Stimulation of ATPase activity in barley (Hordeum vulgare) root plasma membrane after treatment of intact tissues and cell free extracts with triacontanol

Ca²⁺- and Mg²⁺-dependent ATPase activity (EC 3.6.1.3) in a plasma membrane-enriched fraction increased rapidly after in vivo application of physiologically active concentrations of triacontanol (TRIA) to the roots of barley ( Hordeum vulgare L. cv. Conquest) seedlings. Ca²⁺- and Mg²⁺-dependent ATPase activity was 64 and 85% higher, respectively, in the roots of seedlings germinated in the presence of growth-promoting concentrations of TRIA compared to controls. The increase in vivo was concentration dependent, with the greatest increase obtained at 2.3 n M TRIA. Maximal stimulation of ATPase activity of excised tissue treated with TRIA coincided with the temperature at which the barley was grown. At this temperature the plasma membrane is primarily in a mixed gel/liquid crystalline state. Pretreatment of barley roots with cyclohexamide did not alter ATPase stimulation by TRIA. Two to three times more [¹⁴C]-TRIA (mg membrane protein)⁻¹ was found associated with plasma membrane-enriched vesicles treated with TRIA than with vesicles enriched for mitochondrial membranes or for vesicles enriched for tonoplast, Golgi and rough endoplasmic reticulum. Both Ca²⁺- and Mg²⁺-dependent ATPase activity increased by 40–60% within 30 min of the addition of 2.3 n M TRIA to cell-free extracts of barley roots. The addition of octacosanol, the C₂₈ analogue of TRIA, to cell-free extracts did not affect metal-dependent ATPase activity. Consistent with many studies in the green-house, simultaneous additions of equimolar amounts of TRIA and octacosanol to cell-free extracts resulted in inhibition of ATPase stimulation by TRIA. TRIA may directly affect plasma membrane function in barley roots.     

Synthesis,characterization and in vitro biological evaluation of some novel 1,3,5-triazine–Schiff base conjugates as potential antimycobacterial agents

A series of some novel 1,3,5-triazine–Schiff base conjugates (1–32) have been synthesized and evaluated for their in vitro antimycobacterial activity against Mycobacterium tuberculosis H37Rv using Alamar Blue assay and the activity expressed as the minimum inhibitory concentration (MIC) in μg/mL. Compounds 4 (4-Methoxy-6-methyl-N-(3,4,5-trimethoxybenzylidene)-1,3,5-triazin-2-amine), 11 (4-Methoxy-6-methyl-N-(2-hydroxy-3-bromo-5-chloro-benzylidene)-1,3,5-triazin-2-amine) and 24 (4-Methoxy-6-methyl-N-(1-(2,5-dihydroxyphenyl)ethylidene)-1,3,5-triazin-2-amine) exhibited a significant activity at 3.125, 6.25 and 6.25 μg/mL, respectively, when compared with the antitubercular drugs such as ethambutol (3.125 μg/mL), pyrazinamide (6.25 μg/mL) and streptomycin (6.25 μg/mL) and it could be a potential starting point to develop new lead compounds in the fight against Mycobacterium tuberculosis H37Rv.     

Bioactive compounds from Stuhlmannia moavi from the Madagascar dry forest

Bioassay-directed fractionation of the leaf and root extracts of the antiproliferative Madagascar plant Stuhlmannia moavi afforded 6-acetyl-5,8-dihydroxy-2-methoxy-7-methyl-1,4-naphthoquinone (stuhlmoavin, 1) as the most active compound, with an IC₅₀ value of 8.1 μM against the A2780 human ovarian cancer cell line, as well as the known homoisoflavonoid bonducellin (2) and the stilbenoids 3,4,5′-trihydroxy-3′-methoxy-trans-stilbene (3), piceatannol (4), resveratrol (5), rhapontigenin (6), and isorhapontigenin (7). The structure elucidation of all compounds was based on NMR and mass spectroscopic data, and the structure of 1 was confirmed by a single crystal X-ray analysis. Compounds 2?5 showed weak A2780 activities, with IC₅₀ values of 10.6, 54.0, 41.0, and 74.0 μM, respectively. Compounds 1?3 also showed weak antimalarial activity against Plasmodium falciparum with IC₅₀ values of 23, 26, and 27 μM, respectively.     

