174 research outputs found

    Synthesis of the western hemisphere of theonellamide C

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    Theonellamides A-F were isolated from Theonella swinhoei by Fusetani and co-workers. Despite considerable synthetic effort to produce theonellamide F by the Shioiri group in the early 1990’s, the total synthesis of a theonellamide has yet to be reported. We report herein our efforts toward some of the required amino acid residues and construction of the western ring of theonellamide C. We describe the synthesis of an uncoded amino acid, (2S,4R)-ɣ-hydroxy-α-amino adipic acid (Ahad), a building block for theonellamide C. We initially investigated the Corey-Lygo method for the catalytic asymmetric generation of the Cα stereocenter. Unfortunately, the alkylation of glycine benzophenone imines with a series of electrophiles, including [(S)-benzyl-3-(tert-butyl dimethylsilyl)oxy]-4-iodobutanoate (104a), was unsuccessful due to low inherent reactivity and steric hindrance. A second approach was based on MacMillan’s enantioselective organocatalytic amine conjugate addition. Addition of CbzNHOTBS (136a) to (E)-benzyl-4-oxo-but-2-enoate (149), in the presence of catalytic (S)-2-diphenyl[trimethylsilyl)oxy]methylpyrrolidine (165) led to β-amino aldehyde (S)-benzyl 2-[(benzyloxycarbonyl)(tert-butyldimethylsilyloxy)amino-4-oxo-butanoate, (148a). A Wittig reaction between 148a and methyl-(triphenylphosphoranylidene)-acetate (142) afforded (2S,4E)-1-benzyl-2-[(benzyloxycarbonyl)(tert-butyldimethylsilyloxy)-amino-6-methyl-hex-4-enedioate (147a). The ɣ-hydroxy group was installed intramolecularly with 4:1 d.r. by treatment of 147a with TBAF. Hydrogenolysis was carried out to give unprotected Ahad. The next challenge was to find the right combination of protecting groups for Ahad that would be compatible with the synthesis of the western hemisphere of theonellamide C. We performed model studies on α-aminoadipic acid (α-AAA) which revealed that the δ-COOMe, introduced in the Wittig reaction, was incompatible with a Cα-acetol ester and a Nα-Alloc carbamate. α-AAA and Ahad bearing a δ-COOtBu group were synthesized in an analogous fashion. The Ahad building block was synthesized in 11 steps and 6.5% overall yield. In readiness for coupling; the tert-butyl ester was cleaved to afford the free δ-acid. Two tetrapeptides were assembled: Boc-Asn-HyAsn(OTBS)-Phe-β-Ala-OAll (249) and the simplified Fmoc-Asn(Trt)-Asn(Trt)-Phe-β-Ala-OAll (254). Removal of the N-terminal Fmoc-group from 254 and coupling with a suitably protected t-histidinoalanine acid afforded a linear hexapeptide that is a precursor to the western hemisphere of theonellamide C

    Awareness of farm workers regarding health problems and use of protective clothing during pesticide application

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    Pesticides are widely used in agricultural production to prevent or control pests, diseases, weeds, and other plant pathogens in an effort to reduce or eliminate yield losses of cotton crop and maintain high product quality. Because of high biological activity, and in some cases, long persistence in the environment, pesticides (pyrethroids, carbamate, oganophosphate, organochlorines) may cause harmful effects to human health and to the environment. Occupational exposure to pesticides often occurs in the case of agricultural workers in open fields and greenhouses. Farmers who perform spray activity are routinely exposed to high levels of pesticides (Monocarbamide dihydrogen sulfate, pyrethroids and carbamates), than the other farm workers such as pesticide loader, evaluator. The dermal and inhalation routes of entry are typically the most common routes of farmers’ exposure to pesticides. Farmers’ exposure to pesticides can be reduced through less use of pesticides and use of the appropriate protective clothing and equipments in all stages of pesticide handling. The present study was conductedon 270 respondents from all nine blocks of Hisar district of Haryana state to create awareness amongst them regarding health problems and use of protective clothing during pesticide application.An educational package in the form of Video CD and Leaflet was used. Pamphlets were distributed; lecture-cum-demonstrations and film shows were organized. Protective clothing and accessories were also exhibited for better impact. It was recorded that respondents succeeded in acquiring awareness at post exposure level, through print and electronic media for each message viz. breathing problems (23.3%), eyes related problems (100%), skin allergy (43.3%), headache (60.3%), fainting due to inhalation of pesticide (64.33%) and stomach related problems (23.56%). &nbsp

