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The aim of this study was to develop the ranostic nanocomposite by conjugating quantum dots with functional, therapeutic and targeting moieties. The quantum dots nanoparticles were used to diagnose and deliver antitumor drugs in a controlled manner to cancerous cells by fusing with tumor cell surfaces. To enhance the attachment of the nano-composite to specific tumor cells without harming neighboring normal cells, folic acid was conjugated with the nano-composite as folate receptors are over expressed in different kinds of tumors. The study was conducted for one year at the University of Punjab. The quantum dots were synthesized by a hydrothermal process using cadmium acetate and sodium sulfide. The response was evaluated on breast tumor samples for binding and nano-composite delivery under a fluorescent microscope. Fourier-transform infrared analysis was performed to confirm CdS conjugation with cysteine, folic acid and curcumin. The results showed that the quantum dot conjugate provides a two-way attack on cancer cells and causes increased cellular apoptosis. Further testing on murine animal models is required to confirm the results of this research study. [ABSTRACT FROM AUTHOR]

Muesli and cereal based breakfast contain generous amounts of fiber that are helpful in the management of blood glucose levels. Muesli contains ß-glucans that ensure gradual rise in blood glucose levels. Muesli also limits the absorption of glucose by making it unavailable. This study explored the effect of muesli in the management of postprandial blood glucose levels. 15 healthy and 15 diabetic females were offered muesli meal after 8h fasting. Fasting blood glucose levels and blood glucose level 30 and 60 minutes after meal were measured. Results of study showed that muesli brought a gradual rise in blood sugar level. Healthy females showed fasting sugar (92.17±11.27), after 30 minutes (110.87±13.85) and after 60 minutes (114.25±15.67) while diabetic females showed fasting sugar (113.25±10.87), after 30 minutes (117.83±18.74) and after 60 minutes (118.26±17.85). The nutritional profile of muesli showed that it contained 202 kcal of energy, 32.7g of carbohydrates, 9g of fiber, 12.4g of protein and 2.5g of fats. It also contained 5.1g of ß-glucans. Muesli found to be effective in the management of postprandial blood glucose levels in healthy and diabetic populations. [ABSTRACT FROM AUTHOR]

Citrus sinensis is an important member of the genus Citrus which contains phenolic compounds and bioflavonoids which have antihyperlipidemic and antiatherogenic effects. It also has the potential to reduce oxidative stress. To investigate the antihyperlipidemic effect of orange peel powder was encapsulated and analyzed in hyperlipidemic patients. Results showed that it contains moisture (12.2%), ash content (7.9%), crude fat (0.78%), crude protein (12.37%) and crude fiber (13.2%). Total phenolic content and total flavonoid content were observed as 163.17 mg and 17.23mg in quercetin equivalent per gram a dry weight basis. Furthermore, the Orange peel powder was given in the form of medicinal capsules to hyperlipidemia male subjects. The experimental groups (G1 and G2) were given orange peel powder in capsules 400mg/d to the G1 group and 800mg/d to the G2 group for the time of 45 days. The serum lipid profile of patients was measured before and after the experimental trial. The result showed that G1 and G2 showed a decrease in plasma lipid parameters and increased high-density lipoprotein content in blood substantially as compared to G0. Thus, it was concluded from the results that orange peel powder depicts a significant impact on treating hyperlipidemia. [ABSTRACT FROM AUTHOR]

Diabetes mellitus (DM) is a metabolic disorder characterized by frequent urination, hunger and high blood sugar level. α-glucosidase inhibitors are considered as a frontline treatment for the DM. This research article deals with the identification of benzothiazine derivatives as α-glucosidase inhibitors through in-silico techniques and then the confirmation through in-vitro analysis. Molecular docking studies were carried out to find out the binding interactions of targeted molecules with receptor molecule i.e., α-glucosidase enzyme. The synthetic compounds 1 (a-n), 2 (a-d) and 3 (ab) were evaluated for in-vitro alpha glucosidase inhibitory activities that resulted in the discovery of various potent molecules. Majority of the compounds (1c, 1f, 1g, 1k-n, 2a-d and 3a-b) exhibited good inhibitory activity against α-glucosidase. Compounds 1c, 1g, 1k and 1m appeared as the potent active compounds with the IC50 values 17.44, 27.64, 24.43, 42.59 and 16.90 µM respectively. Compounds 1c & 2c were found almost 3-folds more active than the standard acarbose. The study may lead to discover potent drug candidates with less complication for the treatment of the type II diabetes mellitus. [ABSTRACT FROM AUTHOR]

