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Chirality plays a key role in the effectiveness and toxicity of bioactive compounds. Usnic acid (UA), a lichen metabolite, exists as two enantiomers. Despite numerous studies on its biological properties, enantioselective aspects remain poorly recognized. This study assessed the cytotoxicity of UA enantiomers against colon, prostate, thyroid, brain, and breast cancer cell lines, as well as non-cancerous cells. Cell viability was determined by the MTT assay after 24, 48, and 72 h. Colon cancer HCT116 cells were the most sensitive (IC50 ~10 µg/mL, 72 h), with no enantiomeric dominance. In prostate cancer PC3 cells, (+)-UA was more effective. Moderate cytotoxic effect was noted for thyroid cancer cells; however, this was evaluated for the first time. MDA-MB-231 breast cancer cells were strongly affected (IC50 15.8 and 20.2 µg/mL for (+)- and (−)-UA, 72 h), as compared to MCF7 cells. Brain cancer cells were the least affected, as so were normal astrocytes. UA had no effect on normal colon epithelial cells but showed moderate toxicity in prostate, thyroid, and breast cells. To conclude, the overall cytotoxicity of (+)-UA was stronger than its (−)-enantiomer, while the latter compound was more toxic to normal cells. These findings highlight the advantage of (+)-UA, especially in chemopreventive strategies.

Erucic acid (EA) is monounsaturated fatty acid (22:1 n-9), synthesized in the seeds of many plants from the Brassicaceae family, with Brassica napus, B. rapa, or B. carinata considered as its richest source. As the compound has been blamed for the poisoning effect in Toxic Oil Syndrome, and some data indicated its cardiotoxicity to rats, EA has been for decades classified as toxic substance, the use of which should be avoided. However, the cardiac adverse effects of EA have not been confirmed in humans, and the experiments in animal models had many limitations. Thus, the aim of this review was to present the results of the so far published studies on both toxic, and pharmacological properties of EA, trying to answer the question on its future medicinal use. Despite the ambiguous and relatively small data on toxic and beneficial effects of EA it seems that the compound is worth investigating. Further research should be particularly directed at the verification EA toxicity, more in-depth studies on its neuroprotective and cytotoxic properties, but also its use in combination with other drugs, as well as its role as a drug carrier.

Levothyroxine (l-thyroxine, l-T4) is a drug of choice for treating congenital and primary hypothyroidism. Although clinically significant interactions between l-T4 and food can alter the safety and efficacy of the treatment, they still seem to be generally underestimated by patients, physicians and pharmacists. This review aimed to investigate the effects of meals, beverages, and dietary supplements consumption on l-T4 pharmacokinetics and pharmacodynamics, to identify the most evident interactions, and to perform the recommendations for safe co-administering of l-T4 and food. A total of 121 studies were identified following a systematic literature search adhering to PRISMA guidelines. After full-text evaluation, 63 studies were included. The results proved that l-T4 ingestion in the morning and at bedtime are equally effective, and also that the co-administration of l-T4 with food depends on the drug formulation. We found limited evidence for l-T4 interactions with coffee, soy products, fiber, calcium or iron supplements, and enteral nutrition but interestingly they all resulted in decreased l-T4 absorption. The altered l-T4 efficacy when ingested with milk, juices, papaya, aluminium-containing preparations, and chromium supplements, as well as observed enhancement effect of vitamin C on l-T4 absorption, shall be further investigated in larger, well-designed studies. Novel formulations are likely to solve the problem of coffee, calcium and iron induced malabsorption of l-T4. Maintaining a proper time interval between l-T4 and food intake, especially for coffee and calcium, or iron supplements, provides another effective method of eliminating such interactions.

