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1.
Int J Mol Sci ; 25(7)2024 Apr 03.
Article En | MEDLINE | ID: mdl-38612798

Brassica vegetables are widely consumed all over the world, especially in North America, Asia, and Europe. They are a rich source of sulfur compounds, such as glucosinolates (GLSs) and isothiocyanates (ITCs), which provide health benefits but are also suspected of having a goitrogenic effect. Adhering to PRISMA guidelines, we conducted a systematic review to assess the impact of dietary interventions on thyroid function, in terms of the potential risk for people with thyroid dysfunctions. We analyzed the results of 123 articles of in vitro, animal, and human studies, describing the impact of brassica plants and extracts on thyroid mass and histology, blood levels of TSH, T3, T4, iodine uptake, and the effect on thyroid cancer cells. We also presented the mechanisms of the goitrogenic potential of GLSs and ITCs, the limitations of the studies included, as well as further research directions. The vast majority of the results cast doubt on previous assumptions claiming that brassica plants have antithyroid effects in humans. Instead, they indicate that including brassica vegetables in the daily diet, particularly when accompanied by adequate iodine intake, poses no adverse effects on thyroid function.


Brassica , Goiter , Iodine , Animals , Humans , Vegetables , Isothiocyanates , Glucosinolates
2.
Molecules ; 29(5)2024 Feb 28.
Article En | MEDLINE | ID: mdl-38474555

BACKGROUND: Prostate cancer (PC) and benign prostatic hyperplasia (BPH) are common health problems in the aging male population. Due to the unexplored and unconfirmed impact of food containing isoflavones, like sprouts, on the development of the management of BPH and prostate cancer, we decided to extend the knowledge in this area. RESULTS: We have demonstrated for the first time that chickpea sprouts may play an important role in the chemoprevention of prostate disorders. However, attention should be paid to the isoflavone content in the sprouts, as in our study, chickpea sprouts with a moderate concentration of the compounds, harvested in natural light conditions (CA10L) and blue LED light (CA7B), showed the best scores in terms of their potential towards prostate disorders. METHODS: Chickpea seeds were grown in LED chambers. The methanol extracts from sprouts were quantitatively defined using the HPLC system. Experiments such as the determination of PSA, 5-α-reductase, and dihydrotestosterone were performed on PNT2 and LNCaP cells. For anti-inflammatory assays (determination of NO, IL-6, and TNF-alpha release), murine RAW264.7 macrophages were used. CONCLUSIONS: The role of legume products as a diet element should be deeply evaluated for the development of future dietary recommendations for prostate cancer and BPH prevention.


Cicer , Isoflavones , Prostatic Hyperplasia , Prostatic Neoplasms , Male , Humans , Animals , Mice , Cicer/chemistry , Prostate , Isoflavones/chemistry , Diet
3.
Plant Foods Hum Nutr ; 79(1): 151-158, 2024 Mar.
Article En | MEDLINE | ID: mdl-38231454

Amaranth, quinoa, and buckwheat are the representatives of pseudocereals, different parts and by-products of which are used in daily nutrition and food processing industry. However, only scarce information exists on the bioactivity of their oils. Thus, oils obtained from amaranth, buckwheat, and red, yellow, and white quinoa seeds were evaluated in terms of their nutritional (fatty acid profile, squalene), cytotoxic (against normal and neoplastic gastrointestinal, prostate, and skin cells), anti-inflammatory and antiradical (interleukin 6, TNF-alpha, nitric oxide, DPPH, Total phenolics, and superoxide dismutase) potential in the in vitro model. Linoleic (42.9-52.5%) and oleic (22.5-31.1%) acids were the two main unsaturated, while palmitic acid (4.9-18.6%) was the major saturated fatty acid in all evaluated oils. Squalene was identified in all evaluated oils with the highest content in amaranth oil (7.6 g/100 g), and the lowest in buckwheat oil (2.1 g/100 g). The evaluated oils exerted a high direct cytotoxic impact on cancer cells of different origins, but also revealed anti-inflammatory and antiradical potentials. Yellow quinoa oil was the most active, especially toward skin (A375; IC50 6.3 µg/mL), gastrointestinal (HT29 IC50 4.9 µg/mL), and prostate cancer cells (LNCaP IC50 7.6 µg/mL). The observed differences in the activity between the oils from the tested quinoa varieties deserve further studies. High selectivity of the oils was noted, which indicates their safety to normal cells. The obtained results indicate that the oils are good candidates for functional foods with perspective chemopreventive potential.


