN
A pair of enantiomers with a rearranged dimeric phenylethanol skeleton, namely (±)-disyringol A (1a and 1b), were isolated from the stem barks of Syringa pinnatifolia. The structures were established using IR, UV, MS, and NMR data, and their absolute configurations were resolved by experimental and calculated ECD data analysis. Their biosynthetic pathway was speculated on the basis of a phenylethanoid precursor and was proved by a total synthesis. Compounds 1a and 1b showed the inhibition against NO production in LPS-induced RAW264.7 cells with their IC50 values of 27.28 and 24.64 µM, respectively, however no protective effect was observed against the hypoxia-induced injuries to H9c2 cells.
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Syringa , Animales , Ratones , Estructura Molecular , Células RAW 264.7 , Esqueleto , Estereoisomerismo , Syringa/químicaRESUMEN
ETHNOPHARMACOLOGICAL RELEVANCE: Acer truncatum Bunge is a multifunctional plant in northern China. It has traditionally been used to prevent cardiovascular and cerebrovascular diseases and treat skin trauma by different linguistic groups including Mongolian, Tibetan, and Korean. Although research has verified that A. truncatum contains a variety of active ingredients, especially nervonic acid, an important component in delaying brain aging, to date no review has been made to compile its traditional use, phytochemistry, and pharmacology. AIMS OF THE REVIEW: This review aimed to update the traditional uses, phytochemistry, and pharmacology of A. truncatum, which expect to provide theoretical support for the future utilization as well as highlight the further investigation of this important plant. MATERIALS AND METHODS: The ethnobotanical, phytochemical, and pharmacological information related to A. truncatum from 1949 to March 2021 were collated by surveying the traditional medicinal books and ethnomedicinal publications and searching the online databases including Google Scholar, Sci Finder, Web of Science, Springer Link, PubMed, Wiley, China National Knowledge Infrastructure (CNKI), Baidu Scholar, and Wan Fang Database. RESULTS: A. truncatum has traditionally been used for medicinal, edible and ornamental purposes in northern China for many centuries. Different parts of the plant including leaves, fruits and bark, are mainly used as herbal medicine to treat hyperpiesia, hyperlipidemia, bruises, back pain, etc. A total of 288 compounds in A. truncatum, including polyphenols, organic acids or lipids, and biological volatile organic compounds were isolated or identified by phytochemical studies. Pharmacological research showed that A. truncatum has various bioactivities such as acetylcholinesterase inhibition, antibacterial, antioxidant, antitumor, and fatty acid synthase inhibition effects. CONCLUSION: A. truncatum has been used as a traditional herbal medicine for centuries in northern China. Polyphenols, organic acids, lipids and other compounds were isolated or identified from different parts of the plant. Most of the pharmacological activities of A. truncatum have been reported, which showed its potential in the development of new drugs or nutraceuticals. However, detailed information on the molecular mechanisms, metabolic activity, and toxicology of active components is limited. Further comprehensive research to evaluate the medicinal properties of A. truncatum will be necessary.
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Acer , Medicamentos Herbarios Chinos , Etnobotánica/métodos , Medicamentos Herbarios Chinos/química , Medicamentos Herbarios Chinos/farmacología , Etnofarmacología/métodos , Etnofarmacología/tendencias , Humanos , Medicina Tradicional China/tendencias , Fitoquímicos/química , Fitoquímicos/farmacologíaRESUMEN
Three pairs of enantiomeric sesquiterpenoids, (∓)-syringanoid A (1a and 1b) and (±)-pinnatanoids A (2a and 2b) and B (3a and 3b), that represent an unprecedented 5/4/6 tricyclic backbone and a rare 6/7 bicyclic backbone, respectively, were isolated from the peeled stems of Syringa pinnatifolia. The structures were elucidated by extensive spectroscopic analysis, single-crystal X-ray diffraction, a modified Mosher's method, and quantum chemical calculations. A plausible biotransformation pathway for 1-3 was proposed, and their cardiomyocyte-protective and anti-inflammatory activities were evaluated.
