RESUMEN
ETHNOPHARMACOLOGICAL RELEVANCE: Labisia pumila (Blume) Fern.-Vill, also known as Kacip Fatimah, is a traditional medicinal herb common throughout Southeast Asia. It is primarily used to facilitate childbirth and postpartum recovery in women. Additionally, it can also be used to treat dysentery, rheumatism, gonorrhea, and as an anti-flatulent. AIM OF THIS REVIEW: This article aims to provide a comprehensive review of the traditional uses, botany, cultivation, phytochemistry, pharmacological effects, practical applications, and potential uses of L. pumila (LP). Furthermore, we also explore the safety of this plant and its potential prospects for application. MATERIALS AND METHODS: The keywords "Labisia pumila," "Kacip Fatimah," and "Marantodes pumilum" were used to collect relevant information through electronic searches (including Elsevier, PubMed, Google Scholar, Baidu Scholar, CNKI, ScienceDirect, and Web of Science). RESULTS: This review summarizes 102 chemical components from different parts of the plant, including flavonoids, phenolic acids, saponins, and other chemical components. In addition, we also address the associated cultivation conditions, traditional uses, pharmacological effects and toxicity. A large number of reports indicate that LP has various pharmacological effects such as antioxidant, phytoestrogenic, anti-inflammtory, antimicrobial, anti-osteoporosis and anti-obesity properties. These results provide valuable references for future research on LP. In addition, LP is also a potential medicinal and edible plant, and is currently sold on the market as a dietary supplement. CONCLUSIONS: LP is a renowned traditional ethnic medicine with numerous pharmacological activities attributed to its bioactive components. Therefore, isolation and identification of the chemical components in LP can be a focus of our future research. Current studies have focused only on the effects of LP on estrogen deficiency-related diseases in women and bone diseases. There is no scientific evidence for other traditional uses. Therefore, it is important to further explore its pharmacological activities and fill the research gaps related to other traditional uses. Furthermore, research on its safety should be expanded to prepare clinical applications.
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Etnofarmacología , Medicina Tradicional , Fitoquímicos , Extractos Vegetales , Humanos , Fitoquímicos/farmacología , Fitoquímicos/química , Medicina Tradicional/métodos , Etnofarmacología/métodos , Extractos Vegetales/farmacología , Extractos Vegetales/química , Animales , Fitoterapia , Plantas Medicinales/química , Primulaceae/químicaRESUMEN
The abuse of antibiotics leads to the rapid spread of bacterial resistance, which seriously threatens human life and health. Now, 8 resorcylic acid derivatives, including 4 new compounds (1-4) were isolated from Lysimachia tengyuehensis by bio-guided isolation, and they inhibited both methicillin-resistant Staphylococcus aureus (MRSA) and vancomycin-resistant Enterococcus (VRE) (MIC = 4-8 µg/mL). Notably, 1 and 2 rapidly killed MRSA and VRE within 40 min without drug resistance in 20 days. Mechanically, they potently disrupted biofilm and cell membrane by interfering with bacterial metabolic imbalance. The structure-activity relationship (SAR) revealed that the lipophilic long carbon chains (C-5/C-6) and hydrophilic hydroxyl/carboxyl groups were essential for the anti-MRSA and VRE bioactivity. Additionally, they effectively recovered MRSA-infected skin wounds and VRE-infected peritoneal in vivo. Resorcylic acid derivatives showed significant anti-MRSA and VRE bioactivity in vitro and in vivo with potential application for the first time.
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Antibacterianos , Staphylococcus aureus Resistente a Meticilina , Pruebas de Sensibilidad Microbiana , Primulaceae , Enterococos Resistentes a la Vancomicina , Animales , Humanos , Ratones , Antibacterianos/farmacología , Antibacterianos/química , Antibacterianos/síntesis química , Biopelículas/efectos de los fármacos , Relación Dosis-Respuesta a Droga , Lysimachia , Staphylococcus aureus Resistente a Meticilina/efectos de los fármacos , Estructura Molecular , Primulaceae/química , Relación Estructura-Actividad , Enterococos Resistentes a la Vancomicina/efectos de los fármacosRESUMEN
Seven new oleanane-type triterpene saponins, lysimaponins A-G, were isolated from aerial parts of Lysimachia laxa Baudo. Their chemical structures have been elucidated by analysis of spectroscopic and chemical methods. All compounds were evaluated for their antibacterial effects against Microcystis aeruginosa, Vibrio parahaemolyticus, V. harveyi, V. vulinificus, V. cholerae, and V. alginolyticus. All compounds showed potent antibacterial activities against the cyanobacteria M. aeruginosa with IC50 values ranging from 14.4 ± 1.2 to 35.3 ± 2.2 µg/mL. Compounds 1, 2, 4-7 inhibited V. parahaemolyticus with MIC values ranging from 64 to 256 µg/mL. The results suggested that saponins from L. laxa could be potential anti-cyanobacteria agents.