Seeds , Squalene , Squalene/analysis , Spectroscopy, Fourier Transform Infrared , Seeds/chemistry , Fatty Acids/analysis , Plant Oils/analysis , Anti-Inflammatory Agents/pharmacology , Anti-Inflammatory Agents/analysis
4.
Molecules ; 28(23)2023 Nov 24.
Article En | MEDLINE | ID: mdl-38067491

Melanoma is one of the most dangerous forms of skin cancer, characterized by early metastasis and rapid development. In search for effective treatment options, much attention is given to triterpenoids of plant origin, which are considered promising drug candidates due to their well described anticancer properties and relatively low toxicity. This paper comprehensively summarizes the antimelanoma potential of natural triterpenoids, that are also used as scaffolds for the development of more effective derivatives. These include betulin, betulinic acid, ursolic acid, maslinic acid, oleanolic acid, celastrol and lupeol. Some lesser-known triterpenoids that deserve attention in this context are 22ß-hydroxytingenone, cucurbitacins, geoditin A and ganoderic acids. Recently described mechanisms of action are presented, together with the results of preclinical in vitro and in vivo studies, as well as the use of drug delivery systems and pharmaceutical technologies to improve the bioavailability of triterpenoids. This paper also reviews the most promising structural modifications, based on structure-activity observations. In conclusion, triterpenoids of plant origin and some of their semi-synthetic derivatives exert significant cytotoxic, antiproliferative and chemopreventive effects that can be beneficial for melanoma treatment. Recent data indicate that their poor solubility in water, and thus low bioavailability, can be overcome by complexing with cyclodextrins, or the use of nanoparticles and ethosomes, thus making these compounds promising antimelanoma drug candidates for further development.


Antineoplastic Agents , Melanoma , Triterpenes , Humans , Biological Availability , Melanoma/drug therapy , Triterpenes/pharmacology , Triterpenes/chemistry , Antineoplastic Agents/chemistry
5.
Pharmaceuticals (Basel) ; 16(7)2023 Jul 05.
Article En | MEDLINE | ID: mdl-37513877

Benign prostatic hyperplasia (BPH) is a common urological disease affecting aging men. Its pathogenesis is regarded as complex and multifactorial, with sex hormones and inflammation as key contributory factors. In the current study, we investigated the anti-BPH potential of terpenoids present in the fruits of Sorbus intermedia (EHRH.) PERS. Not only the effects on testosterone-stimulated normal prostate epithelial PNT2 cells, namely suppression of 5-α-reductase activity, PSA secretion, and cell proliferation, were determined but also the inhibitory activity on heat-induced protein denaturation, hyaluronidase, as well as IL-6, TNF-α, and NO release in LPS-treated macrophages. Sorbus terpenoids significantly inhibited 5-α-reductase activity and reduced PSA secretion in PNT2 cells, reversing the stimulatory effect of testosterone. PNT2 cell proliferation was also found to be attenuated. Subsequently, all compounds reduced the release of pro-inflammatory mediators in RAW 264.7 cells. In addition, ursolic acid (UA) and its aldehyde (UAL) were the most potent hyaluronidase inhibitors of all compounds, with IC50 values of 225.75 µg/mL and 369.77 µg/mL, respectively. For better understanding and interpretation of the overall effect of Sorbus terpenoids on different aspects of BPH pathogenesis and development, cluster analysis was applied.