The facile and efficient protocol for the synthesis of N-phenyl piperazine based di-thio-carbamates has been reported under neat conditions. A library of novel piperazine based di-thio-carbamates (3a-h) in excellent yields has been prepared. Solvent free, catalyst free and easy work up conditions make this protocol an attractive synthetic protocol to achieve novel biologically active di-thio-carbamates. The synthesized molecules have been characterized by FT-IR, 1HNMR and 13CNMR spectroscopic techniques. The pharmacological aspects of these derivatives have been evaluated via hemolysis and thrombolysis. All the target molecules (3a-h) exhibit mild to medium potential as hemolytic and thrombolytic agents. Among the synthesized derivatives, compound 3c showed least cytotoxicity and better thrombolytic potential. [ABSTRACT FROM AUTHOR]

Fluoroquinolones are targets of interest due to their broad spectrum antibacterial activity. Structure-activity relationship (SAR) of fluoroquinolones clearly indicates that substitution at C-7 position enhances the lipophilicity of these scaffolds resultantly affording pharmacologically significant compounds. Therefore, various ciprofloxacinoxadiazole hybrids were synthesized and characterized by spectral analysis. Cytotoxic activity of these derivatives was assessed using human liver tumor cells (Huh7). One dose anticancer test results revealed moderate cytotoxicity of the newly synthesized compounds against this cell line. As the only compound 4a depicted comparatively lower cell viability value (81.91% using 100μg/mL concentration) than the other compounds. [ABSTRACT FROM AUTHOR]

A series of new derivatives of 4-(2-chloroethyl)morpholine hydrochloride (5) were efficiently synthesized. Briefly, different aromatic organic acids (1a-f) were refluxed to acquire respective esters (2a-f) using conc. H2SO4 as catalyst. The esters were subjected to nucleophillic substitution by monohydrated hydrazine to acquire hydrazides (3a-f). The hydrazides were cyclized with CS2 in the presence of KOH to yield corresponding oxadiazoles (4a-f). Finally, the derivatives, 6a-f, were prepared by reacting oxadiazoles (4a-f) with 5 using NaH as activator. Structures of all the derivatives were elucidated through 1D-NMR EI-MS and IR spectral data. All these molecules were subjected to antibacterial and hemolytic activities and showed good antibacterial and hemolytic potential relative to the reference standards. [ABSTRACT FROM AUTHOR]

Sixteen derivatives of dithiin diisoimide 2a-2p have been synthesized and screened for antibacterial and antifungal activity. Compounds 2a-2g and 2i-2p are almost same or more active than gentamicine against Acinetobacter. Whereby compound 2,6-didodecyl-1H,5H-pyrrolo[3',4',5,6][1,4]dithiino[2,3-c]pyrrole-1,3,5,7(2H,6H)-tetrone (2d) having zone of inhibition 20 mm against Acinetobacter is the most potent among all these compounds and can be used as lead compound for the treatment of Acinetobacter infection. [ABSTRACT FROM AUTHOR]

Malaria and typhoid fever are among the major infectious diseases which impose significant health and socioeconomic burden on affected populations. Further, co-infection and resembling symptomatology in both infections, mostly leads to misdiagnosis and mistreatment. So co-infection of malaria and typhoid fever is becoming a major issue in tropical and subtropical countries. The current study was planned to explore the rate of co-infection of malaria and typhoid fever to show the diagnostic challenges and people health implications in the local population of Faisalabad- Pakistan. For this purpose, 144 samples (n=144) were collected from suspected subjects both male (n=74) and female (n=70) (comprises of three age group ranges viz >01-10, 11-20 and above 20 years old) of typhoid fever and malaria from October to December 2017 at Children Hospital, Faisalabad-Pakistan. Thick smear as a gold standard technique for malaria diagnosis and Widal agglutination technique for typhoid diagnosis were used. Results revealed that the prevalence of co-infection in selected subjects was 6.3% (n=9) with higher prevalence in female subjects (7.1%) as compared to males (5.4%). Further, it was also reported that age groups >01-10 years old, 11-20 years old and 21-above years old have6.6 % (n=75), 5.7 % (n=35) and 5.8% (n=34), coinfection prevalence respectively. In the present study, it could be concluded that although the prevalence of co-infection of malaria and typhoid fever in the studied population was possible but sensitivity of diagnostic tools was limited, so more reliable, specific and sensitive diagnostic tools are required to report confidently more precise correlation of these infectious diseases. [ABSTRACT FROM AUTHOR]

