N-Methylation has a significant impact on improving the oral bioavailability, lipophilicity and aqueous solubility of peptide-based lead drug structures. The selected mono-amino acid derivatives Ac-X-OMe, where X = Gly, Val, Leu, Ile, Phe, Met, Cys, Ser, Asp and His as well as their corresponding N-methylated analogues were studied. The clog P values of all N-methylated peptides are greater than those of native compounds. Quantum chemical calculations were performed to estimate the aqueous solubility of these lipophilic compounds using density functional theory (DFT). To confirm the contribution of dispersion forces on quantum chemical data, the long-range corrected (LC) hybrid density functional (ωB97X-D) was also probed for some amino acid derivatives. The ωB97X functional gave similar results. Our results reveal that after mono N-methylation of the peptide backbone, ΔGsolv becomes more negative (more water soluble) while polarizability and dipole moment are also increased. Natural atomic charges derived by natural bond orbital (NBO) analysis of N, C, and O atoms involved in amide functional group become more positive/(less negative) after N-methylation. All N-methylated amino acids have higher EHOMO (less negative) in comparison with the amino acid analogues, and in all cases N-methylation decreases EHOMO-LUMO. The calculated amide cis/trans activation energies (EA) of all the N-methylated amino acid derivatives were lower than that of native species. N-methylation of these compounds leads to an increase in lipophilicity, aqueous solubility, polarization, dipole moment and lowering of the cis/trans amide energy barrier (EA).

SUMMARY:The present observation was aimed to evaluate the gross and histometric parameters of the vesicular glands of indigenous bulls. Twenty-eight bulls of three age groups were selected from the local market: the pre pubertal group A (<1 year n=4), pubertal group B (1.5-2.5 years, n=16) and post pubertal or adult group C (above 3 years, n=8). The weight, length (anterio-posterior), width (latero-medial) and the thickness (dorso-ventral) of the both left and right vesicular glands were recorded separately after slaughter of each animal. The left and right vesicular gland shows significantly different (p<0.01), in weight and length in every group. Left vesicular glands were slightly higher than the right in all parameters. The lobules of the gland showed folded mucosa, lined with pseudostratified columnar epithelium. Three types of cells were identified in the epithelium containing A, B and C cell. Type A cells were tall columnar cells having distinct cell boundaries with the oval, round or elongated nucleus. Type B cells were located in the basal lamina having round or oval nucleus with indistinct cell boundaries. Type C cells were narrow columnar cells interspersed between A cells with darkly stained cytoplasm. Lamina propria consisted of loose connective tissue surrounded the alveoli, tubules and some solid end pieces. The numbers of secretory end pieces were variable. The diameters of luminated or non-luminated acini of the glandular end pieces and ducts were increased gradually and significantly (p<0.01) with the advancement of age. The epithelial height of the duct and alveoli were increased with the advancement of age, but no significantly differences among them. Tunica adventitia and muscularis grew with the advancement of age while the interstitial tissue shrunk equally. Above all parameters help to conclude that the vesicular glands of the pubertal indigenous bulls were more functional.

To investigate the epidemiology of fascioliosis in cattle of different ages, sexes, seasons and different district in Sylhet division of Bangladesh. Epidemiological studies on fascioliosis of cattle were under taken in such localities under different climatic conditions existing in Sylhet division of different district. Cattle were divided into young and adult groups. Rectal fecal samples from household live and livers from slaughterhouse cattle were collected randomly and examined by direct/and sedimentation techniques and grossly from July 2014 to June 2015. A total of 920 liver samples from slaughter house and 920 rectal fecal samples from household live cattle were examined of which 139 (15.11%) slaughter house and 204 (22.17%) household live cattle were found positive for Fasciola gigantica. The overall prevalence was 18.64%. It was noticed that prevalence of slaughterhousewere 1.5 times less susceptible than household live cattle. The prevalence of fascioliosis was significantly (p<0.001) higher in rainy season followed by winter and summer season. Significantly (p <0.001) the highest prevalence of fascioliosis was recorded in young's. When considered the relationship with sex, the prevalence of fascioliosis in female's cattle was significantly (p <0.001) more than males. Fascioliosis is highly prevalent in both slaughterhouse and household live cattle in Sylhet division of Bangladesh. Effective control measures to proper management, improved hygiene and the strategic use of regular deworming is need for the treatment of intensive fascioliosis in cattle.