6.
Pharmaceutics ; 15(5)2023 Apr 28.
Article En | MEDLINE | ID: mdl-37242592

Saponins are plant metabolites that possess multidirectional biological activities, among these is antitumor potential. The mechanisms of anticancer activity of saponins are very complex and depend on various factors, including the chemical structure of saponins and the type of cell they target. The ability of saponins to enhance the efficacy of various chemotherapeutics has opened new perspectives for using them in combined anticancer chemotherapy. Co-administration of saponins with targeted toxins makes it possible to reduce the dose of the toxin and thus limit the side effects of overall therapy by mediating endosomal escape. Our study indicates that the saponin fraction CIL1 of Lysimachia ciliata L. can improve the efficacy of the EGFR-targeted toxin dianthin (DE). We investigated the effect of cotreatment with CIL1 + DE on cell viability in a 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) assay, on proliferation in a crystal violet assay (CV) and on pro-apoptotic activity using Annexin V/7 Actinomycin D (7-AAD) staining and luminescence detection of caspase levels. Cotreatment with CIL1 + DE enhanced the target cell-specific cytotoxicity, as well as the antiproliferative and proapoptotic properties. We found a 2200-fold increase in both the cytotoxic and antiproliferative efficacy of CIL1 + DE against HER14-targeted cells, while the effect on control NIH3T3 off-target cells was less profound (6.9- or 5.4-fold, respectively). Furthermore, we demonstrated that the CIL1 saponin fraction has a satisfactory in vitro safety profile with a lack of cytotoxic and mutagenic potential.

7.
Life (Basel) ; 13(4)2023 Apr 19.
Article En | MEDLINE | ID: mdl-37109575

Inflammation is a response of the organism to an external factor that disrupts its natural homeostasis, and it helps to eliminate the cause of tissue injury. However, sometimes the body's response is highly inadequate and the inflammation may become chronic. Thus, the search for novel anti-inflammatory agents is still needed. One of the groups of natural compounds that attract interest in this context is lichen metabolites, with usnic acid (UA) as the most promising candidate. The compound reveals a broad spectrum of pharmacological properties, among which anti-inflammatory properties have been studied both in vitro and in vivo. The aim of this review was to gather and critically evaluate the results of the so-far published data on the anti-inflammatory properties of UA. Despite some limitations and shortcomings of the studies included in this review, it can be concluded that UA has interesting anti-inflammatory potential. Further research should be directed at the (i) elucidation of the molecular mechanism of UA; (ii) verification of its safety; (iii) comparison of the efficacy and toxicity of UA enantiomers; (iv) design of UA derivatives with improved physicochemical properties and pharmacological activity; and (v) use of certain forms or delivery carriers of UA, especially in its topical application.

8.
Molecules ; 28(5)2023 Feb 22.
Article En | MEDLINE | ID: mdl-36903308

Due to problems with selenium deficiency in humans, the search for new organic molecules containing this element in plant biofortification process is highly required. Selenium organic esters evaluated in this study (E-NS-4, E-NS-17, E-NS-71, EDA-11, and EDA-117) are based mostly on benzoselenoate scaffolds, with some additional halogen atoms and various functional groups in the aliphatic side chain of different length, while one compound contains a phenylpiperazine moiety (WA-4b). In our previous study, the biofortification of kale sprouts with organoselenium compounds (at the concentrations of 15 mg/L in the culture fluid) strongly enhanced the synthesis of glucosinolates and isothiocyanates. Thus, the study aimed to discover the relationships between molecular characteristics of the organoselenium compounds used and the amount of sulfur phytochemicals in kale sprouts. The statistical partial least square model with eigenvalues equaled 3.98 and 1.03 for the first and second latent components, respectively, which explained 83.5% of variance in the predictive parameters, and 78.6% of response parameter variance was applied to reveal the existence of the correlation structure between molecular descriptors of selenium compounds as predictive parameters and biochemical features of studied sprouts as response parameters (correlation coefficients for parameters in PLS model in the range-0.521 ÷ 1.000). This study supported the conclusion that future biofortifiers composed of organic compounds should simultaneously contain nitryl groups, which may facilitate the production of plant-based sulfur compounds, as well as organoselenium moieties, which may influence the production of low molecular weight selenium metabolites. In the case of the new chemical compounds, environmental aspects should also be evaluated.