In the present study previously isolated Weissella cibaria CMG DEX3 capable of producing high molecular weight, water soluble dextran (Ahmed et al., 2012) is characterized for most efficient less expensive carbon, nitrogen sources, micro and macro nutrients by utilizing a multifactorial Placket-Burman statistical design for optimization of dextran production. A twelve run Plackett-Burman experimental model with slight modification was utilized to evaluate the impact of ten diverse nutrients on the production of dextran by the bacterial isolate Weissella cibaria CMG DEX3. [ABSTRACT FROM AUTHOR]

A number of novel 5-substituted-2-((6-bromo-3,4-methylenedioxybenzyl)thio)-1,3,4-Oxadiazole derivatives (6a-l) have been synthesized to evaluate their antibacterial activity. Using aryl/aralkyl carboxylic acids (1a-l) as precursors, 5-substituted-1,3,4-Oxadiazol-2-thiols (4a-l) were yielded in good amounts. The derivatives, 4a-l, were subjected to electrophilic substitution reaction on stirring with 6-bromo-3,4-methylenedioxybenzyl chloride (5) in DMF to synthesize the required compounds. All the synthesized molecules were well characterized by IR, 1H-NMR, 13C-NMR and EIMS spectral data and evaluated for antibacterial activity against some bacterial strains of Gram-bacteria. The molecule, 6d, demonstrated the best activity among all the synthesized molecules exhibiting weak to moderate inhibition potential. [ABSTRACT FROM AUTHOR]

Diabetes is a condition where the fasting blood glucose level elevated above the normal range (80-120mg/dL). This increase in blood glucose level may be due to the insulin deficiency i.e. insulin dependent diabetes mellitus (IDDM or type I) or due to insulin resistance i.e. non-insulin dependent diabetes mellitus (NIDDM or type II). Diabetes leads to severe complications in the body even life treating complications e.g. nephropathy, retinopathy, neuropathy increased vascular permeability and delayed wound healing if left untreated. Different drugs are used for the treatment of diabetes mellitus, but synthetic drugs are costly and possess severe side effects. So, more emphasis is being placed on the use of traditional medicines because these sources have fewer side effects than the synthetics drugs and are economical. So the white skinned sweet potato (Ipomoea batatas L.) peel-off was selected for its anti-diabetic effect as well as to see its effects on biochemical parameters. Both young (3-4 months) and old (up to 1 year) Wistar rats were selected for current study. It was found that the aqueous extract of WSSP peel-off had shown beneficial effects. In addition to the decrease in blood glucose level it also decreased protein glycation level total cholesterol, triglycerides, and LDL-cholesterol. Increase in HDL-cholesterol was also observed after treating the rats with aqueous extract of Ipomoea batatas. Additionally, WSSP peel-off had also shown positive results on total protein concentration, albumin, globulin, and plasma enzymes (SGOT and SGPT). Further research would be needed in order to purify the anti-diabetic components and it should be available in compact dose form for all diabetic patients. [ABSTRACT FROM AUTHOR]

To check the nutritional and mineral contents of four medicinal plants viz., Peganum hermla, Solanum nigrum, Mentha longifolia, Achryanthus aspera, which are used as medicine traditionally in Soon Valley Khushab, Pakistan. Proximate analysis of plant sample determined that protein (7.491%) and ash (22.79%) was highest in Mentha longifolia, carbohydrate (75.23%) in Peganum hermla, fats (12.595%) and moisture (6.82%) was highest in Achryanthus aspera. In comparative assessment of the various species, the results showed that Achryanthus aspera. is the most significant species having higher concentrations of fat, fibre values compared to the other species. Absorption Spectrometric method was used for the elemental analysis of essential elements such as Fe, Cd, Cu,Mn, Pb, Cr, Ni and Na in medicinal plants in different range. [ABSTRACT FROM AUTHOR]

