Secondary sulfonamides as effective lactoperoxidase inhibitors

Secondary sulfonamides (4a–8h) incorporating acetoxybenzamide, triacetoxybenzamide, hydroxybenzamide, and trihydroxybenzamide and possessing thiazole, pyrimidine, pyridine, isoxazole and thiadiazole groups were synthesized. Lactoperoxidase (LPO, E.C.1.11.1.7), as a natural antibacterial agent, is a peroxidase enzyme secreted from salivary, mammary, and other mucosal glands. In the present study, the in vitro inhibitory effects of some secondary sulfonamide derivatives (4a–8h) were examined against LPO. The obtained results reveal that secondary sulfonamide derivatives (4a–8h) are effective LPO inhibitors. The Ki values of secondary sulfonamide derivatives (4a–8h) were found in the range of 1.096 × 10−3 to 1203.83 µM against LPO. However, the most effective inhibition was found for N-(sulfathiazole)-3,4,5-triacetoxybenzamide (6a), with Ki values of 1.096 × 10−3 ± 0.471 × 10−3 µM as non-competitive inhibition

The acorn honey used for a published study was mistakenly listed as quercus pyrenaica and should be corrected to quercus species

A critical review letter1 was published concerning the article “Quercus pyrenaica honeydew honey effects on gastric adenocarcinoma cells” published in Integrative Cancer Therapies in 2019.2 According to the letter, the authors reported that the Quercus pyrenaica mentioned in the study was neither found in Mount Ida nor within the borders of Turkey as stated in the study, therefore the results obtained in the study may belong to another Quercus species

Quercus pyrenaica honeydew honey with high phenolic contents cause dna damage, apoptosis, and cell death through generation of reactive oxygen species in gastric adenocarcinoma cells

Many studies have shown that honey with high phenolic contents prevents cancer formation. Furthermore, recent studies have demonstrated that honey can be used for the treatment of cancer as well as cancer prevention. Antineoplastic effects of honey are often associated with their antioxidant phenolic contents. However, very few studies have dealt with the association of phenolic contents of honeys in terms of antiproliferative effects. The aim of this study was, therefore, to elucidate the cytotoxic, genotoxic, apoptotic, and reactive oxygen species (ROS) generating effects of honey samples on the basis of their phenolic and flavonoid contents. Fourteen different honey varieties were collected from various parts of Turkey, and their characteristics regarding total phenols, flavonoids, and antioxidant contents were determined to test their effects on gastric cancer cells (AGS). For convenience, 2 honey varieties were selected, namely, Ida Mountains Quercus pyrenaica honeydew honey (QPHH-IM) having the highest phenolic and antioxidant content and Canakkale multifloral honey (MFH-C) with the lowest phenolic and antioxidant content. Levels of 11 different phenolic compounds in QPHH-IM and MFH-C samples were determined by LC-MS/MS. AGS cells were incubated with different concentrations of QPHH-IM and MFH-C for 24 hours, then the cell viability, DNA damage, apoptosis, and generation of ROS were determined. We found that QPHH-IM had more cytotoxic, genotoxic, and apoptotic effects than that of MFH-C. We think that these effects are probably related to pro-oxidant activities due to the high phenolic contents present. Therefore, further research on high-phenolic honey may contribute to the future development of cancer therapeutics

Artemisia campestris and Artemisia herbaalba: LC-HRESI-MS Profile Alongside Their Antioxidant and Antimicrobial Evaluation