Brassica , Organoselenium Compounds , Selenium Compounds , Selenium , Humans , Selenium/metabolism , Brassica/chemistry , Sulfur Compounds/metabolism
9.
Molecules ; 28(4)2023 Feb 17.
Article En | MEDLINE | ID: mdl-36838911

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.


Brassica napus , Erucic Acids , Humans , Rats , Animals , Fatty Acids, Monounsaturated , Seeds
10.
Molecules ; 28(3)2023 Jan 18.
Article En | MEDLINE | ID: mdl-36770647

The genus Atriplex provides species that are used as food and natural remedies. In this work, the levels of soluble phenolic acids (free and conjugated) and flavonoids in extracts from roots, stems, leaves and flowers of the unexplored Atriplex sagittata Borkh were investigated by LC-ESI-MS/MS, together with their antioxidant and antihyaluronidase activity. Phenolic acids were present in all parts of A. sagittata; and were most abundant in the leaves (225.24 µg/g dw.), whereas the highest content of flavonoids were found in the flowers (242.71 µg/g dw.). The most common phenolics were 4-hydroxybenzoic and salicylic acids, kaempferol-3-glucoside-7-rhamnoside, kaempferol-3-rutinoside and the rare narcissoside, which was present in almost all morphotic parts. The stem extract had the highest antioxidant activity and total phenolic content (611.86 mg/100 g dw.), whereas flower extract exerted the most potent antihyaluronidase effect (IC50 = 84.67 µg/mL; control-quercetin: IC50 = 514.28 µg/mL). Phytochemical analysis of the flower extract led to the isolation of two triterpene saponins that were shown to be strong hyaluronidase inhibitors (IC50 = 33.77 and 168.15 µg/mL; control-escin: IC50 = 307.38 µg/mL). This is the first report on the presence of phenolics and saponins in A. sagittata. The results suggest that both groups of metabolites may contribute to the overall activity of this plant species.


Atriplex , Saponins , Antioxidants/chemistry , Kaempferols , Plant Extracts/chemistry , Saponins/pharmacology , Tandem Mass Spectrometry/methods , Hyaluronoglucosaminidase , Phenols/chemistry , Flavonoids/chemistry
11.
Molecules ; 28(2)2023 Jan 04.
Article En | MEDLINE | ID: mdl-36677535

Plants of the genus Pulicaria are known for providing traditional medicines, spices, herbal teas, and insect deterrents. Pulicaria inuloides (Poir.). DC. is one of the less chemically studied species within the genus. Hydroalcoholic extracts from roots and aerial parts of P. inuloides were analyzed using the UHPLC-PAD-MSn technique and revealed the presence of six caffeoylquinic and eleven caffeoylhexaric conjugates together with hydroxykaempferol dimethyl ether and quercetagetin trimethyl ether. Moreover, constituents of chloroform extract from the whole P. inuloides plants were isolated and identified by spectroscopic methods. One new and four known caryophyllene derivatives, three thymol derivatives, and four polymethoxylated flavonols were found in the analyzed extract. The structure of the new compound was established by spectroscopic methods (HRESIMS, 1H NMR, 13C NMR, COSY, HSQC, HMBC, NOESY). The cytotoxicity of 6-Hydroxykaempferol 3,7-dimethyl ether and quercetagetin 3,7,3'-trimethyl ether (chrysosplenol C), which are major flavonols isolated from the plant, were tested on prostate epithelial cells (PNT2), prostate cancer cells (DU145 and PC3), human keratinocytes (HaCaT), and melanoma cells (HTB140 and A375). Both flavonols demonstrated moderate cytotoxic activity against PC3 cells (IC50 = 59.5 µM and 46.6 µM, respectively). The remaining cell lines were less affected (IC50 > 150 µM).


