Synthesis of hydroxy benzoin/benzil analogs and investigation of their antioxidant, antimicrobial, enzyme inhibition, and cytotoxic activities

In this study, hydroxy benzoin (1-7), benzil (8-14), and benzoin/benzil-O-beta-D-glucosides (15-25) were synthesized to investigate their biological activities. An efficient method for synthesizing hydroxy benzoin compounds (1-7) was prepared from four different benzaldehydes using an ultrasonic bath. Then, antioxidant (FRAP, CUPRAC, and DPPH), antimicrobial (3 Gram (-), 4/6 Gram (+), one tuberculosis and one fungus), and enzyme inhibition (acetylcholinesterase, butyrylcholine esterase, tyrosinase, alpha-amylase, and alpha- glucosidase) for the all synthesized compounds (1-25) were evaluated. And also, four most active compounds (4, 12, 18a+b, and 25) from each group were evaluated to the human cervical cancer cell line (HeLa) and anticancer screening tests against the human retinal normal cell line (RPE). Compound 4 showed HeLa and RPE cancer cell activities as much as cisplatin. The synthesized compounds were characterized by spectroscopic methods (NMR, FT-IR, UV, LC-QTOF-MS) and the ACD NMR program's help

Can intra-articular 1 alpha, 25-dihydroxyvitamin D3 administration be therapeutical in joint cartilage damage?

INTRODUCTION Vitamin D-deficiency is known to cause nerve conduction impairments, cancer and chronic diseases, as well as the pathogenesis of osteoarthritis. Our goal with this study is to evaluate the cartilage healing by applying intraarticular 1 alpha, 25 (OH) 2D3 at different doses in rats with normal vitamin D levels and metabolism, which we made focal chondral damage model in the knee joint. MATERIAL AND METHODS 35 male Sprague-Dawley rats aged 20-24 weeks were used in our study. Both knees of rats were cartilage defected surgically on day 0. Joint injections performed at 06:00 am on 0th and 2nd days and after second injection others performed on days 9-16 and 23 following a weekly period. RESULTS In the fourth week, hematoxylin eosin staining measurements showed statistically significant difference according to the groups (p < 0.01) Metalloproteinase-13 (MMP-13) in histological staining for evaluating cartilage healing and healing levels showed statistically significant differences between the groups at first week and fourth week (p < 0.05). DISCUSSION Vitamin D, which affects many tissues through its receptors, is believed to be chondroprotective and neuroprotective by decreasing the expression of MMP in cartilage fibroblast, macrophage, lymphocyte through its intracellular receptors. To the best of our knowledge, this is the first study known to be intraarticular use of 1 alpha, 25-dihydroxyvitamin D3. Our study has been found to be safe and successful in terms of weight, systemic PTH and 1 alpha, 25-dihydroxyvitamin D3 levels in rats during treatment as well as better healing of cartilage damage

Primary Hydatid Cyst of the Axillary Region: A Case Report

Hydatid disease, which is caused by Echinococcus granulosus, is a common public health problem worldwide. The hydatid cysts may take many years to produce clinical symptoms. The liver is the organ most commonly affected. Diagnosis is made by a combination of clinical, imaging, serological and molecular techniques. Primary axillary hydatid disease is extremely rare and only 9 cases have been reported up to now. Herein, we reported a 48-year-old case with primary isolated hydatid disease in the axilla in whom total cystectomy was performed

Evaluation of the Surgeons’ Approach to HIV Infection

Introduction: The number of persons diagnosed as HIV positive is increasing rapidly in Turkey. Although the overall prevalence of the disease is still low, the increase of newly diagnosed persons emerges an important concern dealing with the awareness of the clinicians, and especially the surgeons. The aim of the study is to evaluate the approach of surgeons to HIV infection in the hospital. Materials and Methods: A 12-item self-administered anonymous questionnaire about the HIV infection with true and false options was developed. The questionnaire also included the specialty, age, duration of occupation and position of the surgeons. The questions were targeted to learn the knowledge and attitude about transmission route, occupational risk of acquiring HIV infection, prophylaxis for prevention, reluctance for operation and current drug therapy. The questionnaires were voluntarily filled by surgeons in November 2017. The descriptive statistics of the study were calculated as numbers and percentages. Yates’ corrected chi-square and Fisher’s exact tests were used in comparative analysis. Mann-Whitney U test and Spearman correlation test was used for comparison of continuous variables and correlation, respectively. Results: The total number of filled questionnaires was 90. In 90 of them, the demographic fields were filled. Among 90 surgeons, 37% (33/90) were assistant doctors between the ages of 25-31 years, and the duration of occupation was between 1-6 years. The remaining was older than 31 years of age and the duration of occupation as surgeon was 5-40 years. Specialties were urology, orthopedics, plastic surgery, obstetrics and gynecology, ophthalmic surgery, ear-nose-throat surgery, cardiovascular, general surgery, and neurosurgery. The results generally denote that the surgeons are aware of the occupational risk of HIV infection. Current knowledge about transmission risk evaluation, existence of prevention prophylaxis, advance in HIV treatment and prolonged life expectancy were less than expected. Correspondingly, half of the surgeons were reluctant to touch the patients. For each question, there was no statistically important difference between the answers of the surgeons according to position (residency doctor or specialist) (p> 0.05). There was also no statistically important difference between the answers of the surgeons according to age and duration of occupation (p> 0.05). Any significant correlation was not detected when age and duration of occupation were evaluated according to the total number of true answers (p= 0.802, r= -0.028 and p= 0.831, r= 0.023 respectively) Conclusion: The survey revealed the need for a meeting to be held with the surgeons of our hospital regarding the current status of the disease in the near future

