Toxicity and mutagenicity of the molluscicidal plant Ambrosia maritima L.

The acute and subchronic toxicity of the molluscicidal plant, Ambrosia maritima L., has been tested on rats. No toxic signs could be detected neither after oral administration of 5 g/kg of dried leaves of the plant as a powder or as a methanolic extract, nor after the incorporation of 50,000 ppm powdered leaves in the feed during 4 weeks. Using an aqueous extract of the plant material of A. maritima or using ambrosin, one of the active molluscicidal components of the plant, no mutagenic activity could be detected in the S. typhimurium strains TA97, TA 98, TA1538, TA100 and TA1535.     

Toxicity of the molluscicidal plant, Ambrosia maritima L., to aquatic non-target organisms

The toxicity of the molluscicidal plant, Ambrosia maritima L., has been evaluated in fish, crustacea and algae. The LC50 for fries of the guppy, Lebistes reticulatus, was respectively 650 and 450 mg/litre using a powder or an ether-methanol-hexane extract from the leaves of the plant. This concentration is much higher than the molluscicidal concentration (LC90) of 35 to 70 mg/litre, which is used in the field (irrigation canals in Egypt). Preliminary tests showed that juveniles of L. reticulatus and Tilapia aurea were as sensitive as the fries. Using the same extract of A. maritima the LC50 for Daphnia magna was 766 mg/litre and no toxic effects could be observed in algae Selenastrum capricornutum at 1 g/litre. It can be concluded that A. maritima has a very low toxicity to aquatic non-target organisms. It is not toxic when used at the molluscicidal concentration of 35 to 70 mg/litre.     

Disinfectant properties of essential oils from Salvia officinalis L. cultivated in Tunisia

The essential oils were obtained by hydro-distillation of the aerial part of Salvia officinalis L. cultivated in Sfax gardens, Tunisia. The obtained oils were analyzed by gas chromatography–mass spectrometry (GC–MS) and 44 compounds were identified. Strong bactericidal and fungicidal effects were shown using the NCCLS broth dilution, EN 1275 and EN 1276 standard methods. The minimal cidal concentrations (MCCs) values ranged from 0.031 to 0.25 μL mL⁻¹. The essential oils concentrations of 0.5% and 1% (v/v) resulted in a reduction in viability higher than 5 and 4 log units per mL for the standard bacteria and fungi, respectively, within a contact time of 5 min. Using an air sampler and an aroma dispenser, vaporisation of 0.25 mL m⁻³ of S. officinalis essential oils resulted in (72%, 73% and 70%) and (54%, 55% and 55%) reduction of the total microbial count and the total count of yeasts and moulds, after a residence time of 1 h, 6 h and 24 h in a selected testing room, respectively. S. officinalis essential oils showed a potent vapour activity against a panel of bacteria, yeasts and fungi. This supported their use as a natural eco-friendly disinfectant to manage airborne microbes.     

Three decades of P-gp inhibitors: skimming through several generations and scaffolds

Many tumor cells become resistant to commonly used cytotoxic drugs due to the overexpression of ATP-binding cassette (ABC) transporters, namely P-glycoprotein (P-gp). The discovery of the reversal of multidrug resistance (MDR) by verapamil occured in 1981, and in 1968 MDR Chinese hamster cell lines were isolated for the first time. Since then, P-gp inhibitors have been intensively studied as potential MDR reversers. Initially, drugs to reverse MDR were not specifically developed for inhibiting P-gp; in fact, they had other pharmacological properties, as well as a relatively low affinity for MDR transporters. An example of this first generation P-gp inhibitors is verapamil. The second generation included more specific with less side-effect inhibitors, such as dexverapamil or dexniguldipine. A third generation of P-gp inhibitors comprised compounds such as tariquidar, with high affinity to P-gp at nanomolar concentrations. These generations of inhibitors of P-gp have been examined in preclinical and clinical studies; however, these trials have largely failed to demonstrate an improvement in therapeutic efficacy. Therefore, new and innovative strategies, such as the fallback to natural products, the design of peptidomimetics and dual activity ligands emerged as a fourth generation of P-gp inhibitors. The chemistry of P-gp inhibitors, as well as their in vitro, in vivo and clinical trials are discussed, and the most recent advances concerning Pgp modulators are reviewed.     

Assessment of anti-inflammatory,antinociceptive, immunomodulatory,and antioxidant activities of Cajanus cajan L. seeds cultivated in Egypt and its phytochemical composition

Context: Cajanus cajan L. (Fabaceae), a food crop, is widely used in traditional medicine.

Objectives: The phytochemical composition of C. cajan seeds and evaluation of the anti-inflammatory, immunomodulatory, antinociceptive, and antioxidant activities were studied.