We report the synthesis, characterization, biological evaluation and quantitative structure-activity relationship of some Schiff base esters as promising new antitumor, antioxidant and anti-inflammatory agents. The Schiff base esters were synthesized by two synthetic routes using variably substituted hydroxy benzaldehydes with para amino phenol in appreciable yields. All the newly synthesized esters have been characterized by ¹H-NMR, 13C-NMR, FT-IR techniques and elemental analysis. The synthesized esters were examined for antioxidant, antitumor and anti-inflammatory potentials through different bioassays and quantitative structure-activity relationship was studied. Bioassays showed encouraging results and indicated that some of these title compounds may have potential for further pharmacological investigations. [ABSTRACT FROM AUTHOR]

Hydrazones of theophylline-7-acetic acid 5a-g have been synthesized using ultrasonic irradiation as well as conventional heating system and analyzed for their anticancer characteristics against human lung cancer cell line (A549). Compound 5g with cell viability 33.19±0.49% (100 μg/μL) compared to the starting reference drug acefylline having cell viability 86.32±11.75% (100 μg/μL) was found to be the most active anticancer agent among all. The synthesized derivatives were also exposed to hemolytic and thrombolytic studies to determine their cytotoxic profile and results revealed their low toxicity and moderate clot lysis activity.

Fluoroquinolones are targets of interest due to their broad spectrum antibacterial activity. Structure-activity relationship (SAR) of fluoroquinolones clearly indicates that substitution at C-7 position enhances the lipophilicity of these scaffolds resultantly affording pharmacologically significant compounds. Therefore, various ciprofloxacin-oxadiazole hybrids were synthesized and characterized by spectral analysis. Cytotoxic activity of these derivatives was assessed using human liver tumor cells (Huh7). One dose anticancer test results revealed moderate cytotoxicity of the newly synthesized compounds against this cell line. As the only compound 4a depicted comparatively lower cell viability value (81.91% using 100μg/mL concentration) than the other compounds.

A series of new derivatives of 4-(2-chloroethyl)morpholine hydrochloride (5) were efficiently synthesized. Briefly, different aromatic organic acids (1a-f) were refluxed to acquire respective esters (2a-f) using conc. H 2 SO 4 as catalyst. The esters were subjected to nucleophillic substitution by monohydrated hydrazine to acquire hydrazides (3a-f). The hydrazides were cyclized with CS2 in the presence of KOH to yield corresponding oxadiazoles (4a-f). Finally, the derivatives, 6a-f, were prepared by reacting oxadiazoles (4a-f) with 5 using NaH as activator. Structures of all the derivatives were elucidated through 1D-NMR EI-MS and IR spectral data. All these molecules were subjected to antibacterial and hemolytic activities and showed good antibacterial and hemolytic potential relative to the reference standards.

Zn, Cu, Co and Ni are biocompatible metals as they are active center of many enzymes in the human body. Incorporation of these biocompatible metals into 3-(o-Sulfamoylphenyl) carbamoylbenzoic acid (I) makes them able to prove an excellent antimicrobial agent. In the present study Ni (II), Co (II), Cu(II) and Zn (II) complexes (III-VI) were synthesized from ligand (I) derive from 3-(o-Sulfamoylphenyl) carbamoylbenzoic acid and zinc, nickel, cobalt acetate tetrahydrate/copper acetate monohydrate. Synthesized complexes (III-VI) were characterized by FT-IR, 1 H NMR and 13 CNMR. III-VI have 81-93% yield while melting points recorded were in the range of 209-239oC. Purity of ligands and their respective complexes was confirmed by TLC. Results of antibacterial properties suggested that III, IV, V and VI were highly active against gram +ve (S. epidermidis, B. subtilis. S. aureus, S. mutans) and gram -ve bacteria (E. coli and P. aruginosa). Comparison was also performed to check whether metal complexes or ligand with its derivative exhibit best result against all tested strains. The anthelmintic activity of the complexes III-VI against tape worm, liver fluke, thread worm, and hook worm using three different concentrations (15, 30, 45mg/mL), significantly (p<0.01) paralyzed the worms followed by death, which was comparable with that of the standard. Overall results indicated that S. epidermidis, S. mutans, E. coli and B. subtilis are very sensitive to complex III & IV and can be used for treatment of bacterial infections whereas Complex-V, could a potent target for anti-parasite therapy.