Antineoplastic Agents , Methyl Ethers , Pulicaria , Humans , Flavonols/pharmacology , Pulicaria/chemistry , Plant Extracts/pharmacology , Plant Extracts/chemistry
12.
Plants (Basel) ; 12(2)2023 Jan 08.
Article En | MEDLINE | ID: mdl-36679006

Abiotic elicitation, a well-known strategy in mushroom biotechnology, promotes increased accumulation of secondary metabolites in mycelial cultures. The study aimed the effects of methyl jasmonate (MeJA) on the production of triterpenes in submerged cultures of Ganoderma applanatum. Further, the study evaluated the cytotoxic activity of the extract corresponding to the optimal elicitation variant in selected human cancer cell lines as well as the selectivity against normal cells. MeJA was added on days 1, 4, 6, and 8 in the 10-day growth cycle at concentrations of 10, 50, 100, 150, and 200 µM MeJA. The HPLC-DAD was used to analyze the triterpenes. The cytotoxic activity was tested using the MTTFc assay in grouped panels of skin, prostate, and gastrointestinal cancer cells. The results of the quantitative analyses confirmed the stimulating effect of MeJA on the production of ganoderic acid A and ganoderic acid C. The greatest increase in total triterpenes was found on day 6 of the culture cycle compared to the control group-with the concentration of MeJA-150 µM. Compared to the control samples, mycelial culture extract after the most productive elicitation variant showed significant cytotoxic activity against prostate cancer cells and moderate effects on melanoma cells. Ganoderma applanatum mycelial cultures can be proposed as a model to study the dynamics of the accumulation of compounds with therapeutic values through abiotic elicitation.

13.
Nat Prod Res ; 37(10): 1693-1697, 2023 May.
Article En | MEDLINE | ID: mdl-35876228

Cuphea ingrata is a traditional medicinal plant species of the Lythraceae family. This work reports on the cytotoxic activity of the methanolic extract from the aerial parts of C. ingrata and the n-butanol and ethyl acetate fractions against human skin and prostate cancer cells. The selectivity of action was tested in normal skin keratinocytes HaCaT and prostate epithelial cells PNT2. The ethyl acetate fraction showed the highest activity in all three human skin cancer cell lines: A375, HTB-140, WM793, with IC50 = 15.90; 3.40; 18.75 µg/mL, respectively. To obtain comparative information on the chemical composition, a quantitative analysis of oenothein B was performed using the UHPLC-PDA method. An analysis of its cytotoxic activity was also carried out.


Antineoplastic Agents , Cuphea , Plants, Medicinal , Male , Humans , Plant Extracts/pharmacology , Plant Extracts/chemistry , Cuphea/chemistry
14.
Molecules ; 27(24)2022 Dec 18.
Article En | MEDLINE | ID: mdl-36558162

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.


Cicer , Isoflavones , Lupinus , Isoflavones/pharmacology , Functional Food , Prostate
15.
Molecules ; 27(22)2022 Nov 16.
Article En | MEDLINE | ID: mdl-36432013