    Effect of microencapsulated plant extracts on mosquito repellency

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    Mosquitoes are the most important single group of insects in terms of public health importance. Mosqui-toes not only cause nuisance by their bites but also transmit deadly diseases. The activity of mosquitoes is affected by climate, light and temperature. In tropical areas like India, the population of mosquitoes is found huge day by day. Repeated use of synthetic insecticides for mosquito control has disrupted environment as well as human health. To overcome this problem, plant derived compounds may be the better alternate over synthetic insecticides. To enhance the health and hygiene qualities by means of use of medicinal plants through effective application technique on textiles, marigold (petals) and nirgundi (leaves) methanol extract was used as mosquito repellent finish on 100 % woven cotton. For applying mosquito repellent finish on fabric, complex coacervation technique of microencapsulation was used through pad-dry-cure method. Finished cotton samples were tested against Anopheles stephensi by using laboratory cage method for their efficacy and durability to washing and sun-drying as per standard test methods. Marigold (petals)and nirgundi (leaves) extract finished fabric samples showed 96 and 94 % repellency respectively after 60 minutes of observation. It remained 56 % and 54 % (after 15 washes) and 54 and 52 % (after expo-sure in sun for 3 hours) by the application of marigold and nirgundi extracts respectively. Hence, microencapsulation technique on selected cotton textile proved effective to repel mosquitoes up to acceptable level according to WHO (1996)

    Integration of ICT in Classroom: Some Reflections

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    Many studies have been conducted to investigate barriers to the integration of ICT in education.  This paper provides a meta-analysis of this literature that aims to present the perceived barriers of technology integration in education and particularly teacher level barriers are highlighted here. This analysis aims to bring together the findings and key points from a review of a significant part of the available literature associated with teachers’ integration of ICT into their teaching. Studying the obstacles to the use of ICT in teaching and learning environments is crucial because this knowledge could provide guidance for ways to enhance technology integration and encourage greater use of ICT on the part of teachers themselves. Identifying the fundamental barriers may assists teachers and educators to overcome these barriers and become successful technology adapters

    EVALUATION OF MUTAGENIC EFFECT (ANTIMUTAGENIC) OF DALBERGIA LATIFOLIA ON SWISS ALBINO MICE

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    Dalbergia latifolia Roxb. (Family: Fabaceae) is a traditional herb, contain latinone and     dalcriodain flavonoid having excellence medicinal value8.Thepresentstudy wasdesignedtoevaluatetheanti-mutagenicpotentialofMethanolic extractof Dalbergia latifolia,usingmicronucleus(MN)andchromosomalaberration(CA)assay inmice bonemarrow.Theanti-mutageniceffectofDalbergia latifoliawasassessed usingcyclophosphamideMNformationandCAinmice.Theanimalswerepre-treatedwiththe MethanolicextractofDalbergia latifoliaorallyattwodosesof100, 200mg/kgbody weightforsevendays.InMNandCAtestthetwodosesprovidedprotectionwhengiven24hrs priortoasinglei.padministrationofcyclophosphamide(100mg/kgbodyweight). Theseresults demonstrate thatMethanolic extractofDalbergia latifoliahas got anti-mutagenic potential.Keywords: Dalbergia latifolia, Methanolic extract, anti-mutagenic activit

    Neuroprotective and hepatoprotective effect of whole red rice forms against oxidative stress in streptozotocin induced diabetic rats.

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    151-160Whole red rice (Oryza sativa L.), consumed as staple food in many countries worldwide, is rich in phytochemicals, mainly antioxidants having health potency. The present study evaluated the neuro- and hepatoprotective efficacy of raw and parboiled whole red rice against streptozotocin (STZ) induced oxidative stress, and antioxidant metabolism both in diabetic and normal non-diabetic rats. Wistar rats were rendered diabetic by a single intraperitoneal (i.p.) injection of streptozotocin (45 mg/kg body wt.), supplemented with raw and parboiled whole red rice for six weeks. Results revealed a drastic increase in oxidative stress markers, such as lipid peroxidation, nitric oxide (NO) level, hydroperoxide (HP) level; antioxidant enzymes superoxide dismutase (SOD), catalase (CAT), glutathione peroxidase (GPx), glutathione reductase (GR), thioredoxin reductases (TR), glutathione S-transferase (GST), acetylcholinesterase (AChE) activity, and decrease in endogenous antioxidant, glutathione (GSH) in diabetic rat. On the other hand, addition of raw and parboiled whole red rice in the diet counteracted the STZ induced oxidative stress in diabetic groups and improved the neuro and hepatic antioxidant system. Both, parboiled and raw red rice forms, exercised similar impacts in diabetic as well as in normal rats suggesting improved antioxidant defence mechanism. Results have shown that the whole red rice possess antidiabetic potential with the antioxidant improving ability, and could be utilized as dietary supplements in diabetes management