Molecular docking, synthesis and biological evaluation (enzyme inhibition, antimicrobial and antioxidant) of methoxy benzoin/benzil/stilbenoid derivatives

In this study. methoxy benzoin compounds (1-10) were synthesized from the corresponding aromatic aldehydes based on a screening of biological activity. Oxidation and reduction of benzoins (1-10) yielded the corresponding benzils (11-20) and stilbenoids (21-29), respectively. The enzyme inhibition, antimicrobial, and antioxidant activities of 1-29 were evaluated. 1, 14, 19, and 28 against alpha-amylase, 15 and 19 against a-glucosidase, 2, 4, 14, 18, 25 and 26 against tyrosinase, 2, 7, and 23 against AChE, and 7, and 13 against BChE showed similar activity to the standard used. Among the methoxy benzoin derivatives, 4 proved to be the most active compound against E.coli, Y.pseudotuberculosis, M. smegmatis, and C.albicans in the range of 41-82 mu g/mL MIC values. All benzil derivatives displayed bioactivity against M.smegmatis and C. albicans. Compounds 18 and 11 were found to be most effective against M.smegmatis, and compounds 11 and 17 were found to be the most effective against C.albicans. All stilbenoid type compounds showed selective activity against B.cereus. Compounds 21 and 22 were the most effective stilbenoid compounds against M. smegmatis. Benzoins (1-10) were the most effective antioxidants among all three groups compared to the tested methods, which can be attributed to the free hydroxyl at the benzylic position. As a result, the change of carbon skeleton and substitution at different positions of synthesized organic compounds also caused the variation of biological activity

Synthesis, biological evaluation (antioxidant, antimicrobial, enzyme inhibition, and cytotoxic) and molecular docking study of hydroxy methoxy benzoin/benzil analogous

In this work, due to the biological activity evaluation, a series of hydroxy methoxy benzoins (1–8), benzils (10–16) and methoxy benzoin/benzil-O-β-D-glucosides (17–28) were synthesized. Antioxidant (FRAP, CUPRAC, DPPH), antimicrobial (16 microorganisms, and two yeast), enzyme inhibition (α-amylase, α-glucosidase, AChE, BChE, and tyrosinase) of all synthesized benzoin/benzil analogs were investigated. Benzoins (1–8) showed the most effective antioxidant properties compared to all three methods. Compound 28 against α-amylase, compound 9 against α-glucosidase, compound 11 against AChE, compound 2 against BChE, and compound 13 against tyrosinase showed the best activities with the better or similar IC50 values as used standards. Hydroxy methoxy benzoin compounds (1–8) among all four groups were seen as the most effective against the tested microorganism. Molecular docking analysis showed that all tested compounds 1–28 (0.01–2.22 µM) had the best binding affinity against AChE enzyme. Cytotoxic effects of the many of compounds (1–16, 21, and 24) also investigated and it was found that they caused different effects in different cells. The LDH tests of compounds 1a + b, 4, 7, 8, 9, 11, 12, 21, and 24, seemed to be effective compared to the positive control cisplatin. The cytotoxicity of compounds 6 (9.24%) for MCF7 cancer cells, 8 (5.16%) and 4 (8.26%) for HT29 cancer cells, 24 (9.84%) for Hep3B cells and 8 (8.52%), 7 (5.70%), 4 (6.94) and 9 (7.22%) for C6 cells were at normal values. And also cytotoxic activity of four compounds (5, 9, 21, and 24) among the all synthetic groups, were evaluated to the HeLa and RPE. Compound 5 showed anticancer activity on HeLa and RPE cancer cells as much as or better than cisplatin which was used as standard. © 2021 Elsevier Inc