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Planta medica [journal]
- Aspidosperma Species as Sources of Antimalarials. Part III. A Review of Traditional Use and Antimalarial Activity. [JOURNAL ARTICLE]
- Planta Med 2014 Mar 3.
Several plant species belonging to the genus Aspidosperma are traditionally used in Brazil and other Meso- and South American countries for the treatment of malaria and fevers. These traditional uses were motivation for this review. A literature survey completed for this review has identified scientific bibliographical references to the use of 24 Aspidosperma species to treat malaria/fevers and to 19 species that have had their extracts and/or alkaloids evaluated, with good results, for in vitro and/or in vivo antimalarial activity. Indole alkaloids are typical constituents of Aspidosperma species. However, only 20 out of more than 200 known indole alkaloids isolated from this genus have been assayed for antimalarial activity. These data support the potential of Aspidosperma species as sources of antimalarials and the importance of research aimed at validating their use in the treatment of human malaria.
- Plant Extracts of the Family Lauraceae: A Potential Resource for Chemopreventive Agents that Activate the Nuclear Factor-Erythroid 2-Related Factor 2/Antioxidant Response Element Pathway. [JOURNAL ARTICLE]
- Planta Med 2014 Feb 28.
Cells and tissues counteract insults from exogenous or endogenous carcinogens through the expression of genes encoding antioxidants and phase II detoxifying enzymes regulated by antioxidant response element promoter regions. Nuclear factor-erythroid 2-related factor 2 plays a key role in regulating the antioxidant response elements-target gene expression. Hence, the Nrf2/ARE pathway represents a vital cellular defense mechanism against damage caused by oxidative stress and xenobiotics, and is recognized as a potential molecular target for discovering chemopreventive agents. Using a stable antioxidant response element luciferase reporter cell line derived from human breast cancer MDA-MB-231 cells combined with a 96-well high-throughput screening system, we have identified a series of plant extracts from the family Lauraceae that harbor Nrf2-inducing effects. These extracts, including Litsea garrettii (ZK-08), Cinnamomum chartophyllum (ZK-02), C. mollifolium (ZK-04), C. camphora var. linaloolifera (ZK-05), and C. burmannii (ZK-10), promoted nuclear translocation of Nrf2, enhanced protein expression of Nrf2 and its target genes, and augmented intracellular glutathione levels. Cytoprotective activity of these extracts against two electrophilic toxicants, sodium arsenite and H2O2, was investigated. Treatment of human bronchial epithelial cells with extracts of ZK-02, ZK-05, and ZK-10 significantly improved cell survival in response to sodium arsenite and H2O2, while ZK-08 showed a protective effect against only H2O2. Importantly, their protective effects against insults from both sodium arsenite and H2O2 were Nrf2-dependent. Therefore, our data provide evidence that the selected plants from the family Lauraceae are potential sources for chemopreventive agents targeting the Nrf2/ARE pathway.
- Protective Effects of Crocin on Hemodynamic Parameters and Infarct Size in Comparison with Vitamin E after Ischemia Reperfusion in Isolated Rat Hearts. [JOURNAL ARTICLE]
- Planta Med 2014 Feb 28.
Although reperfusion is a useful method for the survival of ischemic heart, harmful effects have been observed. This study was carried out to investigate the preconditioning and cardioprotective potential effects of crocin and vitamin E on the hemodynamic and infarct size in the ischemia-reperfusion model of isolated rat hearts. Animals were divided into a control group, an ischemia-reperfusion control group and three treatment groups: crocin (10, 20, and 40 mg/kg), vitamin E (100 mg/kg), and combination (crocin 40 mg/kg with vitamin E 100 mg/kg). The hearts were excised, quickly transferred to a Langendorff apparatus, and subjected to 30 min of global ischemia followed by 60 min of reperfusion. Left ventricular developed pressure, coronary perfusion pressure, left ventricular systolic pressure, myocardial contractility, rate pressure product, coronary flow, and infarct size were assessed. The successful induction of ischemia was determined by ST elevation on the electrocardiogram.The results showed that crocin significantly improved cardiac dysfunction and also reduced infarct size in the rat hearts. However, the combination of crocin 40 mg/kg and vitamin E 100 mg/kg had an even more significantly improved effect on the hemodynamic parameters and infarct size.Therefore, it can be suggested that the protective role of crocin may be due to the stability or reinforcement of antioxidant systems, and crocin could be useful for the treatment or prevention of cardiac dysfunction.