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Sesquiterpenos , Syringa , Cristalografía por Rayos X , Estructura Molecular , EstereoisomerismoRESUMEN
Fumaria species, commonly known as fumitory or earth smoke, are considered weeds in many regions. However, several Fumaria species have long been used in folk medicine, such as F. capreolata L., F. densiflora DC., F. indica (Hausskn.) Pugsley, F. officinalis L., F. parviflora Lam., and F. vaillantii Loisel. as well. The ethnobotany, phytochemistry, and pharmacology of 24 Fumaria species have been investigated. Phytochemical studies on Fumaria species revealed the presence of numerous alkaloids, flavonoids, saponins, and terpenoids. Phthalideisoquinolines (PTIs), protoberberines, and spirobenzylisoquinolines (SBIs) are the major alkaloids in the genus Fumaria. The plants biosynthesize a diverse group of biologically active isoquinoline alkaloids, and these may help to explain the use of various Fumaria species in folk medicine. Pharmacological studies revealed a broad spectrum of bioactivities such as hepatoprotective, anti-inflammatory, antimicrobial, antioxidant, and antitumor activities. We found 159 articles published from 1969-2019 by searching the keyword "Fumaria" using databases such as SciFinder, Google Scholar, and PubMed. Based on our reading of these papers, Fumaria species appear to be a source of bioactive isoquinoline alkaloids and ethnomedicines. The lack of studies on pharmacological mechanisms, pharmacokinetics, clinical efficacy, quality control, and toxicology are discussed in this review. There is great potential for broader medicinal applications of this genus.
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Alcaloides/farmacología , Fumaria/química , Isoquinolinas/farmacología , Alcaloides/aislamiento & purificación , Alcaloides de Berberina , Isoquinolinas/aislamiento & purificación , Medicina Tradicional , Estructura Molecular , Fitoquímicos/aislamiento & purificación , Fitoquímicos/farmacologíaRESUMEN
Plants in Acorus have been used as herbal medicine by various linguistic groups for thousands of years. Arguments of taxonomy of Acorus among scientists resulted in confusions and misuses of Acorus plants. The present study used different methods to investigate the classification of the genus, based on folk taxonomy. The relationships among Acorus species were revealed through phylogenetic analyses by constructing the Maximum Likelihood and Bayesian phylogenetic analyses based on sequences of two chloroplast regions (trnL-trnF and rbcL). All samples named with two so-called synonyms, Acorus macrospadiceus (Yamam.) F. N. Wei and Y. K. Li and Acorus tatarinowii Schott collected from different habitats, were clustered into separate groups, which revealed that they represented two independent species. Multivariate statistical analysis of metabolites from different Acorus populations were carried out based on UPLC-QTOF-MS data. Three independent analysis, principal component analysis, heat-map analysis, and hierarchical cluster analysis, showed that A. macrospadiceus and A. tatarinowii are different from two recognized species in the genus, A. calamus L. and A. gramineus Aiton. The results of phylogenetics and chemotaxonomy, together with morphological and ecological evidences, were consistent with traditional knowledge of local people related to Acorus taxa, which proved the significance of parataxonomy. Multiple evidences including morphological, ecological, folk taxonomic, phylogenetic, and chemical taxonomic results suggested that there are four species in the genus Acorus.