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Antibacterianos , Pruebas de Sensibilidad Microbiana , Ácido Oleanólico , Primulaceae , Saponinas , Antibacterianos/farmacología , Antibacterianos/química , Antibacterianos/aislamiento & purificación , Saponinas/farmacología , Saponinas/química , Saponinas/aislamiento & purificación , Primulaceae/química , Ácido Oleanólico/farmacología , Ácido Oleanólico/química , Ácido Oleanólico/análogos & derivados , Ácido Oleanólico/aislamiento & purificación , Microcystis/química , LysimachiaRESUMEN
Exine, this complex sporopollenin-containing and highly variable among taxa envelope of the male gametophyte, consists of two layers, ectexine and endexine. We traced in detail the pollen wall development in Lysimachia vulgaris (Primulaceae), with emphasis on driving forces and critical ontogenetic time. By observation on the sequence of the emergent patterns and by analysis of their substructure with TEM, we intended to clarify the obvious and not-obvious ways of exine construction and to find out the common features in pattern development in other representatives in living nature. The ectexine and endexine ontogeny follows the main stages observed in many other species: first, the appearance of microspore plasma membrane invaginations with isotropic contents within, changed later to anisotropic state; then successive appearance of spherical, rod-like, and lamellate units in the periplasmic space. The lamellate endexine appears unusually early in the exine development. All these elements and their aggregations are manifestation of well-known physical phenomena: phase separation and micellar self-assembly. A consideration of similar surface patterns in very remote taxa suggests the participation in their development of some general nature phenomena as the lows of space-filling operations.
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Polen , Primulaceae , Polen/crecimiento & desarrollo , Primulaceae/crecimiento & desarrollo , Primulaceae/química , Pared Celular , LysimachiaRESUMEN
This study aims to investigate the mechanism of total saponins of Paridis Rhizoma in inducing the ferroptosis of MCF-7 cells and provide a theoretical basis for the clinical treatment of breast cancer with total saponins of Paridis Rhizoma. The methyl thiazolyl tetrazolium(MTT) assay was employed to examine the effects of different concentrations of total saponins of Paridis Rhizoma on the proliferation of MCF-7 cells. A phase contrast inverted microscope was used to observe the morphological changes of MCF-7 cells. The colony formation assay was employed to test the colony formation of MCF-7 cells. The lactate dehydrogenase(LDH) release test was conducted to determine the cell membrane integrity of MCF-7 cells. The cell scratch assay was employed to examine the migration of MCF-7 cells. After that, the level of reactive oxygen species(ROS) in MCF-7 cells was observed by an inverted fluorescence microscope, and the content of Fe~(2+) in MCF-7 cells was detected by the corresponding kit. Transmission electron microscopy was employed to observe the mitochondrial ultrastructure of MCF-7 cells. Western blot was employed to determine the expression of ferroptosis-related proteins, such as p53, solute carrier family 7 member 11(SLC7A11), glutathione peroxidase 4(GPX4), acyl-CoA synthetase long-chain family member 4(ACSL4), and transferrin receptor protein 1(TFR1) in MCF-7 cells. The results showed that 1.5, 3, 4.5, 6, 7.5, and 9 µg·mL~(-1) total saponins of Paridis Rhizoma significantly inhibited the proliferation of MCF-7 cells, with the IC_(50) of 4.12 µg·mL~(-1). Total saponins of Paridis Rhizoma significantly damaged the morphology of MCF-7 cells, leading to the formation of vacuoles and the gradual shrinkage and detachment of cells. Meanwhile, total saponins of Paridis Rhizoma inhibited the colony formation of MCF-7 cells, destroyed the cell membrane(leading to the release of LDH), and shortened the migration distance of MCF-7 cells. Total saponins of Paridis Rhizoma treatment significantly increased the content of ROS, induced oxidative damage, and led to the accumulation of Fe~(2+) in MCF-7 cells. Furthermore, total saponins of Paridis Rhizoma changed the mitochondrial structure, increased the mitochondrial membrane density, led to the decrease or even disappear of ridges, promoted the expression of p53 protein, down-regulated the expression of SLC7A11 and GPX4, and up-regulated the expression of ACSL4 and TFR1. In summary, total saponins of Paridis Rhizoma can significantly inhibit the proliferation and migration of MCF-7 cells and destroy the cell structure by inducing ferroptosis.
