ABSTRACT
Cancer is a multifactorial disease that can cause morbidity and mortality in humans. An altered gene expression in cancer leads to a change in the overall activity of the human cell. Overexpression of cancer protein may give a piece of wide information about the specific type of tumor. Sphingosine kinase-1 (SK-1) is a metabolic enzyme that is mainly overexpressed in several types of cancer and other inflammatory diseases. Similarly, pyruvate kinase-M2 (PK-M2) is an important oncogenic ATP-producing glycolytic enzyme that is upregulated in most cancer cells. The phytocompound of medicinal plants such as Nigella sativa contains a variety of micronutrients that inhibit the proliferation and activity of tumor cells. In this study, the role of phytocompounds in combating cancer was studied against the model kinase proteins, that is, PK-M2 and SK-1. In silico tool like the PASS-Way2Drug server was used to predict the anticancer properties of phytocompounds. Moreover, the CLC-Pred web server provided the cytotoxicity prediction of chemical compounds against several human cancer cell lines. The pharmacokinetics and toxicity profiles were predicted by the SwissADME and pkCSM software. The binding energies were obtained by molecular docking to confirm the intermolecular interaction of selected phytocompounds with proteins. Consequently, molecular dynamics (MD) simulation confirmed the stability, conformational changes, and dynamic behavior of the kinase proteins complexed with the lead phytocompounds, that is, epicatechin, apigenin, and kaempferol.Communicated by Ramaswamy H. Sarma.
Subject(s)
Neoplasms , Nigella sativa , Phosphotransferases (Alcohol Group Acceptor) , Humans , Early Detection of Cancer , Pyruvate Kinase , Molecular Docking Simulation , Neoplasms/drug therapyABSTRACT
OBJECTIVE: To find out if there is a difference in the efficacy of propolis and seventh-generation dentine bonding agent in reducing dentine hypersensitivity. METHODS: The randomised, single-blind study was conducted at the Department of Periodontology, Dow International Dental College, Dow University of Health Sciences, Karachi, from December 2018 to November 2019, and comprised patients with complaint of dentine hypersensitivity who were divided in group A which received 30% ethanolic extract of propolis, and group B which received dentine bonding agent. Recordings of dentine hypersensitivity were obtained at baseline, before and after the application of experimental agents, and on days 7, 15 and 30. The response was measured using the Schiff Cold Air Sensitivity Scale. Data was analysed using SPSS 20. RESULTS: Of the 52 patients, 19 (36.5%) were males and 33 (63.5%) were females. The overall mean age was 29.9 ± 6.5 years. Majority of the subjects were students i.e. 16 (30.8%) and housewives i.e. 11 (21.2%), while drivers, teachers, businessmen etc. constituted of 25 (48%) subjects. Significant reduction of dentine hypersensitivity was observed in both groups (p<0.05). Intergroup comparison showed non-significant differences (p>0.05). CONCLUSIONS: Propolis and dentine bonding agent had significant effect in reducing dentine hypersensitivity. The difference between the two was not significant.
Subject(s)
Dentin Desensitizing Agents , Dentin Sensitivity , Propolis , Adult , Female , Humans , Male , Young Adult , Dentin , Dentin Sensitivity/drug therapy , Propolis/therapeutic use , Single-Blind MethodABSTRACT
OBJECTIVE: To determine the effect of pre-cooling agent on the intensity of pricking pain at the intraoral injection site in adult patients. METHODS: The in-vivo interventional study was conducted at the Department of Operative Dentistry, Dr. Ishrat-ul-Ebad Khan Institute of Oral Health Sciences, Dow University of Health Sciences, Karachi, from September 2018 to August 2019, and comprised adult patients of either gender. The pricking pain perception during needle administration was assessed using split-mouth technique. Topical anaesthesia benzocaine gel was applied on the left side, which was treated as controls, for 1 min, while on the right side, which was treated as the experimental side, refrigerated cartridge was placed for 2 min. Infiltration anaesthesia was then administered on both sides. Pain perception ratings were measured through visual analogue scale. After profound anaesthesia was achieved, restorative treatment was performed under rubber dam isolation. Data was analysed using SPSS 24. RESULTS: Of the 152 subjects, 77(50.65%) were females and 75(49.34%) were males. The overall mean age was 35.97±8.669 years (range: 21-50 years). The effect of refrigerated cartridge was significant on the intensity of pricking pain at the intraoral injection site in patients aged 41-50 years, and in female patients aged 21-30 years (p<0.05), whereas its effect was non-significant in males aged 21-30 years and patients aged 31-40 years (p>0.05). CONCLUSIONS: Pre-cooling agent was found to be effective in decreasing pricking pain felt by patients.
Subject(s)
Anesthetics, Local , Pain , Adult , Anesthesia, Local , Benzocaine , Female , Humans , Male , Pain/drug therapy , Pain MeasurementABSTRACT
Anthelmintic activity of condensed tannins (CT) was evaluated both in vitro and in vivo. In vitro tests included egg hatch test and paralysis/mortality assay on adult Haemonchus contortus. In vivo anthelmintic effect was determined by faecal egg count reduction test in lambs. To this end, 18 lambs were divided into three groups (low tannin, high tannin and control). The lambs of low and high tannin groups were fed diets containing 2 and 3% CT while the control group was fed on diets without CT. In vitro trials showed a dose-dependent inhibition of nematode egg hatching; whereas, there was no effect of CT on adult H. contortus. In vivo trials indicated reduction in faecal egg counts in lambs fed diets containing CT. Feed intake and nutrient digestibility of CT-fed sheep was lower and nitrogen balance was higher as compared to control. Maximum weight gain was observed in animals fed diets containing 3% CT. The direct anthelmintic effect of CT, therefore, was evidenced by inhibited egg hatching; whereas, faecal egg counts reduction in sheep was through improved nutrient utilization.