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ETHNOPHARMACOLOGICAL RELEVANCE: Hypericum species have been used traditionally as astringent, antipyretic, diuretic, antiphlogistic, analgesic, and antidepressant in Europe, America, Africa, and Asia. One of the most extensively investigated medicinal herbs, H. perforatum L. (St. John's wort), is widely used in many countries to treat mild to moderate mental depression. Hypericum species are abundant throughout China, including 30 used as ethnomedicines. There are limited publications describing the ethnobotanical uses and biological activities associated with Hypericum species in China. Some reported activities include the treatment of wounds and bruises, irregular menstruation, dysentery, hepatitis, mastitis, jaundice, hemoptysis, and epistaxis. AIM OF THE REVIEW: This review aims to critically examine how Hypericum species are used ethnomedicinally in China, to see if the ethnobotanical data may be useful to help prioritize Hypericum species and certain phytochemical constituents that may be new drug leads, and consider the focus and lack of the phytopharmacological study on Hypericum species in China. MATERIALS AND METHODS: Classic medicinal books and ethnomedicinal publications were reviewed for the genus Hypericum (called jin si tao in Chinese). In addition, relevant information about ethnobotany, phytochemistry, and pharmacology were from online databases including SciFinder, Science Direct, PubMed, Google Scholar, and China National Knowledge Infrastructure (CNKI). "Hypericum", "", "ethnobotany", "traditional use", "ethnomedicine", "phytochemistry", "pharmacology" and "bioactivity" were used as keywords when searching the databases. Thus, available articles from 1959 to 2019 were collected and analyzed. RESULTS: Among 64 Hypericum species recorded in China, 30 have been used as ethnomedicines by 15 linguistic groups such as Dai, Dong, Han, Miao, and Mongolian people. Hypericum species in China possess traditional uses which are also mirrored in Europe, America, Africa, and other countries in Asia. However, there are some unique ethnomedicinal uses in China. For example, several Hypericum species are used as a local remedy in southwest China, and H. attenuatum Fisch. ex Choisy is used to treat cardiac disorders in northeast China. Antitumor, anti-inflammatory, antimicrobial, neuroprotective, antidepressant, hepatoprotective, cardioprotective, and antiviral activities have been reported in numerous biological studies. The main phytochemical constituents in Hypericum consist of phloroglucinols, naphthodianthrones, xanthones, flavonoids, and terpenoids. CONCLUSIONS: There is a rich traditional knowledge regarding the ethnomedicinal uses of Hypericum species in China. Through phytochemical and pharmacological studies, several medicinal Hypericum from China have yielded many bioactive phytochemicals, possessing antitumor, anti-inflammatory, antimicrobial, and neuroprotective properties. Hypericum species from China are potential sources of drugs to fight cancer and other chronic diseases. Remarkably, nearly half of Hypericum species in China have rarely been studied, and their ethnomedicinal potential have not been scientifically evaluated. Thus, in vitro mechanistic studies, in vivo pharmacology, and clinical efficacy are all needed, prioritizing those studies that relate most closely with their traditional uses. In addition, a comprehensive plant-resource evaluation, quality control, and toxicology studies are needed.
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Hypericum , Animales , Antioxidantes/química , Antioxidantes/farmacología , Antioxidantes/uso terapéutico , China , Etnobotánica , Etnofarmacología , Humanos , Medicina Tradicional China , Fitoquímicos/química , Fitoquímicos/farmacología , Fitoquímicos/uso terapéutico , Fitoterapia , Preparaciones de Plantas/química , Preparaciones de Plantas/farmacología , Preparaciones de Plantas/uso terapéuticoRESUMEN
Three new eremophilane-type sesquiterpenoids, alashanoids K-M (1-3), and one known analogue (4) were isolated from the peeled stems of Syringa pinnatifolia. All the compounds were isolated from the genus Syringa for the first time. Structures of these compounds were established using 1D and 2D NMR and MS data. The absolute configurations were determined by experimental and calculated electronic circular dichroism analysis, a modification of Mosher's method, and X-ray diffraction. Compounds 2 and 3 inhibited NO production in LPS-induced RAW264.7 macrophage cells with IC50 values of 14.23 and 12.20 µM, respectively, and showed cytotoxic activities against HepG2 cells with the IC50 values of 34.41 and 40.86 µM, respectively.
