Preliminary structure-activity relationship studies on some novel s-substituted aliphatic analogues of 5-{1-[(4- chlorophenyl) sulfonyl]-3-piperidinyl}-1, 3, 4-oxadiazol-2-yl sulfide

Purpose: To study the structure-activity relationships of synthetic multifunctional sulfides through evaluation of lipoxygenase and anti-bacterial activities.Methods: S-substituted derivatives of the parent compound 5-(1-(4- chlorophenylsulfonyl) piperidin-3- yl)-1, 3, 4-oxadiazole-2-thiol were synthesized through reaction with different saturated and unsaturated alkyl halides in DMF medium, with NaH catalyst. Spectral characterization of each derivative was carried out with respect to IR, 1H - NMR, 13C - NMR and EI - MS. The lipoxygenase inhibitory and antibacterial activities of the derivatives were determined using standard procedures.Results: Compound 5e exhibited higher lipoxygenase inhibitory potential than the standard (Baicalein®), with % inhibition of 94.71 ± 0.45 and IC50 of 20.72 ± 0.34 μmoles/L. Compound 5b showed significant antibacterial potential against all the bacterial strains with % inhibition ranging from 62.04 ± 2.78, 69.49 ± 0.41, 63.38 ± 1.97 and 59.70 ± 3.70 to 78.32 ± 0.41, while MIC ranged from 8.18 ± 2.00, 10.60 ± 1.83, 10.84 ± 3.00, 9.81 ± 1.86 and 11.73 ± 5.00 μmoles/L for S. typhi, E. coli, P. aeruginosa, B. subtilis and S. aureus, respectively. Compounds 5d, 5e and 5g showed good antibacterial activity against S. typhi and B. subtilis bacterial strains.Conclusion: The results suggest that compound 5e bearing n-pentyl group is a potent lipoxygenase inhibitor, while compound 5b with n-propyl substitution is a strong antibacterial agent. In addition, compounds 5d, 5e and 5g bearing n-butyl, n-pentyl and n-octyl groups, respectively, are good antibacterial agents against S. typhi and B. subtilis.Keywords: Sulfides, Antibacterial activity, Lipoxygenase activity, Spectral analysi

Common Methods to Understand and Develop Indigenous Probiotics Yeast for Ruminant

Probiotic yeast enhanced the ruminal gut microbial balance by producing intercellular effectors and important metabolites. The impact of yeast addition on animal health is influenced by different interlinked factors including animal genomics, its gut microbiota, and environment. Therefore, all factors should be considered regarding achieving the maximum outputs from animal probiotic yeast. In the situation of a high feeding cost, microbial feed supplements provide a suitable nutritional approach, which allows increased nutrient digestion rate and accordingly improves animal performance. Many yeast products are commercially available, but their efficiency as probiotic dietary addition in a particular breed is mostly questionable. Therefore, identification of ideal probiotic yeast strain is of great interest in this context. Innovative methods in relation to develop new probiotic are mainly focused on the exploring novel microbial strains from indigenous sources. It has been noted that for the identification of best probiotic strain for the host, a linkage between culture-independent and culture-dependent methods is a functional step. In this chapter, we will discuss the mode of action of probiotic yeast on animal lower gut microbiota and identification of ideal probiotic yeast by using advanced molecular methods

Evaluating the learning environment in Dental colleges from students’ perspective; a qualitative exploratory research

Objective: Learning environment has a great role in students learning, achievement and success. It is also essential for the development of curriculum. The aim of this study is to document the perception of dental students regarding their learning environment. Material and methods: This qualitative research were conducted from Dec 2021 to May 2022, at four dental colleges of Rawalpindi. A total of 16 students from all these college who were regularly enrolled and voluntary participating in the study were included. Focus group interview (n=4 in each group) comprised of students from both basic sciences year (1st and 2nd year BDS) and clinical years (3rd and final year BDS). Data was transcribed verbatim and thematic analysis was done. Result: Students overall expressed a good level of satisfaction with the learning environment but pointed out some issue which were summed up under major themes identified such as issues in lectures, issues in clinical teaching, issue in the dental curriculum and lack of academic motivation. Conclusion: This study suggests that the dental students generally hold a positive perception towards their learning environment, but they pointed out the short comings in their lectures, clinical teaching, dental curriculum and dearth of motivation. Taking students view point regarding their learning environment will help the stake holders and policy makers to provide better learning environment with more facilities and support system for the students to enhance their learning.