Materials and methods: Unsaponifiable matter and fatty acids were analyzed by GC and GC/MS. The n-butanol fraction was chromatographed on polyamide column. The anti-inflammatory activity of hexane extract (200 and 400?mg/kg, p.o.) was evaluated using the carrageenan-induced rat paw edema at 1, 2, and 3 h. The serum tumor necrosis factor-α, interleukin-6, and immunoglobulin G levels were detected by ELISA. The hexane extract antinociceptive activity was determined by adopting the writhing test in mice. DPPH radical scavenging, total reduction capability, and inhibition of lipid peroxidation of butanol fraction were evaluated.

Results and conclusion: Twenty-one unsaponifiable compounds (mainly phytol, 2,6-di-(t-butyl)-4-hydroxy-4-methyl-2,5-cyclohexadiene-1-one, β-sitosterol, stigmasterol, and campesterol), as well as 12 fatty acids (primarily 9,12-octadecadienoic and palmitic acids) were identified in hexane extract of C. cajan seeds. n-BuOH fraction contains quercetin-3-O-β-d-glucopyranoside, orientin, vitexin, quercetin, luteolin, apigenin, and isorhamnetin. For the first time, quercetin-3-O-β-d-glucopyranoside is isolated from C. cajan plant. The hexane extract (200 and 400?mg/kg) inhibited carrageenan-induced inflammation by 85 and 95%, respectively, 3 h post-carrageenan challenge. This was accompanied by an 11 and 20%, 8 and 13%, respectively, decrease of TNF-α and IL-6, as well as significant decrease in IgG serum levels. Moreover, hexane extract (200 and 400?mg/kg) decreased the number of writhings by 61 and 83%, respectively. The butanol fraction showed DPPH radical scavenging (inhibitory concentration (IC₅₀) value: 9.07 μg/ml).     

Constituents and biological activity of Bidens pilosa L. grown in Egypt.

Column chromotography and preparative TLC of the light petroleum-diethyl ether extract from Bidens pilosa L. afforded tridecapentyn-1-ene, trideca-2,12-diene-4,6,8,10-tetrayne-1-ol, trideca-3,11-diene-5,7,9-triyne-1,2-diol and trideca-5-ene-7,9,11-triyne-3-ol. The compounds were identified on the bases of UV, 1H-NMR spectra and comparison with reported data. The chloroform extract was chromatographed to yield B-amyrin, phytosterin-B, esculetin and B-sitosterol glucoside. The petroleum ether extract afforded long chain ester, saturated hydrocarbon, long chain alcohol, B-amyrin, phytosterin-B, lupeol and lupeol acetate. GLC analysis of the fatty acids indicated the presence of 5 acids. The antimicrobial test was carried out to indicate an evident activity. The antidiabetic activity showed non significant decrease of blood glucose.     

New isoflavone glycosides from <Emphasis Type="Italic">Iris spuria</Emphasis> L. (Calizona) cultivated in Egypt

Two new isoflavone glycosides, tectorigenin 7-O-β-d-glucopyranoside-4′-O-[β-d-glucopyranosyl-(1″″ → 6′′′)-β-d-glucopyranoside] (1) and iristectorigenin B 4′-O-[β-d-glucopyranosyl-(1′′′ → 6″)-β-d-glucopyranoside] (2), together with 11 known compounds, including six isoflavones, tectorigenin 7-O-β-d-glucopyranoside-4′-O-β-d-glucopyranoside (3), tectorigenin 4′-O-[β-d-glucopyranosyl-(1′′′ → 6″)-β-d-glucopyranoside] (4), tectorigenin 7-O-β-d-glucopyranoside (5), genistein 7-O-β-d-glucopyranoside (6), tectorigenin 4′-O-β-d-glucopyranoside (7), and tectorigenin (8); two phenolic acid glycosides, vanillic acid 4-O-β-d-glucopyranoside (9) and glucosyringic acid (10); a phenylpropanoid glycoside, E-coniferin (11); an auronol derivative, maesopsin 6-O-β-d-glucopyranoside (12); and a pyrrole derivative, 4-(2-formyl-5-hydroxymethylpyrrol-1-yl) butyric acid (13), were isolated from fresh Iris spuria (Calizona) rhizomes. The structures of these compounds were established on the basis of spectroscopic and chemical evidence. Inhibitory effects on the activation of Epstein–Barr virus early antigen were examined for compounds 1–8 and 12.     

人工栽培光果甘草不同根系黄酮含量的测定

目的测定并比较人工栽培光果甘草不同根系中总黄酮的含量,为光果甘草的合理种植、采收利用及质量评定提供依据。方法以柚皮苷作为对照品,用紫外分光光度法于417 nm处测定黄酮的含量。结果总黄酮含量水平根为1.62%,主根为1.22%,侧根为1.13%。结论光果甘草的不同根系总黄酮含量不同,且有明显差异。     

Extraction and Cytochemical Localization of Alkaloids in Plants of Vallota speciosa L. f. cultivated in Apulia

Abstract

Localization of total alkaloids in Vallota speciosa L. f. was studied during the flowering period. The alkaloids synthesized in the epigeal leaves were translocated to the bulbs and unripe fruits. Total alkaloids content of bulbs, leaves and unripe fruits are reported.     