Among all legumes sprouts’ active compounds, isoflavones seem to be the most important; nevertheless, their high content is not always associated with beneficial effects. These compounds may prevent or stimulate hormone-dependent cancers due to their estrogen-like activity. Different LED light quality can change the synthesis of active compounds and significantly influence the biological activity of the sprouts. This study aimed to evaluate the effects of LED light (red, blue, green, yellow), as well as total darkness, and natural light conditions (as reference), on isoflavones content, determined by HPLC-UV-VIS, during 10 days of harvesting of chickpea and lupin sprouts. Due to the ambiguous estrogenic potential of isoflavones, the impact of these sprouts on normal and cancer prostate and breast cells was evaluated. Yellow LED light resulted in the highest sum of isoflavones in chickpea sprouts (up to 1 g/100 g dw), while for green LED light, the isoflavones sum was the lowest. The exact opposite effect was noted for lupin sprouts, with the predominance of green over the yellow LED light. The examined sprouts were of high safety to non-neoplastic breast and prostate cells, with interesting cytotoxic effects on breast MCF7 and prostate DU145 cancer cells. No clear relationship was observed between the activity and isoflavones content.

The Fabaceae family is known for the presence of isoflavones—phytoestrogens with potential chemopreventive effects against hormone-dependent cancers. This study aimed to optimize isoflavones extraction using a fractional factorial design and to quantitatively and qualitatively analyze 32 Fabaceae species native to Polish flora by HPLC-UV-VIS to indicate new, rich plant sources of isoflavones. The optimal extraction method was a 60 min reflux with 50% methanol and a plant material-to-solvent ratio of 1:125. The highest isoflavone levels were found in Trifolium medium (26.70 mg/g d.m.), Genista tinctoria (19.65 mg/g d.m.), and Trifolium pratense (12.56 mg/g d.m.). The obtained extracts were further evaluated for cytotoxic and antiproliferative activity against MCF7 and MDA-MB-231 human breast cancer cells. Genista tinctoria showed the highest cytotoxicity against MCF7, while Cytisus scoparius and Ononis arvensis were most effective against MDA-MB-231 at a dose of 500 µg/mL. The extracts were also characterized by varied, potent antioxidant properties, important in chemoprevention. A strong correlation was observed between isoflavone content and cytotoxic and antiproliferative activity exclusively in the estrogen receptor-positive MCF7 cell line. Importantly, the tested extracts demonstrated no toxic effects on normal human liver (HepG2), thyroid (Nthy-ori 3-1), or breast (MCF10A) cells, indicating a favorable safety profile.

This review is focused on the comparison of the biological and pharmacological activities of usnic acid enantiomers. Most of the available data refer to (+)-usnic acid, while the left-handed isomer has been less often significantly studied. Special attention was paid to the experiments comparing both (+)- and (−)-usnic acid at the same time, the results of which indicated interesting differences, however no tendency as to which enantiomer was more potent could be observed. Nevertheless, more studies, especially on (−)-usnic acid, are needed to give a final explanation for the similarities and differences between both usnic acid enantiomers. These should be especially directed to steric structure–activity relationship of the enantiomers, tested under the same experimental conditions, which may help to explain the possible mechanisms of their actions.

Dragon fruits are a valued source of bioactive compounds with high potential to become a functional food. The aim of the study was to evaluate and compare the chemopreventive potential and chemical composition of fruits harvested in Thailand and Israel. The amount of different compounds in water and methanol extracts and antioxidant activity was investigated. Moreover, cytotoxic activity against cancer and normal cells of skin, prostate, and gastrointestinal origin was performed, accompanied by anti-inflammatory assay based on NO production in RAW 264.7 macrophage model. Additionally, the quenching properties of polyphenols from fruits were determined by the interaction of the main drug carrier in blood human serum (HSA). The chemometric analysis was used to reveal the relationships between the determined parameters. Dragon fruits harvested in Israel revealed higher antioxidant properties and total content of polyphenols and betacyanins when compared to those from Thailand. The examined fruits of both origins showed significant cytotoxic activity toward colon and prostate cancer cells, with no toxic effect on normal cells, but also no anti-inflammatory effect. Moreover, a high binding ability to HSA was observed for water extracts of dragon fruits. All these predestine dragon fruits are the candidates for the attractive and chemopreventive elements of daily diet.