    Efficacy of different doses of NPK on growth and yield of rice bean (Vigna umbellata) in Khadbari, Sankhuwasabha, Nepal

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    An essential cultural technique for ensuring correct development and maximizing output is administering fertilizer sources for the crops. The experiment was carried out from February 2022 to May 2022 at Khadbari-3, Maruwa, Sankhuwasabha, to determine the efficacy of various dosages of NPK on the growth performance of the rice bean variety (Sunehri). The trial used a Randomized Complete Block Design (RCBD) with seven treatments replicated three times. The treatments were listed and named as T1 (0:0:0 kg NPK/ha); T2 (20:30:10 kg NPK/ha) (Recommended dose); T3 (10:20:15 kg NPK/ha); T4 (40:80:40 kg NPK/ha); T5 (20:20:20 kg NPK/ha); T6 (80:100:60 kg NPK/ha); and T7 (20:0:30 kg NPK/ha), respectively. The experimental results revealed that the highest yield/plant (39g) was obtained from the plot treated with T4 (40:80:40 kg NPK/ha), followed by 24.93 g and 24.13 g from the plot receiving T2 (20:30:10 kg NPK/ha) and T6 (80:100:60 kg NPK/ha), respectively. The lowest yield of 14.07 g was obtained from the control plot, followed by 15.27 g and 21.20 g from the plot receiving T7 (20:0:30 kg NPK/ha) and T3 (10:20:15 kg NPK/ha), respectively. Vegetative parameters such as plant height, branch numbers, and leaves numbers were recorded as a maximum of 19.72 cm, 6.88, and 18.97 in plots treated with T5 (20:20:20 kg NPK/ha), T7 (20:0:30 kg NPK/ha), and T1 (0:0:0 kg NPK/ha), consecutively, and corresponding minimum values were found 18.12 cm, 5.36 and 15.63 in T3 (10:20:15 kg NPK/ha), T1 (0:0:0 kg NPK/ha), and T7 (20:0:30 kg NPK/ha), respectively. Conclusively, the study's findings suggest that the rice bean crop responds to fertilizers and applying T4 (40:80:40 kg NPK/ha) enhances crop production considerably

    Traditional Knowledge – Going Multidimensional

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    Traditional knowledge (TK) is going multidimensional. On one side it is penetrating Intellectual Property Rights (IPR) marking its association, besides Patents, with Trade Marks, Copyrights, Geographical Indication. On the other hand, the debate as to the protection of TK at the international level is gaining whilst becoming complex. The said debate is, still, not mature enough to have a legal protection covering benefit sharing. The paper discusses the multidimensional nature of TK. It is desired that this would throw light on different aspects of TK whilst analyzing that TK is really a complex concept when it comes to securing an international protection regime. The paper may allow ways to secure protection after witnessing the multidimensional nature of TK

    Assessment of optimal growth conditions for specific carotenoids production by Chlorella vulgaris

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    Exploration of regional microalgae for carotenoids production under optimized cultural conditions is a sustainable economic and technical perspective. This study details comprehensive research on the influence of growth conditions on microalgal carotenoids. Carotenoid triggering factors were optimized to identify suitable growth conditions to produce specific carotenoids by Chlorella vulgaris.  Media optimization and cultivation conditions were the factors considered and the results revealed the optimum growth conditions for carotenoid production by C. vulgaris was pH 8, 35°C temperature, 0.04 M salinity and 160 µE\m²\sec light intensity. Among the nutrient sources, potassium nitrate and potassium phosphate were suitable for nitrogen and phosphorous supplements. The results indicated optimizing the culture conditions and nutrient sources help to attain desirable carotenoid production by C. vulgaris. Specific carotenoids were extracted from the algal extract and were identified by high-performance liquid chromatography in which lutein (8.8%) was present as major carotenoid followed by astaxanthin (4.6%) and ?-carotene (3.9%). This study revealed that that carotenoid production by C. vulgaris could be enhanced by manipulating culture conditions thereby attain desirable carotenoid production.
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