Artemisia species have been traditionally used to treat various ailments and health problems like colds, digestive troubles, gastric ulcer, menstrual pain, and diarrhea. In our study, total phenolic and flavonoid contents of 80% aqueous methanol extracts of Artemisia campestris and Artemisia herba-alba plants were investigated. Furthermore, their in vitro antioxidant and antimicrobial activities were evaluated. Also, their phytochemical profiling was performed via using LC-HRESI-MS analysis. Both plant extracts showed strong antioxidant activity using DPPH, ABTS, and phosphomolybdenum assays. The results revealed A. herba-alba extract showed moderate antimicrobial activity against bacteria including Staphylococcus epidermidis and Staphylococcus aureus. While A. campestris extract exhibited antimicrobial activity against different microbial populations such as Pseudomonas aeruginosa and Candida albicans. Also, the results revealed that A. herba-alba extract contains high amounts of 3-O-methylquercetin, eupatilin and acacetin (ranging from 22.04 to 31.88 mg/g), while A. campestris extract contains significant amounts of 3-O-methylquercetin, rutin and chlorogenic acid (82.98, 79.44 and 29.54 mg/ g, respectively). In conclusion, the aqueous methanol extracts of both studied Artemisia species could be promising candidates for treating microbial infections and oxidative stress

Ent-kaurene Diterpenoids from Sideritis lycia with Antiviral and Cytotoxic Activities

The genus Sideritis (Lamiaceae) is represented by 45 species (54 taxa) in Anatolia with high endemism ratio (74%), and Turkey is one of the gene centers of the genus along with Spain. Acetone extract of the aerial parts of Sideritis lycia afforded eight known ent-kaurene diterpenoids, structures of which have been identified as linearol, isolinearol, isosidol, sidol, siderol, sideridiol, 7-epi-candicandiol and foliol through 1H NMR, 13 C NMR and mass spectroscopic analyses. Cytotoxic and antiviral activities of the acetone extract, linearol, sidol and isosidol were investigated together with insecticidal activity of species. The antiviral index of linearol, isosidol and acetone extract of S. lycia were determined as 2.31, 2.01 and 2.58, respectively, except sidol. 7-Epi-candicandiol was found to be the most active diterpene against a series of cancer cell lines with ED50 values; KB (13.3 mu g/mL), COL-2 (11.8 mu g/mL), LU1 (17.9 mu g/mL), LNCaP (14.9 mu g/mL) and A2780 (9.0 mu g/mL). Activity results of this study indicated that ent-kaurane diterpenes have potential to be considered as antiviral and cytotoxic lead compounds

Sambulin A and B, non-glycosidic iridoids from Sambucus ebulus, exert significant in vitro anti-inflammatory activity in LPS-induced RAW 264.7 macrophages via inhibition of MAPKs's phosphorylation

WOS: 000406564500035PubMed ID: 28606808Ethnopharmacological relevance: The leaves of Sambucus ebulus L. (Adoxaceae) are widely used in Turkish folk medicine particularly against inflammatory disorders. The fresh leaves after wilted over fire or the poultices prepared are directly applied externally to heal burns, edema, eczema, urticarial and abscess. Two iridoids were recently isolated (sambulin A, sambulin B) from the leaves of S. ebulus. Aim of the study: This study aims to investigate the in vitro anti-inflammatory activities of these iridoids on LPS-induced RAW 264.7 macrophages. Materials and methods: Raw 264.7 macrophages were treated with 12.5, 25 and 50 mu g/ml Sambulin A and 6.25, 12.5 and 25 mu g/ml Sambulin B and induced with 1 mu g/ml lipopolysaccaharides (LPS). Effect of the compounds on nitric oxide (NO) production and cytoldnes (TNF alpha, IL-6) were determined by Griess and ELISA assays respectively. iNOS and the phosphorylation levels of MAPKs (ERK, JNK) were examined by Western Blot. Results: Sambulin A and sambulin B inhibited 52.82% and 72.88% of NO production at 50 and 25 mu g/ml concentrations respectively. The levels of iNOS were significantly decreased by both molecules, sambulin B at 25 mu g/ml almost completely decreased iNOS levels (97.53%). Both molecules significantly inhibited TNF alpha productions. However, only sambulin B inhibited IL-6 production. Consequently, it was shown that sambulin B exerted its effect through the inhibition of ERK and JNK phosphorylations. Conclusion: The prominent bioactivities exerted by two iridoids will contribute to explanation of the usage of S. ebulus in traditional medicine against rheumatoid diseases.Scientific and Technological Research Council of Turkey [TUBITAK] [110S197]This work was supported by The Scientific and Technological Research Council of Turkey [TUBITAK Project no: 110S197]