Characterisation of microemulsions containing orange oil with water and propylene glycol as hydrophilic components

The current study aims to investigate the effect of incorporation of orange oil, mainly consisting of the cyclic mono-terpene linolene, a known skin penetration enhancer, as oil component on microemulsion formation both in water and propylene glycol containing systems. Phase diagrams of pseudoternary mixtures containing orange oil, ethyloleate or a 1:1 mixture (w/w) of orange oil and ethyloleate as oil components, a 6:4 (w/w) mixture of polyoxyethylene 20 sorbitan monooleate and sorbitan monolaurate as surfactant components and water or propylene glycol as hydrophilic components were investigated. Smaller microemulsion regions were observed when orange oil was used as a substitute for ethyloleate in both water and propylene glycol containing systems. Polarising light microscopy, viscosity measurements, electrical conductivity measurements and cryo-field emission scanning electron microscopy were used to identify structural features of the microemulsions. Solution-type, w/o droplet-type microemulsions and microemulsion areas containing liquid crystals were found in varying areas in the phase diagrams of water containing systems. Liquid crystals formation occurs when the water concentration reaches 20%-22.5% (w/w). Only solution-type microemulsions were observed in propylene glycol containing systems. The dimension of solution-type microemulsion areas in the phase diagrams is likely to depend on the miscibility of components and larger microemulsion areas were found when ethyloleate was used instead of orange oil and propylene glycol was used instead of water. W/o droplet-type microemulsions of systems containing orange oil and ethyloleate as oil components appear in different areas of the phase diagrams. Incorporation of orange oil as a penetration enhancer into a topical microemulsion affects its physical characteristics. This in turn may lead to instability of the microemulsion and/or can influence the release patterns of drugs from these microemulsions when applied as topical formulations.     

Comparison of chemical profiles,antioxidation, inhibition of skin extracellular matrix degradation,and anti-tyrosinase activity between mycelium and fruiting body of Cordyceps militaris and Isaria tenuipes

ContextCordyceps militaris and Isaria tenuipes (Cordycipitaceae) are high-value fungi that are used for health-promoting food supplements. Since laboratory cultivation has begun for these fungi, increased output has been achieved.ObjectiveThis study compared the chemical profiles, antioxidant, anti-tyrosinase, and skin extracellular matrix degradation inhibition between mycelium and fruiting body of C. militaris and I. tenuipes.Materials and methodsThe antioxidative potential of 10% v/v aqueous infused extract from each fungus was separately investigated using 2,2-azinobis(3-ethylbenzo-thiazoline-6-sulphonic acid) (ABTS), 1,1-diphenyl-2-picrylhydrazyl (DPPH), ferric reducing antioxidant ability, and ferric thiocyanate methods. The inhibition against MMP-1, elastase, and hyaluronidase were determined to reveal their anti-wrinkle potential. Anti-tyrosinase activities were determined.ResultsC. militaris and I. tenuipes extracts were found to contain a wide range of bioactive compounds, including phenolics, flavonoids, and adenosine. A correlation was discovered between the chemical compositions and their biological activities. The extract from I. tenuipes fruiting body (IF) was highlighted as an extraordinary elastase inhibitor (IC₅₀ = 0.006 ± 0.004 mg/mL), hyaluronidase inhibitor (IC₅₀: 30.3 ± 3.2 mg/mL), and antioxidant via radical scavenging (ABTS IC₅₀: 0.22 ± 0.02 mg/mL; DPPH IC₅₀: 0.05 ± 0.02 mg/mL), thereby reducing ability (EC₁: 95.3 ± 4.8 mM FeSO₄/g extract) and lipid peroxidation prevention (IC₅₀: 0.40 ± 0.11 mg/mL). IF had a three-times higher EC₁ value than ascorbic acid and significantly higher elastase inhibition than epigallocatechin gallate.Discussion and conclusionsIF is proposed as a powerful natural extract with antioxidant and anti-wrinkle properties; therefore, it is suggested for further use in pharmaceutical, cosmeceutical, and nutraceutical industries.     