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Sesquiterpenos , Syringa , Animales , Ratones , Estructura Molecular , Corteza de la Planta , Sesquiterpenos PolicíclicosRESUMEN
Hypericum stellatum, a species endemic to China, is used to treat hepatitis by several ethnic groups in Guizhou Province. This research was inspired by the traditional medicinal usage of H. stellatum, and aims to explore the phytochemistry and bioactivity of H. stellatum to explain why local people in Guizhou widely apply H. stellatum for liver protection. In this study, two new prenylated xanthones, hypxanthones A (8) and B (9), together with seven known compounds, were isolated from the aerial parts of the plant. Spectroscopic data as well as experimental and calculated ECD spectra were used to establish the structures of these compounds. Six xanthones isolated in this study, together with four xanthones previously isolated from H. stellatum, were evaluated for their growth-inhibitory activities against five human liver carcinoma cell lines to analyze the bioactivity and structure-activity relationship of xanthones from H. stellatum. Isojacareubin (6) showed significant cytotoxicity against five human liver carcinoma cell lines, with an IC50 value ranging from 1.41 to 11.83 µM, which was stronger than the positive control cisplatin (IC50 = 4.47-20.62 µM). Hypxanthone B (9) showed moderate cytotoxicity to three of the five cell lines. Finally, structure-activity analysis revealed that the prenyl and pyrano substituent groups of these xanthones contributed to their cytotoxicity.
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Antineoplásicos Fitogénicos/química , Antineoplásicos Fitogénicos/farmacología , Hypericum/química , Xantonas/química , Xantonas/farmacología , Línea Celular Tumoral , Proliferación Celular/efectos de los fármacos , Supervivencia Celular/efectos de los fármacos , Ensayos de Selección de Medicamentos Antitumorales , Células Hep G2 , Humanos , Concentración 50 Inhibidora , Neoplasias Hepáticas/tratamiento farmacológico , Medicina Tradicional China , Estructura Molecular , Componentes Aéreos de las Plantas/química , Relación Estructura-ActividadRESUMEN
BACKGROUND: Beverages prepared by fermenting plants have a long history of use for medicinal, social, and ritualistic purposes around the world. Socio-linguistic groups throughout China have traditionally used plants as fermentation starters (or koji) for brewing traditional rice wine. The objective of this study was to evaluate traditional knowledge, diversity, and values regarding plants used as starters for brewing glutinous rice wine in the Dong communities in the Guizhou Province of China, an area of rich biological and cultural diversity. METHODS: Semi-structured interviews were administered for collecting ethnobotanical data on plants used as starters for brewing glutinous rice wine in Dong communities. Field work was carried out in three communities in Guizhou Province from September 2017 to July 2018. A total of 217 informants were interviewed from the villages. RESULTS: A total of 60 plant species were identified to be used as starters for brewing glutinous rice wine, belonging to 58 genera in 36 families. Asteraceae and Rosaceae are the most represented botanical families for use as a fermentation starter for rice wine with 6 species respectively, followed by Lamiaceae (4 species); Asparagaceae, Menispermaceae, and Polygonaceae (3 species respectively); and Lardizabalaceae, Leguminosae, Moraceae, Poaceae, and Rubiaceae (2 species, respectively). The other botanical families were represented by one species each. The species used for fermentation starters consist of herbs (60.0%), shrubs (23.3%), climbers (10.0%), and trees (6.7%). The parts used include the root (21.7%), leaf (20.0%), and the whole plant (16.7%). Findings indicate a significant relationship between knowledge of plants used as fermentation starters with age (P value < 0.001) and educational status (P value = 0.004) but not with gender (P value = 0.179) and occupation (P value = 0.059). The species that are most used by informants include Pueraria lobata var. montana (Lour.) van der Maesen (UV = 1.74; Leguminosae), Actinidia eriantha Benth. (UV = 1.51; Actinidiaceae), Oryza sativa L. var. glutinosa Matsum (UV = 1.5; Poaceae). CONCLUSION: This study highlights that while most of the Dong informants continue to use a diverse range of plants as a fermentation starter for brewing glutinous rice wine, knowledge of these plants is being lost by the younger generations. Documentation of traditional ethnobotanical knowledge and outreach is thus needed to conserve biocultural diversity in the rural Dong communities in southern China.