- Protective Effects of Sulphonated Formononetin in a Rat Model of Cerebral Ischemia and Reperfusion Injury. [JOURNAL ARTICLE]
- Planta Med 2014 Mar; 80(4):262-268.
Sodium formononetin-3'-sulphonate is a derivative of the plant isoflavone formononetin. The present study aimed to investigate the neuroprotective and angiogenesis effects of sodium formononetin-3'-sulphonate in vivo and in vitro. Treatment with sodium formononetin-3'-sulphonate (3, 7.5, 15, and 30 mg/kg, intravenous injection) could protect the brain from ischemia and reperfusion injury by improving neurological function, suppressing cell apoptosis, and increasing expression levels of vascular endothelial growth factor and platelet endothelial cell adhesion molecule 1 by middle cerebral artery occlusion. Treatment with sodium formononetin-3'-sulphonate (10 and 20 µg/mL) significantly increased cell migration, tube formation, and vascular endothelial growth factor and platelet endothelial cell adhesion molecule levels in human umbilical vein endothelial cells. Our results suggest that sodium formononetin-3'-sulphonate provides significant neuroprotective effects against cerebral ischemia and reperfusion injury in rats, and improves cerebrovascular angiogenesis in human umbilical vein endothelial cells. The protective mechanisms of sodium formononetin-3'-sulphonate may be attributed to the suppression of cell apoptosis and improved cerebrovascular angiogenesis by promoting vascular endothelial growth factor and platelet endothelial cell adhesion molecule expression.
- Biomarker-Guided Screening of Juzen-taiho-to, an Oriental Herbal Formulation for Immunostimulation. [JOURNAL ARTICLE]
- Planta Med 2014 Mar; 80(4):283-289.
Juzen-taiho-to is an immunostimulatory herbal formulation that is clinically used in East Asia for cancer patients undergoing chemotherapy and radiation. The formulation stimulates various leukocytes, including T, B, and NK cells and macrophages. Although Juzen-taiho-to is known to contain numerous compounds with various pharmacological activities, it is not clear which compounds are responsible for the stimulation of individual cell types. Here, we conducted what we call "biomarker-guided screening" to purify compounds responsible for the macrophages stimulatory activity. To this end, gene expression was analyzed by a DNA array for macrophages treated with Juzen-taiho-to and DMSO (vehicle control), which identified intercellular adhesion molecule 1 as a biomarker of macrophage stimulation by Juzen-taiho-to. A quantitative reverse transcription polymerase chain reaction assay of intercellular adhesion molecule 1 was then used to guide the purification of active compounds. The screening resulted in the purification of a glycolipid mixture, containing β-glucosylceramides. The glycolipid mixture potently stimulated intercellular adhesion molecule 1 expression in primary dendritic cells as well as in primary CD14+ (macrophages) cells. The identification of this glycolipid mixture opens up an opportunity for further studies to understand how plant-derived glycolipids stimulate macrophages and dendritic cells in a safe and effective manner as demonstrated by Juzen-taiho-to.
- Libiguins A and B: Novel Phragmalin Limonoids Isolated from Neobeguea mahafalensis Causing Profound Enhancement of Sexual Activity. [JOURNAL ARTICLE]
- Planta Med 2014 Mar; 80(4):306-314.
In a screening programme directed towards the discovery of drugs that could enhance sexual activity, we found that a decoction of the root bark of Neobeguea mahafalensis displayed an extraordinarily high potency and remarkably long duration in augmenting sexual activity in male rodents. Bioassay-guided fractionation led to the isolation of two pharmacoactive constituents, which turned out to be novel 1,8,9-orthoacetate phragmalin limonoids that we named libiguins A and B, each with a C-16/30 δ-lactone ring. Chemical structures were established by the interpretation of their 1D and 2D NMR data. In vivo pharmacological tests showed that starting with a treatment from 0.004-0.4 mg/kg/day for three consecutive days, over a 3-h sampling period, these limonoids induced a long-lasting augmentation of frequency and sustainment of mounting behaviour in male rodents, with an effect lasting for up to 11 days post-treatment. Libiguin A proved to be markedly more potent than libiguin B. This report is the first of limonoids having such an effect, and the findings could lead to novel therapies for the treatment of sexual dysfunction. Moreover, the results can serve as an opening to elucidate the central physiological control of mating behaviour, which is still not well mapped out.
- Comprehensive Chemical Analysis of the Rhizomes of Drynaria fortunei by Orthogonal Pre-Separation and Liquid Chromatography Mass Spectrometry. [JOURNAL ARTICLE]
- Planta Med 2014 Mar; 80(4):330-336.
