The anticancer/cytotoxic effect of a novel gallic acid derivative in non-small cell lung carcinoma A549 cells and peripheral blood mononuclear cells from healthy individuals and lung cancer patients.

Gallic acid (GA) is a naturally occurring polyphenol with a strong antioxidant capacity. GA stimulates the apoptosis of cancer cells, thereby suppressing cancer cell invasion. However, the low oral permeability of GA limits its therapeutic use. In order to enhance the antioxidant capacity and oral permeability of GA, a series of compounds analogous to GA were synthesized: 4-methoxybenzenesulfonamide (MBS), 3,4-dimethoxybenzenesulfonamide (DMBS) and 3,4,5-trimethoxybenzenesulfonamide (TMBS). In the new compounds, hydroxyl groups were replaced with various numbers of methoxy groups (stronger electron-donating groups), to increase hydrophobicity and oral permeability compared to GA. In addition, the carboxylic group was replaced with a sulfonyl group (a stronger electron-withdrawing group), to increase the molecular polarity and antioxidative activities of the compounds. The cell counting kit-8 (CCK-8) assay was used to detect the effect of GA, MBS, DMBS, and TMBS on cell proliferation and apoptosis in peripheral blood mononuclear cells (PBMCs) from healthy individuals and non-small cell lung carcinoma A549 cells. Additionally, the comet assay was used to assess the genotoxicity of these compounds in PBMCs from healthy individuals, lung cancer patients, and A549 cells. Compared to untreated cells, TMBS reduced DNA damage more effectively than GA in PBMCs from lung cancer patients and healthy donors. Furthermore, in comparison to GA, TMBS was more cytotoxic in A549 cells. Moreover, TMBS was not cytotoxic in healthy PBMCs, suggesting that TMBS demonstrates therapeutic potential in cancer.

Alcohol delamination of the corneal epithelium for recalcitrant recurrent corneal erosion syndrome: a prospective study of efficacy and safety.

AIM: To investigate the safety and efficacy of alcohol delamination of the corneal epithelium for recalcitrant recurrent corneal erosion syndrome (RCE) in a prospective non-comparative interventional case series. METHODS: Patients with RCE who remained symptomatic despite topical lubrication and 3-month use of an extended wear (bandage) contact lens were included. The intensity of pain on a scale of 1 to 10, and duration and frequency of attacks were recorded. Patients were treated with alcohol delamination and followed up at 1 week, 1 month and then at 12 months, which was the minimum follow up time. Success was defined as a resolution of symptoms after 1 month of treatment, and partial success as a significant reduction in symptoms manageable with topical lubricants, and failure where symptoms were unchanged or worsened. RESULTS: 20 eyes of 20 patients with RCE caused by trauma (n = 14), anterior basement membrane dystrophy (n = 5) or idiopathic (1) were studied. The mean age of patients was 44 years and mean follow-up 24 months. Two eyes were lost to follow-up. 15 (83%) eyes were qualified as successes, 3 as partial successes and no failures were seen. No intraoperative complications were observed. 1 patient developed transient subepithelial haze that resolved with topical steroid, 1 had a change in refraction and 1 developed herpetic stromal keratitis 2 months postoperatively, which was successfully treated. No loss of vision was observed in any of the patients. CONCLUSION: Alcohol delamination of the corneal epithelium is a safe and effective method for treating patients with recalcitrant RCE.

Alcohol delamination of the corneal epithelium: an alternative in the management of recurrent corneal erosions.

PURPOSE: To investigate the efficacy of alcohol delamination in the management of recurrent corneal erosions (RCEs). DESIGN: Prospective single-center consecutive descriptive case series. PARTICIPANTS: Twelve patients with RCEs who did not respond to conservative management were treated with alcohol delamination. METHODS: A consecutive case series of 12 patients with RCEs who did not respond to conservative management were treated by alcohol delamination. A pain score was generated based on a visual analog scale of pain intensity. The duration of pain and frequency were also recorded. Patients were followed up at 1 week, 4 weeks, 3 months, 6 months, and 1 year and then at yearly intervals and monitored for recurrence of symptoms and corneal morphology. The removed epithelial sheet was examined by electron microscopy in 4 patients. INTERVENTION: The affected area of epithelium was peeled off after an application of 20% alcohol for 40 seconds under topical anesthesia. Eyes of patients were treated with an antibiotic and preservative-free artificial tear medication, and a bandage contact lens was inserted until epithelial healing was complete. MAIN OUTCOME MEASURES: Frequency of recurrence of erosions and duration and intensity of symptoms after alcohol delamination were studied. RESULTS: Eleven of the 12 eyes of patients had dramatic relief of symptoms over the follow-up period, ranging from 6 to 40 months. Eight patients were symptom free, and 1 patient had 2 mild symptom episodes in the first posttreatment month before becoming symptom free. The average follow-up period was 23.5 months. There were no residual effects from the application of alcohol noted in any patient. Electron microscopy of removed epithelium showed features of the underlying pathology. The separation of the epithelium occurred at the interface of the subepithelial abnormal deposit and the surface of Bowman's zone. CONCLUSION: Alcohol delamination appears to be a novel, simple, inexpensive treatment for RCEs. Unlike other methods, the removed epithelium is available as a sheet that may be subjected to further examination, though some of the changes observed may reflect the effect of alcohol on the epithelium.

Aqueous humor levels of topically applied bupivacaine 0.75% in cataract surgery.

PURPOSE: To measure the intraocular levels of bupivacaine 0.75% topically applied before phacoemulsification and to develop standards for topical anesthesia in cataract surgery. SETTING: Department of Ophthalmology, University Hospitals of Leicester, Leicester, United Kingdom. METHODS: Forty eyes having phacoemulsification for senile cataract under topical anesthesia without sedation were randomly assigned to 1 of 2 preoperative topical anesthesia regimens. Bupivacaine 0.75% was applied in 0.1 mL drops 3 times in the 30 minutes before surgery in 18 eyes and 6 times in the 60 minutes before surgery in 22 eyes. Aqueous humor and serum samples were taken at the start of surgery and the bupivacaine levels measured. A visual analog pain score scale was used to indicate intraoperative pain. RESULTS: The mean aqueous humor level of bupivacaine was 5.9 microg/mL +/- 4.3 (SD) after 3 drops and 5.7 +/- 4.0 microg /mL after 6 drops. The blood levels were less than 1.0 microg/mL. There was no statistically significant difference in the intraocular level of bupivacaine between the 2 groups. There was no difference in the age or sex distribution between the 2 groups, although there was an increase in the intraocular level of bupivacaine with age (approximately 1.4 microg/mL per decade; P =.048). There was no clear pattern associating the pain score with age, sex, or intraocular level of bupivacaine. CONCLUSIONS: A 3-drop regimen of bupivacaine 0.75% in the half hour before cataract surgery penetrated the eye as effectively as 6 drops in the 1 hour before surgery and provided good analgesia for phacoemulsification. Bupivacaine 0.75% penetrated the eye increasingly effectively with increasing age.