Characterization of saponins and phenolic compounds: antioxidant activity and inhibitory effects on α-glucosidase in different varieties of colored quinoa (Chenopodium quinoa Willd)

ABSTRACT

This study investigated the contents of saponins and phenolic compounds in relation to their antioxidant activity and α-glucosidase inhibition activity of 7 colored quinoa varieties. The total saponin content was significantly different among 7 varieties and ranged from 7.51 to 12.12 mg OAE/g DW. Darker quinoa had a higher content of phenolic compounds, as well as higher flavonoids and antioxidant activity than that of light varieties. Nine individual phenolic compounds were detected in free and bound form, with gallic acid and ferulic acid representing the major compounds. The free and bound phenolic compounds (gallic acid and ferulic acid in particular) exhibited high linear correlation with their corresponding antioxidant values. In addition, the free phenolic extracts from colored quinoa exhibited higher inhibitory activity against α-glucosidase than the bound phenolic extracts. These findings imply that colored quinoa with abundant bioactive phytochemicals could be an important natural source for preparing functional food.     

Isolation of a Novel Carotenoid,OH-chlorobactene Glucoside Hexadecanoate,and Related Rare Carotenoids from Rhodococcus sp. CIP and Their Antioxidative Activities

In the course of screening for antioxidative carotenoids from bacteria, we isolated and identified a novel carotenoid, OH-chlorobactene glucoside hexadecanoate (4), and rare carotenoids, OH-chlorobactene glucoside (1), OH-γ-carotene glucoside (2) and OH-4-keto-γ-carotene glucoside hexadecanoate (3) from Rhodococcus sp. CIP. The singlet oxygen (¹O₂) quenching model of these carotenoids showed potent antioxidative activities IC₅₀ 14.6 μM for OH-chlorobactene glucoside hexadecanoate (4), 6.5 μM for OH-chlorobactene glucoside (1), 9.9 μM for OH-γ-carotene glucoside (2) and 7.3 μM for OH-4-keto-γ-carotene glucoside hexadecanoate (3).     

Design and development of ethosomal transdermal drug delivery system of valsartan with preclinical assessment in Wistar albino rats

Abstract

Valsartan (VLT) is a highly selective and orally active antihypertensive drug. However, its oral administration is associated with drawbacks like low bioavailability. The objective of this study was to design and develop a transdermal delivery system for VLT using ethosomal carriers to investigate their enhanced transdermal delivery potential. VLT ethosomes were prepared by cold method. VLT ethosomes were characterized by scanning electron microscopy. The prepared ethanolic liposomes were characterized to be spherical having low polydispersity of nano-size range with good entrapment efficiency. ETC5 ethosomal suspension with 4% of phospholipon 90H and 40% of ethanol was found to have highest entrapment efficiency, i.e. 80.230?±?0.8748%. The permeation study of ethosomes was evaluated by ex vivo diffusion study through rat abdominal skin using Franz’s diffusion cells and ETC5 ethosomal suspension was found to have highest permeation with flux of 92.819?±?1.539?µg/cm²/h, when compared to the permeation profiles of drug solutions either in water or in a water–ethanol mixture. Transdermal application of ethosomal VLT on Wistar rats showed better and prolonged antihypertensive activity in comparison to orally administered VLT suspension by virtue of transdermal permeation through Wistar rat skin. Histopathological study of skin applied with ETC5 showed intercellular permeation across skin by dissolving intercellular lipids in epidermis without causing any rigorous changes in the skin cellular structure. In conclusion, ethosomes enabled the transdermal permeation of VLT, which amply proves its superiority over oral administration for antihypertensive treatment.     