Rapanone is a plant-derived simple alkyl-dihydroxybenzoquinone structurally close to embelin, a well-known cytotoxic agent. The pharmacological characterization of rapanone is still incomplete, and to fill the data gap, a good source for its acquisition is required to conduct further research. This study aimed to optimize the conditions for the extraction of rapanone from the leaves of white-berried Ardisia crenata Sims. For this purpose, three methods were employed: heat reflux (HRE), shaking (SE), and ultrasound-assisted extraction (UAE), and such parameters as the extraction time, solvent, and the number of extractions from the same sample were set as experimental variables. Furthermore, cytotoxic activity toward prostate cancer, thyroid cancer, and colorectal carcinoma cell lines was investigated and compared with doxorubicin and embelin. The most effective and economical method for the extraction of rapanone was shown to be 20 min UAE with ethyl acetate or chloroform. Rapanone exhibited high cytotoxic activity against PC3 (IC50 = 6.50 µg/mL), Du145 (IC50 = 7.68 µg/mL), FTC133 (IC50 = 6.01 µg/mL), 8505C (IC50 = 7.84 µg/mL), and Caco-2 (IC50 = 8.79 µg/mL) cell lines after 24 h and against the HT29 cell line after 48 h (IC50 = 11.67 µg/mL). Furthermore, it revealed a more favorable safety profile than either its homologue, embelin, or doxorubicin. The set of optimal extraction parameters obtained may be utilized for scientific and industrial purposes to achieve the best rapanone yield. Moreover, this benzoquinone revealed a high cytotoxic activity with good selectivity.


Antineoplastic Agents , Benzoquinones , Male , Humans , Caco-2 Cells , Benzoquinones/pharmacology , Antineoplastic Agents/pharmacology , Doxorubicin
16.
Plants (Basel) ; 11(21)2022 Oct 23.
Article En | MEDLINE | ID: mdl-36365268

Carpesium divaricatum Sieb. & Zucc. is a plant species rich in terpenoids of anti-inflammatory and cytotoxic activity, especially germacranolides of potential medicinal value. The present study describes in vitro multiplication of C. divaricatum, analysis of active constituents in the multiple shoots, and assessment of cytotoxic activities of extracts prepared from in vitro- and field-grown plants. The plant extracts were evaluated for cytotoxicity using two melanoma cell lines (HTB140 and A375); human keratinocytes (HaCaT); two colon cancer cell lines (Caco2 and HT29); human hepatocellular carcinoma cells (HepG2); two lines of prostate cancer cells (DU145 and PC3) and prostate epithelial cells (PNT2). Chemical compositions of the assayed extracts were analyzed by HPLC/DAD, in reference to isolated compounds. Maximum of 4.07 ± 1.61 shoots regenerated from a nodal explant of C. divaricatum, cultivated in a liquid MS medium supplemented with thidiazuron (1 µM). In vitro grown shoots and plantlets of C. divaricatum accumulated terpenoids that are known as active constituents of the intact plant. Cytotoxic activity of the extracts prepared from the in vitro cultured plants was like that demonstrated by the extracts prepared from field-grown plants and seemed to be more selective than cytotoxicities of the individual germacranolides.

17.
Plants (Basel) ; 11(20)2022 Oct 18.
Article En | MEDLINE | ID: mdl-36297774

Broccoli sprouts are a super vegetable; however, they have possible negative effects on thyroid function, which is especially important for patients with hypothyroidism. As the data on this issue are scarce, this study aimed to determine the safety and possible beneficial effect of broccoli sprouts both in vitro and in vivo. The in vitro model comprised the evaluation of the impact of broccoli sprouts on normal and neoplastic thyroid cells and the determination of their anti-inflammatory and antioxidant (IL-6, TNF-alpha, NO, and SOD) potential in macrophages. The in vivo model concerned the histopathological analysis of thyroid glands in healthy rats and rats with hypothyroidism (induced by iodine deficiency or sulfadimethoxine ingestion) fed with broccoli sprouts. The results of our study indicated that broccoli sprouts decreased the viability of thyroid cancer cells and prevented inflammation. The results also confirmed the satisfactory safety profile of the sprouts, both in vitro and in vivo; however, a further in-depth evaluation of this problem is still needed. Information on the influence of brassica vegetables on thyroid function is of great importance in terms of public health, particularly when taking into account that the risk of iodine deficiency, hypothyroidism, and thyroid cancer in the global population is still increasing.