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Neoplasias de la Mama , Ferroptosis , Especies Reactivas de Oxígeno , Rizoma , Saponinas , Humanos , Saponinas/farmacología , Saponinas/química , Ferroptosis/efectos de los fármacos , Células MCF-7 , Rizoma/química , Neoplasias de la Mama/tratamiento farmacológico , Neoplasias de la Mama/metabolismo , Neoplasias de la Mama/genética , Especies Reactivas de Oxígeno/metabolismo , Femenino , Medicamentos Herbarios Chinos/farmacología , Medicamentos Herbarios Chinos/química , Proliferación Celular/efectos de los fármacos , Primulaceae/químicaRESUMEN
Lysimachia capillipes Hemsl., a traditional Chinese medicine (TCM), is commonly prescribed for its anti-inflammatory and anti-tumor properties. Pharmacological studies have demonstrated that Lysimachia capillipes Hemsl. saponins (LCS) are the primary bioactive component. However, its mechanism for treating colorectal cancer (CRC) is still unknown. Increasing evidence suggests a close relationship between CRC, intestinal flora, and host metabolism. Thus, this study aims to investigate the mechanism of LCS amelioration of CRC from the perspective of the gut microbiome and metabolome. As a result, seven gut microbiotas and fourteen plasma metabolites were significantly altered between the control and model groups. Among them, one gut microbiota genera (Monoglobus) and six metabolites (Ureidopropionic acid, Cytosine, L-Proline, 3-hydroxyanthranilic acid, Cyclic AMP and Suberic acid) showed the most pronounced callback trend after LCS administration. Subsequently, the correlation analysis revealed significant associations between 68 pairs of associated metabolites and gut microbes, with 13 pairs of strongly associated metabolites regulated by the LCS. Taken together, these findings indicate that the amelioration of CRC by LCS is connected to the regulation of intestinal flora and the recasting of metabolic abnormalities. These insights highlight the potential of LCS as a candidate drug for the treatment of CRC.
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Neoplasias Colorrectales , Microbioma Gastrointestinal , Primulaceae , Saponinas , Saponinas/farmacología , Saponinas/aislamiento & purificación , Microbioma Gastrointestinal/efectos de los fármacos , Animales , Ratones , Primulaceae/química , Neoplasias Colorrectales/tratamiento farmacológico , Masculino , Metaboloma/efectos de los fármacos , Ratones Endogámicos BALB C , LysimachiaRESUMEN
The chemical composition and anti-inflammatory activity of the endemic Lysimachia baviensis were investigated for the first time in this study. A phytochemical fractionation of the methanol extract of L. baviensis resulted in the isolation of a new stilbene (bavienside A, 1) and two new chalcone glycosides (baviensides B and C, 2 and 3). Their structures were elucidated via the interpretation of NMR and HRESIMS spectroscopic data. Compounds 1-3 strongly inhibited the production of nitric oxide in LPS-induced RAW264.7 cells with the IC50 values of 6.23, 2.86 and 3.51 µM, respectively. The C-acetylstilbene and carbomethyl chalcone structures in compound 1 and 3 were found for the first time from natural source and could be important markers for chemotaxonomy of Lysimachia baviensis.
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Chalconas , Estilbenos , Chalconas/química , Chalconas/farmacología , Antiinflamatorios/química , Antiinflamatorios/farmacología , Estilbenos/química , Estilbenos/farmacología , Lysimachia , Glicósidos/química , Primulaceae/química , Óxido Nítrico/químicaRESUMEN
ETHNOPHARMACOLOGICAL RELEVANCE: Marantodes pumilum (MP) herbs, locally known as Kacip Fatimah, are widely used traditionally to improve women's health. The herb is frequently used for gynecological issues such as menstrual problems, facilitating and quickening delivery, post-partum medication, treats flatulence and dysentery, and. MP extracts are thought to aid in the firming and toning of abdominal muscles, tighten breasts and vaginal muscles, and anti-dysmenorrhea. It also was used for the treatment of gonorrhea and hemorrhoids. As MP product has been produced commercially recently, more in-depth studies should be conducted. The presence of numerous active compounds in MP might provide a synergistic effect and potentially offer other health benefits than those already identified and known. AIM OF THE STUDY: This study aimed to use a computational target fishing approach to predict the possible therapeutic effect of Marantodes pumilum and evaluated their effectivity. MATERIALS AND METHODS: This study involves a computational approach to identify the potential targets by using target fishing. Several databases were used: PubChem database to obtain the chemical structure of interested compounds; Traditional Chinese Medicine Systems Pharmacology Database and Analysis Platform (TCMSP) server and the SWISSADME web tool to identify and select the compounds having drug-likeness properties; PharmMapper was used to identify top ten target protein of the selected compounds and Online Mendelian Inheritance in Man (OMIM) was used to predict human genetic problems; the gene id of top-10 proteins was obtained from UniProtKB to be analyzed by using GeneMANIA server to check the genes' function and their co-expression; Gene Pathway established by Kyoto Encyclopedia of Genes and Genomes (KEGG) and Gene Ontology (GO) of the selected targets were analyzed by using EnrichR server and confirmed by using DAVID (The Database for Annotation, Visualization and Integrated Discovery) version 6.8 and STRING database. All the interaction data was analyzed by Cytoscape version 3.7.2 software. The protein structure of most putative proteins was obtained from the RCSB protein data bank. Thedocking analysis was conducted using PyRx biological software v0.8 and illustrated by BIOVIA Discovery Studio Visualizer version 20.1.0. As a preliminary evaluation, a cell viability assay using Sulforhodamine B was conducted to evaluate the potential of the predicted therapeutic effect. RESULTS: It was found that four studied compounds are highly correlated with three proteins: EFGR, CDK2, and ESR1. These proteins are highly associated with cancer pathways, especially breast cancer and prostate cancer. Qualitatively, cell proliferation assay conducted shown that the extract has IC50 of 88.69 µg/ml against MCF-7 and 66.51 µg/ml against MDA-MB-231. CONCLUSIONS: Natural herbs are one of the most common forms of complementary and alternative medicine, and they play an important role in disease treatment. The results of this study show that in addition to being used traditionally to maintain women's health, the use of Marantodes pumilum indirectly has the potential to protect against the development of cancer cells, especially breast cancer. Therefore, further research is necessary to confirm the potential of this plant to be used in the development of anti-cancer drugs, especially for breast cancer.