keçilerinde fascioliasisin (Fasciola gigantica) epidemiyolojik çalışması. Amaç: Siyah Bengal keçilerinde farklı yaş, cinsiyet ve mevsimde facioliasisin epidemiyolojisini araştırmaktır. Gereç ve Yöntem: Siyah Bengal keçilerindeki fascioliasisinin epidemiyolojik araştırması Upazilla'nın beş farklı bölgesinin Sylhet bölgesinde farklı iklim koşulları altında gerçekleştirildi. Keçiler genç ve yaşlı olmak üzere iki gruba ayrıldı. Temmuz 2012-Haziran 2013 döneminde çiftliklerdeki keçilerden rektal sıvap örnekleri ve mezbahalardan karaciğer örnekleri toplandı. Örnekler direk/sedimentasyon teknikleri ve makroskobik olarak incelendi. Bulgular: Toplamda 1288 rektal sıvap ve 2000 karaciğer örneği incelendi. Bunlardan çiftlik keçilerinin 405 (%31.75) ve kesilen keçilerin 202 (%10.10)'u Fasciola gigantica açısından pozitif bulundu. Genel prevalans %20.93 olarak belirlenirken, çiftlik keçilerindeki prevalans kesilen keçilerden yüksek belirlendi. Genel prevalans yağmurlu mevsimde yüksek ve yaz mevsiminde düşük belirlendi. Gençlerde yüksek prevalans belirlenirken, dişilerde erkeklerden yüksek tespit edildi. Öneri: Bangladeş'te evde beslenen ve kesime sevk edilen siyah Bengal keçilerinde yoğun olarak fascioliasis bulunmaktadır. Siyah Bengal keçilerinde yoğun olarak gözlenen fascioliasisin tedavisi için etkili kontrol ile stratejik antelmentik uygulamasına ihtiyaç bulunmaktadır.

Mutation causes inactivation of 'p53' tumor suppressor protein in almost fifty percent of cancers in humans. Outside the DNA-binding surface of p53, Y220C is the most common cancerous mutation. Previous studies have shown that a surface cavity is created by this mutation which destabilizes p53. PhiKan083, a carbazole derivative capable of binding with that cavity, and slows down its thermal denaturation rate. We investigated, theoretically, on mechanisms of structural stability loss due to Y220C mutation and mechanisms of stability restoration by PhiKan083 at the atomic level. From this study it is found that in Tp53C, Tyr220 has five electrostatic interactions with residues Val 147, Prol51, Pro153 and Pro223 located on S3/S4 loop and S7/S8 loop. The S7/S8 loop is stabilized by these electrostatic interactions. Due to the Y220C mutation all these electrostatic interactions are lost. As a result the structural fluctuation occurs at S7/S8 loop, and the loop is displaced from its original position after 6 ns MD simulation. When PhiKan083 is present (inserted) at the mutation site it provides five electrostatic interactions with Pro155, Glu221 and Thr230, and two hydrogen bonds with Leu145 and Asp228, respectively. These interactions provided by Pkikan083 stabilized the S7/S8 loop, and as a result it couldn't be displaced. Our results showed that due to Y220C mutation p53 became destabilized through structural fluctuations surrounding the mutation site. When PhiKan083 is present at the Y220C mutation site (in 2vuk), it provides electrostatic and hydrogen bonding interactions among residue-220, its neighboring residues and PhiKan08. These interactions give additional stability to Y220C mutant p53, thus Y220C mutant p53 doesn't destabilize.