Prevalence of High Grade Squamous Intraepithelial Lesion (HSIL) and Invasive Cervical Cancer in Patients with Low Grade Squamous Intraepithelial Lesion (LSIL) at Cervical Pap Smear

Objective: To assess the prevalence and factors associated with a histologic diagnosis of high grade squamous intraepithelial lesion (HSIL) and invasive cervical cancer in patients with low grade squamous intraepithelial lesion (LSIL) cervical pap smear findings. Methods: Medical records (including cytology reports, colposcopic impression, and pathologic results from cervical biopsy, endocervical curetting, cervical conization or hysterectomy) of 226 women with LSIL from conventional cervical pap smears during January 2001 to December 2005, who subsequently underwent colposcopic evaluation at our institution, were reviewed. Results: Mean age of the patients was 39.0 years. The incidences of LSIL, HSIL, microinvasive cervical cancer were 58.8%, 15.0%, 1.3% respectively. No associations were found between age, parity, contraception, anti-HIV or menstrual status and the detection of HSIL/invasive cervical cancer. Conclusion: Approximately 16.3 % of LSIL pap smear cases turn out to be HSIL or invasive cervical cancer from histologic diagnosis.     

Synchronous and metachronous malignancy in endometrial cancer patients treated in a tertiary care center of Thailand

Objective

To evaluate the prevalence and features of non-endometrial cancers in Thai endometrial cancer (EC) patients.

Methods

EC patients treated in our institution were identified and the following data were collected: age, EC stage, histopathology, adjuvant therapy, other cancers, living status, and cause of death.

Results

The mean age of the 344 patients was 56.8±10.8 years. Fifty (14.5%) had other synchronous and metachronous cancers. Mean ages of the patients with or without other cancers were not significantly different, 55.7±10.04 years versus 57.1±11.0 years, respectively (p=0.358). History of any cancer in the family and tumor in the lower uterine segment were more frequent among the patients with other cancers (6.0% vs. 1.7%, p=0.095; 12.0% vs. 1.0%, p<0.001; respectively). Six patients had ≥2 other cancers. Ovarian, breast, and colon were the three most common other cancers. After a median follow-up of 57.1 months, 18.3% of patients had died: 30.0% of patients with other cancers and 16.3% of those without other cancers. The corresponding EC deaths were 14.0% and 11.2%. The 5-year overall survival was significantly lower in patients who had other cancers: 79.3% (95% confidence interval [CI], 68.3 to 90.3) vs. 86.0% (95% CI, 81.7 to 90.3) than in those without (p=0.023). However, the corresponding disease-specific survival was not significantly different: 85.1% (95% CI, 75.5 to 94.7) compared with 89.0% (95% CI, 85.1 to 92.9), respectively (p=0.514).

Conclusion

Thai EC patients had a high incidence of other cancers. Overall survival of EC patients who had other cancers was worse than those without, while disease-specific survival was not significantly different.     

Insight into the molecular mechanism of P-glycoprotein mediated drug toxicity induced by bioflavonoids: an integrated computational approach

In this work, molecular docking, pharmacophore modeling and molecular dynamics (MD) simulation were rendered for the mouse P-glycoprotein (P-gp) (code: 4Q9H) and bioflavonoids; amorphigenin, chrysin, epigallocatechin, formononetin and rotenone including a positive control; verapamil to identify protein–ligand interaction features including binding affinities, interaction characteristics, hot-spot amino acid residues and complex stabilities. These flavonoids occupied the same binding site with high binding affinities and shared the same key residues for their binding interactions and the binding region of the flavonoids was revealed that overlapped the ATP binding region with hydrophobic and hydrophilic interactions suggesting a competitive inhibition mechanism of the compounds. Root mean square deviations (RMSDs) analysis of MD trajectories of the protein–ligand complexes and NBD2 residues, and ligands pointed out these residues were stable throughout the duration of MD simulations. Thus, the applied preliminary structure-based molecular modeling approach of interactions between NBD2 and flavonoids may be gainful to realize the intimate inhibition mechanism of P-gp at NBD2 level and on the basis of the obtained data, it can be concluded that these bioflavonoids have the potential to cause herb–drug interactions or be used as lead molecules for the inhibition of P-gp (as anti-multidrug resistance agents) via the NBD2 blocking mechanism in future.