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Antineoplásicos Fitogénicos/farmacología , Medicamentos Herbarios Chinos/farmacología , Extractos Vegetales/farmacología , Primulaceae/química , Antineoplásicos Fitogénicos/administración & dosificación , Línea Celular Tumoral , Bases de Datos Factuales , Bases de Datos Genéticas , Medicamentos Herbarios Chinos/administración & dosificación , Femenino , Humanos , Concentración 50 Inhibidora , Masculino , Medicina Tradicional China , Simulación del Acoplamiento Molecular , Neoplasias/tratamiento farmacológico , Neoplasias/patología , Farmacología en Red , Extractos Vegetales/administración & dosificaciónRESUMEN
Chemical investigation of the Vietnamese plant Aegiceras floridum Roem. & Schult. (Primulaceae) led to the isolation of the new compound 3-methoxy-5-nonylphenol (1) along with five known ones 2,8,10-trihydroxy-6H-benzo[c]chromen-6-one (2), 2-hydroxy-5-methoxy-3-nonylbenzo-1,4-quinone (3), 5-(3-hydroxypropyl)-7-methoxy-3-(methylbenzofuran-2-yl)-3-methoxyphenol (4), 2,8-dihydroxy-7-methoxy-3,9-diundecyldibenzofuran-1,4-dione (5) and 10-hydroxy-4-methoxy-2,11-diundecylgomphilactone (6). The structures were elucidated by analysis of their HRESIMS and NMR data as well as the comparison of their NMR data with those reported in the literature. The cytotoxic activity of selected isolated compounds against some cancer cell lines such as human epithelial carcinoma (HeLa), human lung cancer (NCI-H460), liver hepatocellular carcinoma (HepG2), human breast cancer (MCF-7), and acute T cell leukemia (Jurkat) was evaluated. Among them, 3 showed moderate activities against MCF-7 with an IC50 of 17.77 µM and NCI-H460 with an IC50 of 25.02 µM. The result of DPPH radical scavenging activity assay indicated that compounds 2-4 and 6 revealed weak antioxidant activity.
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Primulaceae , Antioxidantes/análisis , Antioxidantes/farmacología , Células HeLa , Humanos , Corteza de la Planta/química , Primulaceae/química , Resorcinoles/análisis , Resorcinoles/farmacologíaRESUMEN
Metabolic disturbances in different tissue cells and obesity are caused by excessive calorie intake, and medicinal plants are potential sources of phytochemicals for combating these health problems. This study investigated the role of methanolic extract of the folklore medicinal plant Lysimachia candida (LCM) and its phytochemical, astragalin, in managing obesity in vivo and in vitro. Administration of LCM (200 mg/kg/body weight) daily for 140 days significantly decreased both the body weight gain (15.66%) and blood triglyceride and free fatty acid levels in high-fat-diet-fed male Wistar rats but caused no substantial change in leptin and adiponectin levels. The protein expression of adipogenic transcription factors in visceral adipose tissue was significantly reduced. Further, the 3T3-L1 cell-based assay revealed that the butanol fraction of LCM and its isolated compound, astragalin, exhibited antiadipogenic activity through downregulating adipogenic transcription factors and regulatory proteins. Molecular docking studies were performed to depict the possible binding patterns of astragalin to adipogenesis proteins. Overall, we show the potential antiobesity effects of L. candida and its bioactive compound, astragalin, and suggest clinical studies with LCM and astragalin.
