Yağmur Özhan

Tanacetum parthenium (L.) Sch.Bip., a well-known member of the Asteraceae family, has long been used in traditional medicine against different ailments. Although the biological activities of its extracts and constituents such as parthenolide have been extensively studied, investigations on its essential oil remain limited. This study aimed to investigate the chemical composition and in vitro biological activities of essential oil obtained from T. parthenium wild-growing in Türkiye. The essential oil was obtained via steam distillation and analyzed by GC-FID and GC-MS. Its anti-inflammatory potential was evaluated by measuring nitric oxide (NO) inhibition in LPS-stimulated RAW 264.7 macrophages using the Griess assay. In addition, the cytotoxic effects of the essential oil were assessed on two human breast cancer cell lines (MCF-7 and MDA-MB-231) using the MTT assay. The results showed that the essential oil reduced NO production by 27% and 11% with 0.5 and 1 mg/mL, and exhibited weak cytotoxicity with IC₅₀ values of 333 ± 2.5 µg/mL and 214 ± 13.8 µg/mL against MCF-7 and MDA-MB-231, respectively. These findings highlight the potential of T. parthenium essential oil as a natural source of bioactive compounds with anti-inflammatory and anticancer properties, warranting further pharmacological and phytochemical investigations.

Objectives: Third-hand smoke (THS) is residual smoke after extinguishing a cigarette and adhering to surfaces. Re-emission into the air also makes THS a health concern for those who suffer from respiratory diseases. The present study aimed to elucidate the mechanistic pathways involved in THS-induced respiratory toxicity and the accelerative potential of THS in an H2O2-induced oxidative stress model of human airway epithelia in vitro. Materials and Methods: THS extracted from terrycloth exposed to 3R4F cigarettes was assessed via 3-(4,5-dimethylthiazol-2-yl)-2,5diphenyltetrazolium bromide assay to identify cytotoxicity. The reactive oxygen species (ROS) level was determined via 2,7-dichlorofluorescein diacetate (DCFDA) fluorescence intensity in a flow cytometer, and glutathione (GSH), malondialdehyde (MDA), and catalase (CAT) activity were assessed spectrophotometrically. Interleukin-6 (IL-6) level was measured via enzyme-linked immunosorbent assay. Results: THS 50% (v/v) with significant cytotoxicity in A549 cells upregulated intracellular ROS levels via a right-shifted fluorescence intensity of DCFDA compared with the control (p < 0.05), which was also amplified with H2O2 co-treatment. MDA levels remarkably increased with THS (p < 0.05). Both THS and THS + H2O2 led to notable GSH depletion, increased CAT activity, and increased IL-6 levels, which were attenuated by the negative control (N-acetylcysteine, 1 mM) (p < 0.05). Conclusion: The induction of oxidative stress may be an important event in THS-induced airway toxicity that may contribute to the progression of respiratory diseases.

Crataegus turcicus is a plant endemic to Türkiye. For the first time, this study aimed to comparatively assess its flower-bearing branches, leaves, and fruits with other well-known Crataegus species (C. monogyna, C. pentagyna, and C. orientalis) in terms of chemical composition and bioactivity studies to evaluate its potential use as a food supplement. Firstly, the contents of total phenolics (TPC), flavonoids (TFC), proanthocyanidin (TPAC), and anthocyanin (TAC) in different plant parts of Crataegus species were evaluated. The highest TPAC was found in the hydroalcoholic extract of C. turcicus flower-bearing branches. Moreover, all plant parts had comparatively higher amounts of TPC, TFC, and TAC compared to other Crataegus species. The chemical screening by high-performance thin-layer chromatography (HPTLC) resulted that C. turcicus parts were rich with chlorogenic acid, neochlorogenic acid, quercetin and vitexin derivatives, epicatechin, procyanidin, etc., and their quantities were evaluated by high-performance liquid chromatography (HPLC). In terms of several in vitro antioxidant activity outcomes, the flower-bearing branches of C. turcicus showed the highest antioxidant activity by a 2,2-diphenyl-1-picrylhydrazyl (DPPH) test among the assessed antioxidant assays. Additionally, hydroalcoholic extracts of C. turcicus significantly decreased LPS-induced nitric oxide, tumor necrosis factor-alpha, and interleukin-6 production more potently than indomethacin (positive control). In addition to its remarkable anti-inflammatory activity, C. turcicus showed analgesic activity by reducing prostaglandin E₂ levels.

Cancer is the disease with the highest mortality. Drug studies contribute to promising treatments; however there is an urgent need for selective drug candidates. Pancreatic cancer is difficult to treat and the cancer progresses rapidly. Unfortunately, current treatments are ineffective. In this study, ten new diarylthiophene-2-carbohydrazide derivatives were synthesized and evaluated for their pharmacological activity. The 2D and 3D anticancer activity studies suggested the compounds 7a, 7d, and 7f were promising. Among these, 7f (4.86 µM) showed the best 2D inhibitory activity against PaCa-2 cells. Compounds 7a, 7d and 7f were also tested for their cytotoxic effects on healthy cell line but only compound 7d showed selectivity. Compounds 7a, 7d, and 7f showed the best 3D cell line inhibitory effect according to spheroid diameters. The compounds were screened for their COX-2 and 5-LOX inhibitory activity. For COX-2, the best IC₅₀ value was observed for 7c (10.13 µM) and all compounds showed significantly lower inhibition compared to standard. In the 5-LOX inhibition study, compounds 7a (3.78 µM), 7c (2.60 µM), 7e (3.3 µM), and 7f (2.94 µM) demonstrated influential activity compared to standard. Regarding molecular docking studies, binding mode of compounds 7c, 7e, and 7f to the 5-LOX enzyme were non-redox or redox types, but not the iron-binding type. As dual inhibitors of 5-LOX and pancreatic cancer cell line, 7a and 7f were identified as the most promising compounds.

Novel benzofurane-pyrazolone hybrids have been synthesized for evaluating their anti-inflammatory and cytotoxic properties. 4-(2-chloroacetyl)-1,5-dimethyl-2-phenyl-1,2-dihydro-3H-pyrazol-3-one were reacted with α-hydroxy aldehyde or α-hydroxy ketone derivatives to obtain nine novel pyrazolone derivatives. Structures were successfully elucidated by ¹H NMR, ¹³C NMR, IR and HRMS. Enzyme inhibitory activity was measured on cyclooxygenases (COXs) as considered to address anti-inflammatory activity. Compound 2 showed the highest activity on both COX-1 and COX-2 subtypes with 12.0 μM and 8.0 μM IC₅₀, respectively. This activity was found close to indomethacin COX-2 inhibition measured as 7.4 μM IC₅₀. Rest of the compounds (1, 3–9) showed 10.4–28.1 μM IC₅₀ on COX-2 and 17.0–35.6 μM IC₅₀ on COX-1 (Compound 1 has no activity on COX-1). Tested compounds (1–9) showed activity on NO production. Only compound was the 4, which showed a low inhibition on IL-6 levels. Cell viability was up to 60% at 100 μM for all compounds (1–9) on RAW 264.7 and NIH3T3 cell lines, thus compounds were reported to be noncytotoxic.