S-Alkylated/aralkylated 2-(1H-indol-3-yl-methyl)-1,3,4- oxadiazole-5-thiol derivatives. 2. Anti-bacterial, enzymeinhibitory and hemolytic activities

Purpose: To evaluate the antibacterial, enzyme-inhibitory and hemolytic activities of Salkylated/aralkylated 2-(1H-indol-3-ylmethyl)-1,3,4-oxadiazole-5-thiol  derivatives.Methods: Antibacterial activities of the compounds were evaluated using broth dilution method in 96 well plates. Enzyme inhibitory activities assays were investigated against α-glucosidase, butyrylcholinesterase (BchE) and lipoxygenase (LOX) using acarbose, eserine and baicalien as reference standards, respectively. A mixture of enzyme, test compound and the substrate was incubated and variation in absorbance noted before and after incubation. In tests for hemolytic activities, the compounds were incubated with red blood cells and variations in absorbance were used as indices their hemolytic activities.Results: The compounds were potent antibacterial agents. Five of them exhibited very good antibacterial potential similar to ciprofloxacin, and had minimum inhibitory concentrations (MIC) of at least 9.00 ± 4.12 μM against S. aureus, E.coli, and B. subtilis. One of the compounds had strong enzyme inhibitory potential against α-glucosidase, with IC50 of 17.11 ± 0.02 μg/mL which was better than that of standard acarbose (IC50 38.25 ± 0.12 μg/mL). Another compound had 1.5 % hemolytic activity. Conclusion: S-Alkylated/aralkylated 2-(1H-indol-3-ylmethyl)-1,3,4-oxadiazole-5-thiol deviratives with valuable antibacterial, anti-enzymatic and hemolytic activities have been successfully synthesized. These compounds may be useful in the development of pharmaceutical products.Keywords: 2-(1H-Indol-3-ylmethyl)-1,3,4-oxadiazole-5-thiol derivatives, Enzyme inhibition, Antibacterial activity, Hemolytic activity, Molecular dockin

Berberine ameliorates the progression of primary sclerosing cholangitis by activating farnesoid X receptor

Primary sclerosing cholangitis (PSC) is a rare cholestatic disease characterized by biliary infiltration, hepatic fibrosis and bile duct destruction. To date, treatment options for PSC are very limited. Therefore, the current study is aimed to investigate the therapeutic potential of berberine (BBR) against PSC. The disease was induced by feeding the mice with 3,5-diethoxycarbonyl-1,4-dihydro-2,4,6-collidine (DDC) for four weeks. The serum biochemistry and liver histology were analyzed. Furthermore, the expression of farnesoid X receptor (FXR) was also evaluated by real-time PCR. The results indicated that berberine prevents the progression of PSC by modulating the expression of FXR which ultimately regulates other genes (including Cyp7A1 and BSEP) thus maintaining bile acids homeostasis. Furthermore, the docking analysis showed that berberine interacts with the binding pocket of FXR to activate the protein thus acting as an FXR agonist. In conclusion, data indicate that berberine protects the liver from PSC-related injury. This effect might be due to the modulation of FXR activity

Impregnation on activated carbon for removal of chemical warfare agents (CWAs) and radioactive content

Nuclear, biological, and chemical warfare (NBC) agents cause an inevitable threat to defense forces and civilians. Exposure to these toxic agents causes a lot of damage to lives. One can avoid the damage of these toxic agents by taking appropriate preventive measures. Respiratory protection is obviously necessary when military personnel or civilians get bounded by such type of noxious situation as contaminant-free air is then required for breathing and it can only be provided by means of a proper gas mask and relevant canister. In purification of contaminated atmospheres, activated carbon has so far met with outstanding success. It removes toxic chemicals either by chemical or physical adsorption from the contaminated air. When any toxic chemicals get adsorbed on the modified impregnated carbon's surface, they usually adsorb there by means of chemical reactions. Destruction of adsorbed toxic substances is expected by such a reactive carbon. In this perspective, an attempt has been made to review the literature from past decades on the removal of toxic chemical warfare agents (CWAs) and radioactive content from air stream in case of any nuclear, biological, and chemical attack by selectively modifying or impregnating the activated carbon surface. This review also covers some important adsorption properties of materials being used in gas mask filters for effective removal of chemicals from airstream. The probable removal mechanisms of various chemical warfare agents and radioactive content have also been reviewed

Co-Existence of hypertension worsens post-exercise cardiac autonomic recovery in type 2 diabetes

