Chemical and Fatty Acid Compositions of Crude and Purified Extracts Obtained from Datura innoxia Seeds Extracted with Different Solvents.

Oils play a key role as raw materials in a variety of industries. The aim of this study was to evaluate the potential of Datura innoxia seed oil cultivated in Saudi Arabia for industrial purpose and to study the effects of hexane, chloroform, and isopropanol as extraction solvents on the compositions of the extracts. The results showed that the hexane and chloroform extracts were mainly neutral oils which were rich in linoleic (≈46%) and oleic (≈31%) acids. However, the isopropanol extract contained large amount of neutral oil and organic acids. Neutral oil contained mainly palmitic acid (40.2%) and some important and valuable epoxy (15.4%) and cyclopropane (13.2%) fatty acids. Analysis of the sterol and tocopherol levels of the crude and purified oil extracted revealed that they were significantly affected by the extraction solvent used.

Improving Vesicular Integrity and Antioxidant Activity of Novel Mixed Soy Lecithin-Based Liposomes Containing Squalene and Their Stability against UV Light.

In order to improve the membrane lipophilicity and the affinity towards the environment of lipid bilayers, squalene (SQ) could be conjugated to phospholipids in the formation of liposomes. The effect of membrane composition and concentrations on the degradation of liposomes prepared via the extrusion method was investigated. Liposomes were prepared using a mixture of SQ, cholesterol (CH) and Tween80 (TW80). Based on the optimal conditions, liposome batches were prepared in the absence and presence of SQ. Their physicochemical and stability behavior were evaluated as a function of liposome constituent. From the optimization study, the liposomal formulation containing 5% (w/w) mixed soy lecithin (ML), 0.5% (w/w) SQ, 0.3% (w/w) CH and 0.75% (w/w) TW80 had optimal physicochemical properties and displayed a unilamellar structure. Liposome prepared using the optimal formulation had a low particle size (158.31 ± 2.96 nm) and acceptable %increase in the particle size (15.09% ± 3.76%) and %trolox equivalent antioxidant capacity (%TEAC) loss (35.69% ± 0.72%) against UV light treatment (280-320 nm) for 6 h. The interesting outcome of this research was the association of naturally occurring substance SQ for size reduction without the extra input of energy or mechanical procedures, and improvement of vesicle stability and antioxidant activity of ML-based liposome. This study also demonstrated that the presence of SQ in the membrane might increase the acyl chain dynamics and decrease the viscosity of the dispersion, thereby limiting long-term stability of the liposome.

Optimization of antibacterial activity of ethanolic extracts of Eucalyptus tereticornis and Nigella sativa: Response surface Methodology.

The screening of plants for medicinal purposes represents an effort to discover newer, safer, and possibly more effective drugs. Design of the present study was made aiming to the optimization of the antibacterial activity of ethanolic extracts of Eucalyptus tereticornis (leaves) and Nigella sativa (seeds) against bacteria belongings to both Gram-positive (Bacillus subtilis and Staphylococcus aureus) and Gram-negative (Escherichia coli) spectrum by using response surface methodology. 20 g powder of each E. tereticornis (leaf) and N. sativa (seeds) were mixed with 200ml of ethanol at room temperature, and then it was centrifuged at 4000 rpm for 10 min to separate the supernatants, and allowed to dry in order to obtain ethanol free extracts. A fresh bacterial culture of 100µl of test microorganism was inoculated onto media and spread homogeneously. The antimicrobial activity of ethanolic extracts showed that all the concentrations tested were effective against the test microorganisms. The diameters of zones of inhibition exhibited by S. aureus PCSIR-83 were in the range of 0-28mm, E. coli PCSIR-102 (0-28mm) and B. subtilis PCSIR-05 (15-26mm). The combination of N. sativa (15mg/µl) and E. tereticornis (20mg/µl) were found most effective at pH 9.0 and temperature 35°C. Our results clearly indicate that Gram positive bacteria showed more sensitivity than Gram-negative bacteria.