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Adipogénesis/efectos de los fármacos , Fármacos Antiobesidad , Quempferoles/farmacología , Extractos Vegetales/farmacología , Primulaceae , Transducción de Señal/efectos de los fármacos , Células 3T3-L1 , Adipocitos , Animales , Fármacos Antiobesidad/farmacología , Diferenciación Celular , Dieta Alta en Grasa , Masculino , Ratones , Ratones Endogámicos C57BL , Simulación del Acoplamiento Molecular , PPAR gamma/metabolismo , Primulaceae/química , Ratas , Ratas Wistar , Proteínas de Unión a Tacrolimus/metabolismoRESUMEN
The Labisia pumila (LP) is a traditional plant that is locally known as Kacip Fatimah, Selusuh Fatimah, or Pokok Ringgang by the Malaysian indigenous people. It is believed to facilitate their childbirth, treating their postchild birth and menstrual irregularities. The water extract of LP has shown to contain bioactive compounds such as flavonoids, ascorbic acid, ß-carotene, anthocyanin, and phenolic acid, which contribute extensive antioxidant, anti-inflammatory, antimicrobial, and antifungal. The LP ethanolic extract exhibits significant estrogenic effects on human endomentrial adenocarcinoma cell in estrogen-free basal medium and promoting an increase in secretion of alkaline phosphate. Water based has been used for many generations, and studies had reported that it could displace in binding the antibodies and increase the estradiol production making it similar to esterone and estradiol hormone. LP extract poses a potential and beneficial aspect in medical and cosmeceutical applications. This is mainly due to its phytoestrogen properties of the LP. However, there is a specific functionality in the application of LP extract, due to specific functional group in phytoconstituent of LP. Apart from that, the extraction solvent is important in preparing the LP extract as it poses some significant and mild side effects towards consuming the LP extracts. The current situation of women reproductive disease such as postmenopausal syndrome and polycystic ovary syndrome is increasing. Thus, it is important to find ways in alternative treatment for women reproductive disease that is less costly and low side effects. In conclusion, these studies proven that LP has the potential to be an alternative way in treating female reproductive related diseases such as in postmenopausal and polysystic ovarian syndrome women.
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Enfermedades Urogenitales Femeninas/tratamiento farmacológico , Extractos Vegetales/uso terapéutico , Primulaceae/química , Animales , Densidad Ósea/efectos de los fármacos , Estrógenos/metabolismo , Femenino , Enfermedades Urogenitales Femeninas/fisiopatología , Humanos , Fitoestrógenos/farmacología , Fitoestrógenos/uso terapéutico , Extractos Vegetales/farmacologíaRESUMEN
BACKGROUND: M. pumilum has been claimed to protect the bone against the adverse effect of estrogen deficiency. Additionally, it also exhibits anti-diabetic activity. In view of these, this study aims to identify the mechanisms underlying the bone protective effect of M. pumilum in the presence of both estrogen deficiency and diabetes mellitus (DM). METHODS: Ovariectomized, diabetic female rats were given M. pumilum leave aqueous extract (MPLA) (50 and 100 mg/kg/day), estrogen, glibenclamide and estrogen plus glibenclamide for 28 consecutive days. At the end of the treatment, fasting blood glucose (FBG), serum insulin, Ca2+, PO43- and bone alkaline phosphatase (BALP) levels were measured. Rats were sacrificed and femur bones were harvested for determination of expression level and distribution of RANK, RANKL, OPG and oxidative stress and inflammatory proteins by molecular biological techniques. RESULTS: 100 mg/kg/day MPLA treatment decreased the FBG and BALP levels but increased the serum insulin, Ca2+ and PO43- levels in estrogen deficient, diabetic rats. Expression and distribution of RANKL, NF-κB p65, IKKß, IL-6, IL-1ß and Keap-1 decreased however expression and distribution of RANK, OPG, BMP-2, Type-1 collagen, Runx2, TRAF6, Nrf2, NQO-1, HO-1, SOD and CAT increased in the bone of estrogen deficient, diabetic rats which received 100 mg/kg/day MPLA with greater effects than estrogen-only, glibenclamide-only and estrogen plus glibenclamide treatments. CONCLUSION: MPLA helps to overcome the adverse effect of estrogen deficiency and DM on the bone and thus this herb could potentially be used for the treatment and prevention of osteoporosis in postmenopausal women with diabetes.
