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Kodhati, Venkateshwarlu,Vanga, Malla Reddy,Yellu, Narsimha Reddy Korean Chemical Society 2013 대한화학회지 Vol.57 No.2
The synthesis of title compounds were accomplished by synthetic sequence shown in Scheme 1. Chalcones on cyclocondensation with thiourea in ethanol and potassium hydroxide under reflux yielded the respective dihydropyramidin-2(1H)-thiones. Each of the dihydropyrimidin thiones was, then subjected to the Mannich condensation in alkaline medium using three different secondary amines, viz., dimethylamine, diethylamine and morpholine to obtain a new series of S-Mannich bases. All the synthesised compounds ($C_1-C_{15}$) were evaluated for their antiulcer and antibacterial activities. Compounds $C_4$, $C_5$, $C_6$, $C_{14}$ and $C_{15}$ exhibited relatively more potent antiulcer activity but not comparable to the standard; Omeprazole, while $C_1$, $C_2$, $C_3$ and $C_{13}$ were moderate in activity at 100 mg/kg p.o. All the compounds ($C_1-C_{15}$) showed mild to moderate activity against both Gram-positive (S.aureus, L.delbrueckii) and Gram-negative (P.vulgaris, E.coli) bacteria. Amongst the compounds tested, only $C_6$, $C_9$, $C_{12}$ and $C_{15}$ were found to be potent.
Karanth, Santhosh,Sharma, Prakash,Pal, Asim K.,Venkateshwarlu, G. Asian Australasian Association of Animal Productio 2009 Animal Bioscience Vol.22 No.4
Two experiments in the sequential order were conducted to determine the effects of different dietary lipid sources on the growth and fatty acid composition of rohu (Labeo rohita) and to examine the viability of a return fish oil finisher diet in restoring the human cardio-protective fatty acid profile. In the first experiment, fish were fed either with coconut oil (D1), olive oil (D2), sunflower oil (D3), linseed oil (D4) and fish oil (D5) as the main lipid source in the isonitrogenous diet for 90 days. No significant differences in growth were observed. Among the experimental diets moisture content of fish varied significantly (p<0.05) between the groups. Dietary lipid sources had a profound influence on the fatty acid profile of the muscle and liver as tissue fatty acid profile reflected the dietary fatty acid composition. Increased amounts of eicosapentaenoic acid and docosahexaenoic acid were observed in tissue of fish fed D4 and arachidonic acid was observed in the tissue of fish fed D3. We have also detected the metabolites of n-3 and n-6 pathway in D4 and D3 groups respectively, which prompted us to conclude that rohu, can desaturate and elongate $C_{18}$ essential fatty acids to $C_{20}$ and $C_{22}$ HUFA. A second feeding trial was conducted using the animals from the five different treatment groups for the duration of 30 days with fish oil rich diet (D5). Feeding with fish-oil rich washout diet resulted in the near equalization of all the other treatment groups tissue fatty acid profiles to that of fish oil (D5) fed group. These results indicate that a finishing fish oil diet can be effectively used to restore the human cardioprotective fatty acid profile in rohu fed with vegetable oils as lipid source.
HariKrishna Devalapally,Raghavendra Swamy Navath,Venkateshwarlu Yenamandra,RaghuRam Rao Akkinepally,Rama Krishna Devarakonda 대한약학회 2007 Archives of Pharmacal Research Vol.30 No.6
Anthracycline antibiotics, particularly doxorubicin and daunorubicin, have been used extensively in the treatment of human malignancies. However cardiotoxicity and multidrug resistance are significant problems that limit the clinical efficacy of such agents. Rational design to avoid these side effects includes strategies such as drug targeting and prodrug synthesis. Described here are the synthesis and preliminary biological evaluation of the enzymatically activated two new prodrugs (6 & 11) of doxorubicin. These prodrugs were designed as potential candidates for selective chemotherapy in ADEPT or PMT strategies. They are constituted of a galactose moiety, a spacer and the cytotoxic drug and they differ by the type of spacer. The prodrugs were stable in a buffer, and the in vitro studies showed good detoxification and hydrolysis kinetics. As prodrug 11 was readily hydrolyzed, this could be a valuable candidate for further development.
Devalapally, Harikrishna,Navath, Raghavendra Swamy,Yenamandra, Venkateshwarlu,Akkinepally, RaghuRam Rao,Devarakonda, Rama Krishna 대한약학회 2007 Archives of Pharmacal Research Vol.30 No.6
Anthracycline antibiotics, particularly doxorubicin and daunorubicin, have been used extensively in the treatment of human malignancies. However cardiotoxicity and multidrug resistance are significant problems that limit the clinical efficacy of such agents. Rational design to avoid these side effects includes strategies such as drug targeting and prodrug synthesis. Described here are the synthesis and preliminary biological evaluation of the enzymatically activated two new prodrugs (6 & 11) of doxorubicin. These prodrugs were designed as potential candidates for selective chemotherapy in ADEPT or PMT strategies. They are constituted of a galactose moiety, a spacer and the cytotoxic drug and they differ by the type of spacer. The prodrugs were stable in a buffer, and the in vitro studies showed good detoxification and hydrolysis kinetics. As prodrug 11 was readily hydrolyzed, this could be a valuable candidate for further development.
H.N. Shivaprasad,M. Bhanumathy,G. Sushma,T. Midhun,K.R. Raveendra,K.R. Sushma,K. Venkateshwarlu 한국식품영양과학회 2013 Journal of medicinal food Vol.16 No.6
The present randomized, double-blind, placebo-controlled study evaluated the efficacy and safety of Salacia reticulata leaves and root bark extracts in 29 patients with prediabetes and mild to moderate hyperlipidemia. Patients received either Salacia extracts (500 mg/day) or placebo along with therapeutic lifestyle changes for a period of 6 weeks. Efficacy was evaluated in terms of change in lipid profile and glycemic levels. The safety and tolerability was evaluated by a physical examination and clinical laboratory evaluations. Improvements in lipid profiles and glycemic levels were observed in Salacia extract-treated groups when compared to placebo at week 6. A statistical significant reduction was observed in low-density lipoprotein cholesterol and fasting blood sugar (FBS) levels at week 3 and 6 when treated with root bark extract. The leaves extract-treated group showed statistically significant reduction in FBS levels at week 6 only. No adverse events occurred and all safety parameters were within normal ranges during the study. This study revealed that treatment with S. reticulata was safe and well-tolerated and may be beneficial in the management of prediabetes and mild to moderate hyperlipidemia.