The chemical composition of Drynaria fortunei, a traditional Chinese herbal medicine, is very complicated. In order to separate these chemicals to obtain their structural information, an orthogonal sample enrichment procedure was established. The ethyl acetate extract of D. fortunei was pre-separated by Sephadex LH-20 × polyamide columns to yield 15 fractions. These fractions were analyzed successively using a reversed-phase Agilent Zorbax SB-C18 column, coupled with diode array detection and electrospray ionization tandem mass spectrometry. The method reduced co-elution and enriched minor compounds on the basis of their chemical features. A total of 369 compounds were detected by LC/MSn, compared to less than 50 compounds without pre-separation. The pretreatment facilitated the analytical separation of flavonoids, proanthocyanidins, triterpenoids, phenolic acids, and lignans in D. fortunei, and allowed a comprehensive chemical profiling of these constituents. This method could be applied to other multicomponent herbal extracts.
- Fatsioside A, a Rare Baccharane-Type Glycoside Inhibiting the Growth of Glioma Cells from the Fruits of Fatsia japonica. [JOURNAL ARTICLE]
- Planta Med 2014 Mar; 80(4):315-320.
A novel baccharane-type triterpenoid glycoside named fatsioside A (1), together with ten oleanane glycosides, were isolated from the fruits of Fatsia japonica. The structure of fatsioside A was assigned as 3β,15α,18α-trihydroxy-18,19-secolupane-12,19-dione 3-O-β-D-glucopyranosyl-(1 → 2)-β-D-glucopyranoside by extensive NMR and HRESIMS analyses. F. japonica is the third baccharane glycoside-containing species reported to date in the plant kingdom, while fatsioside A represents the first baccharane glycoside found in the Araliaceae family. Fatsioside A inhibited the growth of rat glioma C6 cells and human glioma U251 cells with IC50 values of 33.48 ± 2.01 µM and 77.58 ± 6.19 µM, respectively. Further investigation indicated that fatsioside A induced apoptosis and necrosis in glioma cells, and arrested the cell cycle at the G0/G1 phase.
- African Medicinal Plants with Antidiabetic Potentials: A Review. [JOURNAL ARTICLE]
- Planta Med 2014 Feb 17.
Diabetes mellitus is one of the major health problems in Africa. The conventional oral synthetic antidiabetic drugs available to manage the disease are costly and not readily affordable to the majority of the affected population. Interestingly, the continent is endowed with a tremendous number of medicinal plants that have been explored for their folkloric treatment of diabetes mellitus. Scientific investigations have validated the antidiabetic potentials of a number of these medicinal plants but there is no repository with information on these scientifically investigated plants as a guide for future research. In this review article, all of the in vivo antidiabetic studies conducted between January 2000 and July 2013 on African plants are systematically compiled with a closer look at some relevant plants from the continent's subregions. Plants of the Asteraceae and Lamiaceae families are the most investigated, and West Africa has the highest number of investigated plants. Although promising results were reported in many cases, unfortunately, only a few studies reported the partial characterization of bioactive principles and/or mechanisms of action. It is hoped that government agencies, pharmaceutical industries, and the scientific community will have a look at some of these plants for future research and, if possible, subsequent commercialization.
- Protective Effects of Oxymatrine on Experimental Diabetic Nephropathy. [JOURNAL ARTICLE]
- Planta Med 2014 Mar; 80(4):269-276.
Diabetic nephropathy, one of the most common and serious vascular complications of both type 1 and type 2 diabetes mellitus, has become a major contributor of end-stage renal failure. The aims of this study were to investigate the effects and possible underlying action mechanism(s) of oxymatrine on renal damage in diabetic rats. Diabetes was induced in male Sprague-Dawley rats by administering a high-fat diet and an intraperitoneal 30 mg/kg streptozotocin injection. The animals were treated orally with saline, metformin hydrochloride, and oxymatrine at 50, 100, and 150 mg/kg/day for 11 weeks. At the end of the treatment, renal tissue, blood, and urine samples were collected for histological and biochemical examination. The results revealed that oxymatrine significantly decreased blood glucose, urinary protein and albumin excretion, serum creatinine, and blood urea nitrogen in diabetic rats, and ameliorated diabetes-induced glomerular and tubular pathological changes. Furthermore, oxymatrine significantly prevented oxidative stress and reduced the contents of renal advanced glycation end products, transforming growth factor-β1, connective tissue growth factor, and inflammatory cytokines in diabetic rats. All these results indicate that oxymatrine has protective effects on experimental diabetic nephropathy by multiple mechanisms.