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Huesos/efectos de los fármacos , Diabetes Mellitus Experimental , Diabetes Mellitus Tipo 2 , Extractos Vegetales/farmacología , Primulaceae/química , Animales , Diabetes Mellitus Experimental/tratamiento farmacológico , Diabetes Mellitus Tipo 2/tratamiento farmacológico , Estrógenos , Femenino , Inflamación , Osteoprotegerina/metabolismo , Ovariectomía , Estrés Oxidativo , Hojas de la Planta/química , Ligando RANK/metabolismo , Ratas , Ratas Sprague-Dawley , Receptor Activador del Factor Nuclear kappa-B/metabolismo , Transducción de SeñalRESUMEN
Herba Lysimachiae inhibits synovial damage in osteoarthritis via regulating two bio labels (integrin alpha 2b/beta 3). However, the relevant active ingredients are still unknown. Here, the active ingredients of herbal medicines were analyzed based on the liquid chromatography-tandem mass spectrometry technology and public bioinformatics platforms. The liquid chromatography-tandem mass spectrometry technology was used for compound analysis, and public databases (PubChem BioAssay and STRING) were applied to establish the links between herbal compounds and both bio labels, and identify which herbal compounds may regulate these bio labels. Subsequently, the osteoarthritis model was used to confirm the results. Totally, ninety compounds in Herba Lysimachiae were identified based on the liquid chromatography-tandem mass spectrometry technology. Bioinformatics analysis showed that five compounds (myricetin, fisetin, esculetin, 7-hydroxycoumarin-4-acetic acid, and caffeic acid) may synergistically regulate bio labels through 11 targets, which may be the active ingredients of Herba Lysimachiae for osteoarthritis treatment. In the verification experiments, five compounds markedly suppressed the overexpression of bio labels in the synovium of the osteoarthritis model. In conclusion, the present study effectively and rapidly analyzed the active ingredients of Herba Lysimachiae for osteoarthritis treatment.
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Biología Computacional , Medicamentos Herbarios Chinos/análisis , Medicamentos Herbarios Chinos/uso terapéutico , Osteoartritis/tratamiento farmacológico , Primulaceae/química , Animales , Cromatografía Liquida , Ácido Yodoacético , Masculino , Osteoartritis/inducido químicamente , Plantas Medicinales/química , Ratas , Ratas Sprague-Dawley , Espectrometría de Masas en TándemRESUMEN
Lysimachia ramosa has been used as a traditional medicine among the tribal population of Meghalaya, northeast India, for the control of helminthosis. The anthelmintic efficacy of L. ramosa has been documented earlier. In the present study, the active compound from L. ramosa has been isolated and identified using mass and NMR spectra. It's in vitro anthelmintic activity was evaluated against Raillietina echinobothrida, one of the most pathogenic cestode of domestic fowl. The isolated active compound was characterized to be a kaempferol derivative which showed potent anthelmintic activity against R. echinobothrida by changing surface ultrastructure and also inhibiting the activity of two neurotransmitter enzymes: acetyl cholinesterase (AChE) and nitric oxide synthase (NOS), both of which are known to perform dynamic roles in the intracellular communication mediated through neuromuscular system. Motility reduction, deformation in the surface architecture, extensive ultrastructural alterations and reduced histochemical stain intensity in both AChE and NOS was observed in the treated parasites. Biochemical result also revealed alteration in the enzyme activities in the treated parasites. Further, depletion in the nitric oxide (NO) production in the bioactive component exposed tissues of R. echinobothrida was also detected. The results provided evidence that the bioactive compound could be further explored to control helminthosis at a large scale.
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Acetilcolinesterasa , Cestodos , Quempferoles , Óxido Nítrico Sintasa , Primulaceae , Acetilcolinesterasa/metabolismo , Animales , Antihelmínticos/farmacología , Cestodos/efectos de los fármacos , Cestodos/enzimología , Activación Enzimática/efectos de los fármacos , Quempferoles/farmacología , Óxido Nítrico/metabolismo , Óxido Nítrico Sintasa/metabolismo , Primulaceae/químicaRESUMEN
With changes in human dietary patterns, the proportion of high-fat and high-cholesterol foods in the daily diet has increased. As a result, the incidence rate of cholelithiasis is increasing rapidly. Many studies have reported on the crucial role that the intestinal microflora plays in the progression of gallstones. Although the whole herb of Lysimachia christinae, a traditional Chinese medicine, has long been extensively used as a remedy for cholelithiasis in China, its effects on the intestinal microflora remain unknown. Hence, in this study, we investigated the ability of the aqueous extract of L. christinae (LAE) to prevent cholesterol gallstones (CGSs) in model animals by affecting the intestinal microflora. The effects of LAE on body weight, serum lipid profile, visceral organ indexes, and histomorphology were studied in male C57BL/6J mice, which were induced by a lithogenic diet. After the 8-week study, CGSs formation was greatly reduced after LAE treatment. LAE also reduced body weight gain and hyperlipidemia and restored the histomorphological changes. Moreover, the intestinal microflora exhibited significant variation. In the model group fed the lithogenic diet, the abundances of the genera unclassified Porphyromonadaceae, Lactobacillus and Alloprevotella decreased, but in contrast, Akkermansia dramatically increased compared with the control check group, which was fed a normal diet; the administration of LAE reversed these changes. These results imply that L. christinae can be considered an efficient therapy for eliminating CGSs induced by a high-fat and high-cholesterol diet, which may be achieved by influencing the intestinal microflora.