Histopathological and biochemical changes in lung tissues of rats following administration of fluoride over several generations

The possible effects of multigenerational administration of sodium fluoride (NaF) via drinking water on lung tissue morphology and biochemistry and body and lung weight were investigated in second-generation adult male rats. For this purpose we selected 45 Albino adult Wistar rats in nine cages, each of which consisted of four females and one male. Twenty-eight pregnant rats were selected for the experiment, divided into four groups of seven rats given 1 (control group), 10, 50 and 100 mg l(-1) NaF in drinking water during the gestation period. After gestation the rats had 165 pups in total. The mothers received fluoridated water during the lactation period and the offspring of the first generation had access to fluoridated water during the suckling period (21 days) and after the weaning period (30 days) until they became mature and at the start of the second part of the experiment. During this time 23 pups died and 79 female and 63 male first-generation rats survived. These first-generation rats were then used to obtain the second-generation offspring in the same manner as before, which were subjected to the same treatments. At the end of 6 months the rats were sacrificed and autopsied. Serum fluoride levels and the activities of principal antioxidant enzymes were determined in lung tissue samples taken from all groups. In addition, the lung tissues were submitted for histopathological examination. Histological findings showed alveolar congestion, alveolar cell hyperplasia and necrosis, prominent alveolar septal vessels, epithelial desquamation and macrophages in the alveolar spaces in the experimental groups. Additionally, there were inflammatory infiltrations in peribronchial, perivascular, intraparenchymal and respiratory tract lumen; intraparenchymal hyperaemic vessels; respiratory epithelial desquamation and proliferation; intraparenchymal thick walled vessels; parenchymal fibrosis; bronchiolitis; pneumonic and focal emphysematous areas. Furthermore, the lung parenchyma was observed to have a distorted appearance with loss of alveolar architecture. These histopathological findings were more pronounced for the rat groups of 50 and 100 mg l(-1) fluoride. No significant histopathological changes were observed in the rats of the control group. The increased activities of superoxide dismutase (SOD) and reduced glutathione peroxidase (GSH-Px) and the decreased activity of catalase (CAT) in the lung tissues with 10 mg l(-1) fluoride might indicate activation of the antioxidant defence mechanism. The decrease in SOD, GSH-Px and CAT activities with 50 and 100 mg l(-1) fluoride and the increase in thiobarbituric acid-reactive substance levels might be related to oxidative damage that occurred in the lung. This multigenerational evaluation of the long-term effect of different doses of fluoride intake through drinking water on lung damage shows that the lung tissues were damaged, there was emphysema and inflammation of lung parenchyma associated with loss of alveolar architecture and the degree of lung damage seemed to correlate with the increased dosage of fluoride. A similar relationship was observed between the degree of lung damage, body and lung weight and serum fluoride levels according to the fluoride dose. Therefore, these results contribute to a better understanding of chronic fluoride toxicity in lung tissue of second-generation rats, especially via drinking water, and the biochemical findings were in agreement with histological observations. In addition, increased fluoride concentration did not affect reproduction or the number of pups dying but the body weight and lung weight ratios were affected by the high dose of fluoride in a dose-related pattern.     

Phytochemical contents and enzyme inhibitory and antioxidant properties of Anethum graveolens L. (dill) samples cultivated under organic and conventional agricultural conditions

Inhibitory effect of the n-hexane, dichloromethane, ethyl acetate, and ethanol extracts from Anethum graveolens L. (dill) cultivated under organic (AG-O) and conventional (AG-C) conditions was tested against acetylcholinesterase (AChE), butyrylcholinesterase (BChE), and tyrosinase at 200 μg mL⁻¹. Their antioxidant activity was determined using 2,2-diphenyl-1-picrylhydrazyl (DPPH), N,N-dimethyl-p-phenylendiamine (DMPD), and nitric oxide (NO) radical scavenging assays as well as ferric ion-chelation capacity, ferric-(FRAP), and phosphomolybdenum-reducing antioxidant power (PRAP). The phytochemical analyses have been performed on both of the plant samples. GC–MS analysis pointed out that α-phellandrene was the main component in both of the essential oils in varying amounts (47.75% for AG-O and 27.94% for AG-C), while oleic acid was the dominant in the fruit oils of two samples (36.39% for AG-O and 53.87% for AG-C). HPLC analysis showed that both of the extracts contained rosmarinic acid as the major phenolic acid. The extracts inhibited BChE at moderate level, while the ethanol extracts exerted remarkable NO scavenging effect. The results emphasize that cultivation conditions may have effect on bioactivity and phytochemical content on plant samples.