18.
Plants (Basel) ; 11(17)2022 Aug 26.
Article En | MEDLINE | ID: mdl-36079600

The dried Glechoma hederacea L. herb has a long history of use in traditional medicine. Its therapeutic potential is related to the presence of phenolic compounds. To optimize extraction efficiency the effect of the use of different techniques (HRE-heat reflux extraction, I/ME-infusion combined with maceration, UE-sonication and SE-Soxhlet extraction), various solvents (water and ethanol) and processing time (15 min to 2 h) on phenolics content was investigated. The HPLC method was applied to determine and compare the content of phenolic acids (rosmarinic, chlorogenic, protocatechuic) and flavonoids (rutin, isoquercetin) in the extracts. Furthermore, the cytotoxic activity of the extracts was examined for the first time against human cancer and normal cells of skin origin (A375, HTB140, HaCaT) and gastrointestinal origin (Caco-2 and HT-29, HepG2). In addition, the antioxidant potential was evaluated using the DPPH and FRAP method. The I/ME-water and HRE/ethanol procedures turned out to be optimal for obtaining extracts of dried G. hederacea L. herb rich in bioactive phenolics. These extracts exhibited high antioxidant activity, correlated with the content of the compounds analyzed. Furthermore, the extracts of the dried Glechoma herb were not toxic to normal human cells, indicating its safe use both internally and externally.

19.
Biomed Pharmacother ; 154: 113592, 2022 Oct.
Article En | MEDLINE | ID: mdl-36027609

In the current study, the fruits of a popular ornamental tree, Sorbus intermedia, were investigated phytochemically and biologically as potential source of bioactive triterpenes. Six terpenoids were isolated and examined with respect to their cytotoxic activity using a broad screening in vitro model and multivariate analysis for better demonstration of the effects on cancer cells. This chemometric approach allowed us to confirm that the structural characteristics of the compounds significantly affected their impact on cell lines. Ursolic acid was found to be the most potent cytotoxic agent with IC50 predominantly < 10 µg/mL after 24 h of incubation. Its 3-acetoxy derivative was less active, however, an improvement in selectivity with regard to prostate panel was observed. Reduction of the carboxylic moiety at C28, as well as introduction of the hydroxyl group at 19α position led to complete loss of cytotoxic activity.


Antineoplastic Agents , Sorbus , Triterpenes , Fruit/chemistry , Molecular Structure , Oleanolic Acid/analogs & derivatives , Sorbus/chemistry , Triterpenes/chemistry , Triterpenes/pharmacology , Ursolic Acid
20.
Nutrients ; 14(14)2022 Jul 08.
Article En | MEDLINE | ID: mdl-35889759

Brassica sprouts, as the rich source of dietary glucosinolates, may have a negative effect on thyroid function. In this study, kohlrabi sprouts diet, combined with two models of rat hypothyroidism, was tested. TSH, thyroid hormones and histopathology analysis were completed with the evaluation of immunological, biochemical, haematological parameters, cytosolic glutathione peroxidase, thioredoxin reductase in the thyroid, and plasma glutathione peroxidase. A thermographic analysis was also adapted to confirm thyroid dysfunction. The levels of TSH, fT3 and fT4, antioxidant enzyme (GPX) as well as histopathology parameters remained unchanged following kohlrabi sprouts ingestion, only TR activity significantly increased in response to the sprouts. In hypothyroid animals, sprouts diet did not prevent thyroid damage. In comparison with the rats with iodine deficiency, kohlrabi sprouts diet decreased TNF-α level. Neither addition of the sprouts to the diet, nor sulfadimethoxine and iodine deficiency, caused negative changes in red blood cell parameters, glucose and uric acid concentrations, or kidney function. However, such a dietary intervention resulted in reduced WBC levels, and adversely interfered with liver function in rats, most likely due to a higher dietary intake of glucosinolates. Moreover, the possible impact of the breed of the rats on the evaluated parameters was indicated.


Brassica , Hypothyroidism , Iodine , Malnutrition , Thyroid Gland , Animals , Glucosinolates , Iodine/deficiency , Malnutrition/complications , Rats , Sulfadimethoxine , Thyroid Gland/physiopathology , Thyrotropin , Thyroxine
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