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Colesterol/metabolismo , Cálculos Biliares/prevención & control , Microbioma Gastrointestinal/efectos de los fármacos , Extractos Vegetales/farmacología , Primulaceae/química , Animales , Bacterias/clasificación , Bacterias/efectos de los fármacos , Bacterias/genética , Bacterias/aislamiento & purificación , Dieta/efectos adversos , Modelos Animales de Enfermedad , Cálculos Biliares/etiología , Cálculos Biliares/metabolismo , Lípidos/sangre , Hígado/efectos de los fármacos , Hígado/patología , Masculino , Ratones , Ratones Endogámicos C57BL , Extractos Vegetales/administración & dosificación , Aumento de Peso/efectos de los fármacosRESUMEN
BACKGROUND: Dionysia tapetodes, a small cushion-forming mountainous evergreen in the Primulaceae, possesses a vast surface-covering of long silky fibres forming the characteristic "woolly" farina. This contrasts with some related Primula which instead form a fine powder. Farina is formed by specialized cellular factories, a type of glandular trichome, but the precise composition of the fibres and how it exits the cell is poorly understood. Here, using a combination of cell biology (electron and light microscopy) and analytical chemical techniques, we present the principal chemical components of the wool and its mechanism of exit from the glandular trichome. RESULTS: We show the woolly farina consists of micron-diameter fibres formed from a mixture of flavone and substituted flavone derivatives. This contrasts with the powdery farina, consisting almost entirely of flavone. The woolly farina in D. tapetodes is extruded through specific sites at the surface of the trichome's glandular head cell, characterised by a small complete gap in the plasma membrane, cell wall and cuticle and forming a tight seal between the fibre and hole. The data is consistent with formation and thread elongation occurring from within the cell. CONCLUSIONS: Our results suggest the composition of the D. tapetodes farina dictates its formation as wool rather than powder, consistent with a model of thread integrity relying on intermolecular H-bonding. Glandular trichomes produce multiple wool fibres by concentrating and maintaining their extrusion at specific sites at the cell cortex of the head cell. As the wool is extensive across the plant, there may be associated selection pressures attributed to living at high altitudes.
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Flavonas/análisis , Primulaceae/ultraestructura , Tricomas/ultraestructura , Microscopía , Microscopía Electrónica , Primulaceae/químicaRESUMEN
ETHNOPHARMACOLOGICAL RELEVANCE: Marantodes pumilum (Blume) Kuntze has been claimed to be beneficial in protecting the bone against loss in post-menopausal women. In view of increased incidence of diabetes mellitus (DM) in post-menopausal period, M. pumilum ability to overcome the detrimental effect of estrogen-deficiency and DM on the bones were identified. AIM OF THE STUDY: To identify the mechanisms underlying protective effect of MPLA on the bone in estrogen-deficient, diabetic condition. METHODS: Adult female, estrogen-deficient, diabetic rats (225 ± 10 g) were divided into untreated group and treated with M. pumilum leaf aqueous extract (MPLA) (50 mg/kg/day and 100 mg/kg/day) and estrogen for 28 days (n = 6 per group). Fasting blood glucose (FBG) levels were weekly monitored and at the end of treatment, rats were sacrificed and femur bones were harvested. Bone collagen distribution was observed by Masson's trichome staining. Levels of bone osteoblastogenesis, apoptosis and proliferative markers were evaluated by Realtime PCR, Western blotting, immunofluorescence and immunohistochemistry. RESULTS: MPLA treatment was able to ameliorate the increased in FBG levels in estrogen deficient, diabetic rats. In these rats, decreased bone collagen content, expression level of osteoblastogenesis markers (Wnt3a, ß-catenin, Frizzled, Dvl and LRP-5) and proliferative markers (PCNA and c-Myc) and increased expression of anti-osteoblastogenesis marker (Gsk-3ß) and apoptosis markers (Caspase-3, Caspase-9 and Bax) but not Bcl-2 were ameliorated. Effects of 100 mg/kg/day MPLA were greater than estrogen. CONCLUSION: MPLA was able to protect against bone loss, thus making it a promising agent for the treatment of osteoporosis in women with estrogen deficient, diabetic condition.
Asunto(s)
Diabetes Mellitus Experimental/tratamiento farmacológico , Osteoblastos/efectos de los fármacos , Extractos Vegetales/farmacología , Primulaceae/química , Animales , Apoptosis/efectos de los fármacos , Huesos/efectos de los fármacos , Huesos/metabolismo , Diabetes Mellitus Experimental/fisiopatología , Regulación hacia Abajo/efectos de los fármacos , Estrógenos/metabolismo , Femenino , Osteoblastos/citología , Hojas de la Planta , Ratas , Ratas Sprague-Dawley , Regulación hacia Arriba/efectos de los fármacos , Vía de Señalización Wnt/efectos de los fármacosRESUMEN
Capilliposide B (CPS-B) and Capilliposide C (CPS-C), as the key components in Lysimachia capillipes Hemsl., increasingly aroused the interest and research concern of many researchers due to the good bioactivities. Nowadays, the reference standards of CPS-B and CPS-C yield were very limited. Due to the deficit of reference standards, the determination could be difficult to carry out, and the quality control and evaluation would be restrained afterwards. To solve this urgent problem, a quantitative analysis of multi-components by single-marker (QAMS) method was proposed and established based on high-performance liquid-chromatography tandem evaporative light-scattering detector. In this QAMS method, the content of the two bioactive components could be calculated by buddlejasaponin IV, which is applied as an external standard and readily obtained. And the methodological experiments were evaluated and indicated accuracy, stability and feasibility of this QAMS method. Therefore, in this study, this built method would properly meet the requirement of determination of CPS-B, CPS-C and quality control of the L. capillipes Hemsl. plant.