National diseases burden of Cardiovascular diseases is the top leading cause of death in Pakistan. In this study, Pakistani has been assessed for Atherosclerotic Cardiovascular Disease (ASCVD) on the basis of American Herat Association (AHA) guidelines. The aim of the study is to assess and inform about 10-year risk and life time risk in people residing in the largest metropolis city Karachi and aware about the use of statins as per revised Pooled Cohort Equation guidelines. The study sample size was 1760 with the age of 39 to >80 years with non-atherosclerotic diseases. Both genders without language barrier with or without elevated lipid were included. Clinical investigations including HDL, B.P and serum TG were included for calculating the ten year and life time risks on the basis of <5%, 5-7% and >7.5%. Results shows that the Odd ratio >1 found between age and TC however significant relationship (p<0.05) between gender, diabetes, hypertension and smokers were established. >50% study population required moderate and high intensity statin however <30% needed life style modification for reducing cardiac on risk. It is concluded that current recommendations are not for South Asians and may under or overlook the risks of individuals living in this continent. This study estimates the cardiovascular risk burden in the population of Karachi, Pakistan who were non-atherosclerotic undiagnosed and un-treated. This risk assessment may modify the algorithm and successfully identify the risk burden in present study groups.

A number of novel 5-substituted-2-((6-bromo-3,4-methylenedioxybenzyl)thio)-1,3,4-Oxadiazole derivatives (6a-l) have been synthesized to evaluate their antibacterial activity. Using aryl/aralkyl carboxylic acids (1a-l) as precursors, 5-substituted-1,3,4-Oxadiazol-2-thiols (4a-l) were yielded in good amounts. The derivatives, 4a-l, were subjected to electrophilic substitution reaction on stirring with 6-bromo-3,4-methylenedioxybenzyl chloride (5) in DMF to synthesize the required compounds. All the synthesized molecules were well characterized by IR, 1 H-NMR, 13 C-NMR and EIMS spectral data and evaluated for antibacterial activity against some bacterial strains of Gram-bacteria. The molecule, 6d, demonstrated the best activity among all the synthesized molecules exhibiting weak to moderate inhibition potential.

Lovastatin is a natural competitive inhibitor of 3-hydroxy-3-methyl glutaryl coenzyme-A (HMG-CoA) reductase and inhibits specifically rate limiting step in cholesterol biosynthesis. Further, lovastatin in comparison with synthetic drugs has no well-reported side effects. Four pure isolated filamentous fungal strains including Aspergillus niger IBL, Aspergillus terreus FFCBP-1053, Aspergillus flavus PML and Aspergillus nidulans FFCBP-014 have been cultured by solid state fermentation (SSF) using rice straw as substrate for the synthesis of lovastatin. After selecting Aspergillus terreus FFCBP-1053 as the best producer of lovastatin, various selected physical parameters including pH, temperature, inoculums size and moisture content were optimized through response surface methodology (RSM) under center composite design (CCD) for lovastatin hyper production. Maximum lovastatin production of 2070±91.5 was predicted by the quadratic model in the medium having moisture content 70% and pH 4.5 at 35°C which was verified experimentally to be 2140±93.25µg/g DW of FM (microgram/gram dry weight of fermentation medium), significantly (P<0.05) high as compared to un-optimized conditions while it was noted that lovastatin production is independent on inoculum size (P>0.05) measured by spectrophotometer at 245 nm against standard. It was determined that optimized conditions for the hyper-production of lovastatin from fungal sources have a significant effect.

To check the nutritional and mineral contents of four medicinal plants viz., Peganum hermla, Solanum nigrum, Mentha longifolia, Achryanthus aspera, which are used as medicine traditionally in Soon Valley Khushab, Pakistan. Proximate analysis of plant sample determined that protein (7.491%) and ash (22.79%) was highest in Mentha longifolia, carbohydrate (75.23%) in Peganum hermla, fats (12.595%) and moisture (6.82%) was highest in Achryanthus aspera. In comparative assessment of the various species, the results showed that Achryanthus aspera. is the most significant species having higher concentrations of fat, fibre values compared to the other species. Absorption Spectrometric method was used for the elemental analysis of essential elements such as Fe, Cd, Cu,Mn, Pb, Cr, Ni and Na in medicinal plants in different range.