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Fermentación , Conocimiento , Oryza , Plantas Comestibles/clasificación , Vino , Adulto , Biodiversidad , China , Femenino , Humanos , Masculino , Persona de Mediana Edad , Adulto JovenRESUMEN
BACKGROUND: Peeled stems of Syringa pinnatifolia Hemsl. (SP) have been widely used to treat extra "He-Yi" induced myocardial ischemia for hundreds of years in Inner Mongolia, China and previous result showed that intragastric pretreatment with total extract (T) of SP has a protective effect against myocardial infarction (MI). HYPOTHESIS: This study aims to describe the pharmacological investigation and chemical characterization of the major (M) and minor (N) fractions obtained from T through column chromatography fractionation on macroporous resin and to explore whether the regulatory effects were linked to the p53-mediated apoptosis pathways. STUDY DESIGN: Left anterior descending (LAD) coronary artery-ligated mice and H9c2 cells cultured in serum-free medium under hypoxic conditions were treated with T, M, and N. METHODS: Echocardiography was performed and biomarkers in serum were determined in mice, and pathological changes were observed through histopathology assay. Immunofluorescence staining and qRT-PCR were used to detect the expression levels of p53 in heart tissue. Flow cytometry was used to measure the level of apoptosis and caspase-3 activity in H9c2 cells. Western blot analysis was conducted to detect p53 and p53-mediated proteins apoptosis pathways of in both tissue and H9c2 cells. RESULTS: Both T and M have an equivalent cardioprotective effect whereas N is non-active. M decreased MI-induced myocardial compensatory expansion by decrease of left ventricular end-systolic diameter (LVESd) and left ventricular end-diastolic diameter (LVEDd) and prevented decreases in ejection fraction (EF) and fractional shortening (FS). The MI-induced increased levels of creatine kinase-MB (CK-MB), lactate dehydrogenase (LDH), and hypersensitive C-reactive protein (hs-CRP) were decreased and the expanded infarction size was reduced. M could also improve cell viability and inhibit apoptosis in H9c2 cells under hypoxic conditions. Immunofluorescence and qRT-PCR assay showed that M suppressed p53 expression in the myocardium. Western blot analysis showed that M could prevent MI-induced activation of p53-mediated apoptosis pathway in both myocardium and H9c2 cells. CONCLUSION: The results demonstrated that M may protect against myocardial ischemia by improving cardiac function and inhibiting cardiomyocytes apoptosis. Overall, the present findings supported the clinical application of SP and enriched the research of anti-myocardial ischemia drug from traditional medicines.
Asunto(s)
Apoptosis/efectos de los fármacos , Cardiotónicos/farmacología , Isquemia Miocárdica/tratamiento farmacológico , Extractos Vegetales/farmacología , Syringa/química , Proteína p53 Supresora de Tumor/metabolismo , Animales , Línea Celular , Masculino , Ratones , Ratones Endogámicos ICR , Infarto del Miocardio/tratamiento farmacológico , Miocardio/metabolismo , Miocitos Cardíacos/efectos de los fármacos , Tallos de la Planta/química , RatasRESUMEN
Two humulane-type sesquiterpenoids, namely (+)-alashanoid I (1a) and (-)-alashanoid I (1b), were isolated as a pair of enantiomers from the peeled stems of Syringa pinnatifolia. Their structures were elucidated by extensive spectroscopic data (1 D and 2 D NMR, UV, and IR), and the absolute configurations were resolved by X-ray diffraction and experimental and calculated ECD data analysis.