Asunto(s)
Medicamentos Herbarios Chinos , Primulaceae , Saponinas , Cromatografía Líquida de Alta Presión , Fitoquímicos/química , Primulaceae/química , Saponinas/químicaRESUMEN
Marantodes pumilum (MP) is a great source of herbal medicine used traditionally by both men and women for various purposes. MP may have potential wound-healing effects due to its diverse biological properties. An extensive study was conducted in a normal male rat model for determining the effects of MP var. pumila (MPvp) and var. alata (MPva) on the wound healing process. Here, 126 male Sprague-Dawley rats were divided randomly into seven groups as follows: sham-operated (SH), vehicle dressing (VD), flavine dressing (FD), MPvp leaves (PL), MPvp roots (PR), MPva leaves (AL), and MPva roots (AR). The parameters studied were the percentage of wound contraction, histomorphology study by hematoxylin and eosin (H&E), Masson-Goldner trichrome (MGT), and immunohistochemistry (IHC) staining. In addition, the levels of enzymatic antioxidants and malondialdehyde were also measured in the wound tissue homogenates. Wounds treated with extracts (PL, PR, AL, and AR) showed significantly faster healing (p < 0.05) compared to untreated and control groups (SH, VD, and FD). Histological analysis among MP-treated groups revealed better re-epithelialization, higher collagen deposition, enhanced fibronectin content and fibroblast cells, and higher fiber transformation from collagen-III to collagen-I, accompanied with a significant surge in enzymatic antioxidant activities and a decline in lipid peroxidation. MP has antioxidant effects that may enhance wound healing in the rat model.
Asunto(s)
Antioxidantes/farmacología , Fitoterapia , Extractos Vegetales/farmacología , Hojas de la Planta/química , Primulaceae/química , Piel/efectos de los fármacos , Cicatrización de Heridas/efectos de los fármacos , Animales , Peroxidación de Lípido/efectos de los fármacos , Masculino , Malondialdehído/análisis , Ratas , Ratas Sprague-Dawley , Piel/lesionesRESUMEN
BACKGROUND: Nonalcoholic steatohepatitis (NASH), a liver disease caused by a nonalcoholic fatty liver, is increasing in incidence worldwide. Owing to the complexity of its pathogenic mechanisms, there are no therapeutic agents for this disease yet. The ideal drug for NASH needs to concurrently decrease hepatic lipid accumulation and exert anti-inflammatory, antifibrotic, and antioxidative effects in the liver. Because of their multipurpose therapeutic effects, we considered that medicinal herbs are suitable for treating patients with NASH. METHODS: We determined the efficacy of the alcoholic extract of Lysimachia vulgaris var. davurica (LV), an edible medicinal herb, for NASH treatment. For inducing NASH, C57BLKS/J lar-Leprdb/Leprdb (db/db) male mice were fed with a methionine-choline deficient (MCD) diet ad libitum. After 3 weeks, the LV extract and a positive control (GFT505) were administered to mice by oral gavage for 3 weeks with a continued MCD diet as needed. RESULTS: In mice with diet-induced NASH, the LV extract could relieve the disease symptoms; that is, the extract ameliorated hepatic lipid accumulation and also showed antioxidative and anti-inflammatory effects. The LV extract also activated nuclear factor E2-related factor 2 (Nrf2) expression, leading to the upregulation of antioxidants and detoxification signaling. Moreover, the extract presented remarkable efficacy in alleviating liver fibrosis compared with GFT505. This difference was caused by significant LV extract-mediated reduction in the mRNA expression of fibrotic genes like the alpha-smooth muscle actin and collagen type 3 alpha 1. Reduction of fibrotic genes may thus relate with the downregulation of transforming growth factor beta (TGFß)/Smad signaling by LV extract administration. CONCLUSIONS: Lipid accumulation and inflammatory responses in the liver were alleviated by feeding LV extract to NASH-induced mice. Moreover, the LV extract strongly prevented liver fibrosis by blocking TGFß/Smad signaling. Hence, LV showed sufficient potency for use as a therapeutic agent against NASH.