Amaranth oil (AMO) and its topical formulation enriched with rose oil (AMOR) were evaluated for anti-inflammatory and cytotoxic properties in skin-relevant models. Two complementary inflammation models were used to assess immunomodulatory potential, (i) LPS-stimulated macrophages and (ii) TNF-α/IFN-γ-stimulated immortalized HaCaT keratinocytes, while cytotoxicity and selectivity were tested on human HaCaT keratinocytes and melanoma cell lines (A375, HTB140). GC-MS and FTIR analyses were performed to confirm the presence of key bioactive compounds (squalene, fatty acids, phenolics). AMOR showed significantly higher polyphenol and palmitic acid content than AMO. In both inflammation models, AMOR more effectively reduced IL-6, IL-1β, and TNF-α release. Cytotoxicity assays revealed that both oils were safe for normal keratinocytes, while selectively cytotoxic to melanoma cells, with AMOR demonstrating greater potency (IC50 A375 = 3.8 μg/mL and HTB140 = 18.9 μg/mL). Albumin-binding studies showed that AMOR had stronger interactions with these proteins, which may enhance delivery and tissue retention. In conclusion, both oils exhibit promising topical safety, but AMOR provides enhanced anti-inflammatory and cytotoxic effects due to its enriched composition. This study supports the therapeutic potential of amaranth oil in different skin diseases, especially when combined with essential oils of complementary bioactivity.

The main aim of this study was to evaluate the effect of space-like environment on the chemopreventive activity of Brassica sprouts against thyroid cancer cells in vitro. For this purpose the sprouts of broccoli, kale, kohlrabi, and Brussels sprouts were cultivated in darkness and in microgravity for 5–7 days. Then, the sprouts’ extracts were examined for cytotoxic and antiproliferative activity against thyroid cancer and normal cells. The tested microgravity environment stimulated the cytotoxic activity of kohlrabi sprouts, causing approximately 50% reduction in thyroid cancer cells’ viability, while at the same time increasing the viability of normal thyroid cells. Broccoli sprouts showed the strongest antiproliferative activity against normal thyroid cells, with the best effect visible for darkness conditions, which may contribute to the reduction of thyroid hyperplasia. Microgravity and darkness significantly enhanced the antiproliferative activity of kale, especially in 7-day-old sprouts (inhibition approximately 90%). The tested conditions also increased the antiproliferative activity of kohlrabi sprouts, but in the case of Brussels sprouts the effect was unfavorable. The study showed that microgravity and darkness conditions may have significant influence on the chemopreventive role of Brassica sprouts against thyroid cancer cells in vitro, especially in the case of broccoli and kohlrabi sprouts.

Type 2 diabetes mellitus (T2DM) is a chronic metabolic disorder characterized by impaired glucose regulation. This study evaluated the antioxidant and antidiabetic potential of aqueous extracts from four plant species from the southern Algarve: Aristolochia baetica, Chelidonium majus, Dittrichia viscosa, and Lavandula viridis, using non-cellular in vitro assays. HPLC/PDA was used to identify active compounds. Antioxidant activity was assessed by using TAA, FRAP, RP, and DPPH assays; antidiabetic potential through alpha-glucosidase and alpha-amylase inhibition; and wound healing relevance through elastase, collagenase, and lipoxygenase inhibition. D. viscosa showed the highest antioxidant activity (FRAP: 1132.99 +/- 19.54 mg TE/g dw; DPPH IC50 = 25.85 +/- 0.75 mu g/mL) and total phenolic/flavonoid content, with a diverse profile including caffeic and chlorogenic acids, isoquercetin, and quercetin. It also exhibited potent alpha-glucosidase inhibition (IC50 = 0.61 +/- 0.06 mg/mL), outperforming acarbose. L. viridis had the highest total phenolic content (39.04 mg/g), while A. baetica demonstrated the strongest anti-elastase, anti-collagenase, and lipoxygenase activity, suggesting wound-healing potential. C. majus showed the weakest effects. A strong correlation was observed between phenolic content and antioxidant/antidiabetic activity. These findings support further in vivo studies on D. viscosa and A. baetica for potential use in T2DM management and diabetic wound healing.