The Physiological and Ergogenic Effects of Khat (Catha edulis Forsk) Extract.

BACKGROUND: Khat (Catha edulis Forsk) is a natural psychoactive substance which contains two main addictive substances; Cathine and Cathinone. Khat is widely used in east Africa and southern Arabian Peninsula. Khat chewers believe that it improves work capacity and increases energy level and alertness. That is why we aimed in this study to investigate the physiological and ergogenic effects of khat extract. METHODS: This study is an experimental study conducted at the Substance Abuse Research Centre in Jazan University, Saudi Arabia. Thirty healthy young volunteers were randomly assigned into two experimental groups. The first group ingested 45 g of grounded khat leaves extract mixed with juice in the first session then placebo (juice only) in the second session. While the second group ingested the placebo in the first session and the grounded khat leaves with juice in the second session. Experiments were done between December 2012 and March 2013. We recorded the blood pressure, heart rate, grip strength, and reaction time every 15 min for 75 min after each ingestion. The study proposal was reviewed and approved by Research Ethics Committee (REC) of the Medical Research Centre in Jazan University. RESULTS: The results showed the consumption of 45 g of grounded khat leaves contributed to the increase in blood pressure (SBP & DBP) and reaction time (p < 0.05); but had no significant effect on heart rate and grip strength (p > 0.05). CONCLUSIONS: The findings of this study showed that Khat has an acute effect on some physiological parameters. These findings support the prohibition of cathinone and cathine by the World Anti-Doping Agency (WADA, 2016).

The physiological and perceptual effects of plant extracts (Catha Edulis Forsk) during sustained exercise.

BACKGROUND: Khat (Catha Edulis Forsk) is a natural psychoactive substance that contains addictive substances such as Cathine and Cathinone which have similar structure and action to amphetamine. This substance has been suggested that it can decrease perceived exertion and thus improve performance. There is no study in the literature regarding the effect of khat on exercise performance. Therefore, the aim of this study is to find out whether khat leaves can decrease perceived exertion in humans. METHODS: This study is an experimental crossover study conducted at the Substance Abuse Research Centre in Jazan University, Saudi Arabia. Twenty one healthy volunteers were randomly assigned into two experiment trials. Each volunteer visited the lab three times. The first visit was a familiarization session about the nature of the study and the equipment. On the second visit, 45 min before the experiment volunteers ingested either 33 ml of fruit juice (placebo) or the juice mixed with 45 g of ground khat leaves. Then the participants were instructed to perform a 10 Km cycling on an ergometer and recorded the following physiological variables repeatedly on every 5 min of cycling: heart rate, time to complete 10 km cycling, tympanic temperature, and perceived exertion rate. On the third visit a crossover trial was conducted one week after the second visit; then the same cycling test was performed and the same variables were recorded as the second visit. The experimental protocol was reviewed and approved by Research Ethical Committee of the Medical Research Centre, Jazan University. RESULTS: According to study results, khat dramatically decreased time taken to complete a 10 km cycling time trail (p < 0.05), and significantly increased heart rate (p < 0.05) and tympanic temperature (p < 0.01). However, khat did not reduce participant's perceived exertion during the physical trial. The Bonferrini simultaneous confidence intervals using multivariate Hotelling's T(2) was performed to test the significance of the mean vectors for the placebo group and the Khat group and found that groups are statistically significant. CONCLUSIONS: Khat showed a clear enhancing effect on physical performance. The most parsimonious explanation for this effect is that, like the related amphetamines, cathine/cathinone act as stimulants to increase the capacity to perform exercise. Thus, khat produces the same effects which lead to the banning of amphetamine. These findings conform & endorse the recent prohibition of cathinone by the World Anti-Doping Agency (WADA, 2014).

Role of oral glutamine in alleviation and prevention of radiation-induced oral mucositis: A prospective randomized study.