伊洛河流域外来草本植物分布格局

外来生物入侵及其防治已经成为生态学关注的重点和热点问题.目前的研究主要集中在外来入侵种上,然而入侵种仅占外来种中很少一部分,因此,研究外来种现有分布格局对研究生物入侵及其防治有重要意义.以伊洛河流域草本植物群落中的外来种为对象,沿河从河源地到入黄河口选取典型样地,在调查流域内草本植物群落中物种组成的基础上选取外来种,并对外来种种类组成及其分布格局进行研究.结果表明:流域内有外来草本植物27种,分属于15科,种类较多的科为菊科、苋科和豆科;引入方式以有意引种为主.流域横向不同生境间,河滩地在水流的养分富集、季节性洪水物理干扰及人为活动扰动作用下,呈现出受外来种分布较多,而受人类活动扰动最强且营养丰富的农田分布较小的分布格局;纵向环境梯度下,上游河源山地属于自然植被区,人为干扰较轻,且受外来种影响较小;中游丘陵区从自然生态系统向农业生态系统的过渡区域,人类活动的扰动有所加强;下游平原农业区,人类活动强烈,区域内以人工生态系统为主,群落物种组成简单但受外来种影响最大,受自然环境和人类活动的双重影响.不同物种在不同生境间差异明显,其中,小蓬草、钻叶紫菀和反枝苋广泛分布于3种生境中.总体上,伊洛河外来草本植物分布格局在自然因素的基础上强烈受人为因素的影响,呈现出从上游到下游逐渐增多的趋势.     

Biocides formulation of essential oils having antimicrobial activity

Essential oils of fennel, peppermint, caraway, eucalyptus, geranium and lemon were tested for their antimicrobial activities against some plant pathogenic micro-organisms (Fusarium oxysporum, Alternaria alternate, Penicilium italicum Penicilium digitatum and Botyritus cinerea). Essential oils of fennel, peppermint, caraway were selected as an active ingredient for the formulation of biocides due to their efficiency in controlling the tested micro-organisms. Successful emulsifiable concentrates (biocides) were prepared from these oils using different emulsifiers (Emulgator B.L.M. Tween20 and Tween80) and different fixed oils (sesame, olive, cotton and soybean oils). Physico-chemical properties of the formulated biocide (spontaneous emulsification, emulsion stability test, cold stability and heat stability tests as well as viscosity, surface tension and pH) were measured. The prepared biocides were ready to be tested for application in a future work as a safe pesticide against different pathogens.     

Holocene vegetation history of the Sahel: pollen, sedimentological and geochemical data from Jikariya Lake, north-eastern Nigeria

Aim This study aims to separate regional and local controls on Holocene vegetation development and examine how well pollen records reflect climate change in a semi‐arid region. The relative importance of climate and human activity as agents of vegetation change in the Sahel during the late Holocene is also considered. Location Jikariya Lake, an inter‐dune depression in the Manga Grasslands of north‐eastern Nigeria. Methods Pollen and charcoal were used to provide a record of Holocene vegetation history. Palaeoclimate and hydrological changes were reconstructed from sedimentary and geochemical data. Regional and local influences were separated by comparing the evidence obtained from Jikariya Lake with previously published data from the Manga Grasslands. Results The Manga Grasslands experienced a prolonged wet period during the early and mid‐Holocene, during which swamp forest vegetation with Guinean affinities (Alchornea, Syzygium, Uapaca) occupied the inter‐dune depressions. However, variation in the pollen records between sites suggests that their establishment was dependent on conditions being locally favourable, rather than being directly coupled to regional climate. The pollen records from the Manga Grasslands are more consistent in suggesting the colonization of the dunefields by trees associated with Sudanian savanna (Combretaceae, Detarium) c. 8700 cal. yr bp . The Jikariya Lake pollen data are in accordance with the sedimentological and geochemical data from the region in indicating that the onset of arid conditions occurred progressively during the late Holocene (from c. 4700 cal. yr bp ). Abrupt changes in pollen stratigraphy, recorded at other Manga Grasslands sites 3500 cal. yr bp , appear to be the product of the local passing of ecological thresholds. The dunefield vegetation (Sahelian savanna) appears to have been resilient to (or at least palynologically silent regarding) to the climatic variability of the late Holocene. Main conclusions While climate appears to have been the primary control on vegetation development in the Manga Grasslands during the Holocene, local conditions (particularly depression size and sand influx) had a strong influence on the timing of pollen stratigraphic changes. Anthropogenic influences are difficult to detect, even during the late Holocene.