Background: Cardiac autonomic neuropathy (CAN) is a commonly overlooked complication of Type 2 Diabetes Mellitus (T2DM) characterized by imbalance between sympathetic and parasympathetic supply to the heart. The susceptibility of heart to dysrhythmias and fatal events increases during and after exercise due to a shift in autonomic regulation. Diabetes and hypertension (HTN) frequently occur concurrently and both conditions lead to impaired cardiac autonomic control. However, their impact together on post-exercise autonomic recovery remains to be explored. Objective: The objective of the study was to investigate the effect of co-existence of HTN on cardiac autonomic recovery (assessed by heart rate recovery and heart rate variability) in patients with T2DM. Methods: Forty eight type 2 diabetic patients (24 normotensive, 24 hypertensive), 24 non-diabetic patients with essential HTN, and 27 healthy controls, were recruited into the study and assessed for heart rate recovery (HRR) following a graded maximal test. Also, heart rate variability (HRV) was recorded before and following the bout of maximal exercise. Results: Heart rate recovery at 1 (HRR1min) and 2 (HRR2min) minute(s) showed significant effects for DM (p < 0.001) and HTN (p < 0.001), while DM × HTN interaction was found to be non-significant. Resting HRV showed a significant decline in time-domain variables for the DM group (p < 0.01). Recovery of HRV showed a significant effect of time (p < 0.05) for all indices, the group effect was found significant only for time-domain measures (p < 0.05). Conclusion: Both HRR and HRV recovery were impaired in DM and HTN. Moreover, the co-existence of HTN had a synergistic effect, causing further worsening of autonomic recovery in T2DM. Keywords: Heart rate recovery, Heart rate variability, Autonomic function, Cardiac autonomic dysfunctio

Phytochemical Screening and Biological Studies of Shilajit (Asphaltum)

Shilajit (asphaltum)  is produced  by the long term humification  of dead plant material  and organic vegetable matter  by different micro-organisms and has great potential for the treatment of a variety of human conditions.  This treatise reviews its origin, sources, chemical composition, biological  and  commercial importance. Phytochemical analysis was done by standard methods to evaluate  different Shilajit (asphaltum) classes of compounds in different samples of shilajit  which are responsible for their  biological activity.  Shilajit`s anti-microbial activity has been evaluated  against four different bacterial strains viz., Escherichia coli, Psuedomonas aeuroginosa, Klebisella pneumonia and Staphylococcus aureus. Phytochemical analysis illustrated  that shilajit contains  terpenoids, cardiac glycosides, saponins and reducing sugars. Surprisingly,  some classes of compounds are absent in shilajit  viz., alkaloids, flavonoids, tannins and anthraquinones. . Shilajit showed no response towards halophytic bacteria and  negligible activity was shown towards other strains of bacteria. Since   anti-microbial activity is based on environmental factors  its activity varied  between locations

Effect of foliar application of Fe and banana peel waste biochar on growth, chlorophyll content and accessory pigments synthesis in spinach under chromium (IV) toxicity

Chromium (Cr) toxicity is becoming one of a major issue for the cultivation of crops. Toxicity of Cr directly affects synthesis of chlorophyll and restricts Fe intake, which decreases crop growth. It is well documented that the reduction of Cr toxicity through the application of biochar. However, current experiment was carried out to investigate any positive effect of, banana peel waste biochar (BC) and foliar application of Fe (FFe) on growth and chlorophyll content of Spinacia oleracea L. under different levels of Cr toxicity. Seeds of Spinacia oleracea L. were grown under three levels of Cr i.e. control (Cr0), Cr35 (35 mg Cr kg−1 soil) and Cr70 (70 mg Cr kg-1 soil). Analyzed data confirmed that Spinacia oleracea L. seeds grown in 1% BC amended soils and 1000mM FFe, showed significantly better growth, Fe uptake and chlorophyll content as compared to control at Cr35 and Cr70. A significant improvement in shoot length (16.9 and 26.9%), root length (16.3 and 20.9%), plant fresh (15.5 and 28.3%) and dry weight (70.3 and 77.8%) as compared to control under Cr35 and Cr70, respectively, validated the efficacious functioning of 1% BC and FFe to mitigate Cr toxicity in Spinacia oleracea L. It is concluded that both 1% banana peel waste BC and 1000mM FFe have potential but sole application of FFe is more effective to alleviate Cr toxicity in Spinacia oleracea L. Fortification of Fe by foliar application is more effective comparative to banana peel waste biochar for improvement in growth, chlorophyll content and accessory pigments synthesis in spinach under chromium (IV) toxicity