BACKGROUND: Oral mucositis is the most frequently occurring painful and dose-limiting side-effect of radiation of the head and neck region. Few studies demonstrated that oral glutamine suspension may significantly reduce the duration and severity of objective oral mucositis during radiotherapy. MATERIALS AND METHODS: A randomized, prospective single institutional case control study was performed between April 2012 and November 2012 comparing the influence of oral glutamine on radiation induced mucositis in head and neck malignancy patients. Seventy biopsy proven patients with head and neck cancer receiving primary or adjuvant radiation therapy were randomized to receive either oral glutamine suspension daily 2h before radiation in the study arm (10 g in 1000 ml of water) (n = 35) or nothing before radiation; control arm (n = 35). RESULTS AND ANALYSIS: Total 32 patients (91.43%) in the glutamine arm and total 34 patients (97.15%) developed mucositis. Grade 3 mucositis (14.29%) and grade 4 mucositis (2.86%) in the study arm (who received oral glutamine) were significantly less (P = 0.02 and P = 0.04, respectively) in the glutamine arm. The mean duration of grade 3 or worse mucositis (grade 3 and grade 4) was significantly less (6.6 days vs. 9.2 days) in study arm with P < 0.001. Mean time of onset of mucositis was significantly delayed in patients who took glutamine in comparison to control arm with P < 0.001. CONCLUSION: Glutamine delays oral mucositis in the head neck cancer patients. Moreover, it reduces the frequency and duration of grade 3 and grade 4 mucositis.

An in vitro screening to identify drug-resistant mutations for target-directed chemotherapeutic agents.

The discovery of oncogenes and tumor suppressors as a driver of cancer development has triggered the development of target-specific small molecule anticancer compounds. As exemplified by Imatinib (Gleevec), a specific inhibitor of the Chronic Myeloid Leukemia-associated BCR/ABL kinase, these agents promise impressive activity in clinical trials, with low levels of clinical toxicity. However, such therapy is susceptible to the emergence of drug resistance mainly due to amino acid substitutions in the target protein. Defining the spectrum of such mutations is important for patient monitoring and the design of next-generation inhibitors. Using Imatinib and BCR/ABL as a paradigm for a drug-target pair, we reported a retroviral vector-based screening strategy to identify the spectrum of resistance-conferring mutations, which has helped in designing the next-generation BCR/ABL inhibitors such as Nilotinib, Dasatinib, and Ponatinib. Here we provide a detailed methodology for the screen, which can be generally applied to any drug-target pair.

Cloning and characterization of the 5'-flanking region of the oxalate decarboxylase gene from Flammulina velutipes.

The oxalate-degrading enzyme, oxalate decarboxylase (OXDC), was purified and characterized from Flammulina velutipes, a basidiomycetous fungus [Mehta and Datta (1991) J. Biol. Chem. 266, 23548-23553]. The cDNA cloning and analyses revealed that OXDC transcription was induced by oxalic acid. However, in this report, we show that OXDC transcription is induced by low pH, not by oxalate. To understand the regulatory mechanism of OXDC expression, we have cloned and analysed a 580-bp genomic fragment from the 5'-flanking region of the OXDC gene. Sequence analysis showed the presence of several eukaryotic transcription factor binding motifs within the -580 bp of the upstream region. Electrophoretic-mobility-shift assays with partially purified cell extracts revealed specific binding of a factor in acid-induced, but not in uninduced, extracts. Furthermore, DNase I protection assays using the partially purified fraction from oxalic acid-induced extract revealed a footprint of a 13-bp sequence 5'GCGGGGTCGCCGA3', termed low pH responsive element (LPRE), corresponding to the -287 to -275 bp region of the OXDC promoter. Our results suggest that in F. velutipes cells, activation of OXDC transcription in response to low pH is mediated by the binding of a novel transcription factor through the LPRE site in the OXDC promoter.