Poncirus trifoliata (L.) Raf. Seed Extract Induces Cell Cycle Arrest and Apoptosis in the Androgen Receptor Positive LNCaP Prostate Cancer Cells.

Prostate cancer (PCa) is the second most common male cancer. Its incidence derives from the interaction between modifiable and non-modifiable factors. The progression of prostate cancer into a more aggressive phenotype is associated with chronic inflammation and increased ROS production. For their biological properties, some phytochemicals from fruits and vegetable emerge as a promise strategy for cancer progression delay. These bioactive compounds are found in the highest amounts in peels and seeds. Poncirus trifoliata (L.) Raf. (PT) has been widely used in traditional medicine and retains anti-inflammatory, anti-bacterial, and anticancer effects. The seeds of P. trifoliata were exhaustively extracted by maceration with methanol as the solvent. The cell proliferation rate was performed by MTT and flow cytometry, while the apoptosis signals were analyzed by Western blotting and TUNEL assay. P. trifoliata seed extract reduced LNCaP and PC3 cell viability and induced cell cycle arrest at the G0/G1phase and apoptosis. In addition, a reduction in the AKT/mTOR pathway has been observed together with the up-regulation of stress-activated MAPK (p38 and c-Jun N-terminal kinase). Based on the study, the anti-growth effects of PT seed extract on prostate tumor cells give indications on the potential of the phytochemical drug for the treatment of this type of cancer. However, future in-depth studies are necessary to identify which components are mainly responsible for the anti-neoplastic response.

Lavandula angustifolia mill. (Lamiaceae) ethanol extract and its main constituents as promising agents for the treatment of metabolic disorders: chemical profile, in vitro biological studies, and molecular docking.

Lavandula angustifolia Mill. (lavender) is one of the most used medicinal plants. Herein, we chemically characterised and investigated the antioxidant properties and the capability to inhibit key enzymes for the treatment of type 2 diabetes (TD2) and obesity such as pancreatic lipase, α-glucosidase, and α-amylase of the ethanolic extract of two lavender samples (La1 and La2) from southern Italy. Both extracts significantly inhibited α-glucosidase, while La1 inhibited α-amylase and lipase more effectively than La2. To investigate whether these properties could be due to a direct interaction of the main constituents of the extracts with the targeted enzymes, molecular docking studies have been performed. As a result, the selected compounds were able to interact with the key residues of the binding site of the three proteins, thus supporting biological data. Current findings indicate the new potential of lavender ethanolic extract for the development of novel agents for T2D and obesity.

Iridoid- and flavonoid-enriched fractions of Cornus sanguinea and Cornus mas exert antioxidant and anti-inflammatory effects and inhibit key enzymes in the treatment of metabolic disorders.

Background: Berry fruits are recognized as a "superfood" due to their high content of bioactive compounds and health benefits. Scope and approach: Herein, extracts of Cornus sanguinea and Cornus mas fresh and dried fruits obtained by different extraction procedures (ethanolic and hydroalcoholic maceration, ultrasound-assisted extraction, and Soxhlet apparatus) were analysed using liquid chromatography-electrospray ionization-quadrupole-time of flight-mass spectrometry (LC-ESI-QTOF-MS) and compared to identify the main healthy compounds and their impact on the inhibition of key enzymes (pancreatic lipase, α-glucosidase, and α-amylase) associated with metabolic disorders. The antioxidant activity and inhibition of nitric oxide (NO) and NF-κB pathway were also investigated. Key findings and conclusions: Flavonoids, iridoids, and phenolic acids were the main classes of identified compounds. Herein, kaempferol 3-O-galactoside, kaempferol 3-O-glucoside, quercetin, quercetin 3-O-xyloside, and myricetin 3-O-galactoside were detected for the first time in C. sanguinea. Remarkable antioxidant effects and promising α-glucosidase and lipase inhibitory activity were observed with extracts obtained by hydroalcoholic maceration of both Cornus dried fruits. Consequently, these extracts were subjected to fractionation using Amberlite XAD-16 resin. The most promising biological activities, which are attributed to the presence of some flavonoids and iridoids, were detected with the C. sanguinea fractions, in particular SD2(II). The results of this study offer new insights into the potential development of functional foods, nutraceuticals, and food supplements using the Cornus species.

Biological Investigation and Chemical Study of Brassica villosa subsp. drepanensis (Brassicaeae) Leaves.

Brassica villosa subsp. drepanensis (Caruel) Raimondo & Mazzola, belonging to the Brassica oleracea complex, is a wild edible plant endemic to western Sicily and a relative of modern cultivated Brassica crops. In this study, the antioxidant properties, anti-inflammatory activities, enzymatic inhibition, and cytotoxicity in cancer cells of B. villosa subsp. drepanensis leaf ethanolic extract were analysed for the first time. In addition, its chemical profile was investigated partitioning the total 70% ethanol extract among ethyl acetate, n-butanol, and water to obtain three residues that were subjected to chromatographic separation. Two flavonol glycosides, a phenol glucoside, two amino acids, and purine/pyrimidine bases were obtained. The presence of the glucosinolate glucoiberin was detected in the water extract by UHPLC-MS analysis. The total polyphenol and flavonoid content of the 70% ethanol extract showed good antioxidant capacities and anti-inflammatory properties by reducing nitric oxide release and reactive oxygen species levels and increasing glutathione in lipopolysaccharide-stimulated RAW 264.7 cells. The extract inhibited the enzymatic activity of α-amylase, α-glucosidase, and, significantly, of lipase. The MTT assay showed that the extract did not affect the viability of normal HFF-1 and RAW 264.7 cells. Among the cancer cell lines tested, an antiproliferative action was only observed in CaCo-2. The cytotoxicity of the extract was further confirmed by LDH release assay and by the destabilization of the oxidative balance. Results confirmed the antioxidant properties of the crude extract responsible for the anti-inflammatory effect on healthy cells and cytotoxicity in cancer cells.

Production of High-Quality Red Fruit Juices by Athermal Membrane Processes.

Membrane-based processes are increasingly used to clarify and concentrate thermo-sensitive fruit juices and plant extracts as alternatives to conventional processes. This work aimed to evaluate the quality of red fruit juices clarified and concentrated by an integrated membrane process with special regard to the preservation of valuable compounds. A red fruit juice obtained from a blend of pomegranate, cactus pear, and red orange juices of Sicilian origin was clarified by microfiltration (MF) and then pre-concentrated up to 33 °Brix by nanofiltration (NF). The pre-concentrated juice was finally concentrated by osmotic distillation (OD) up to 50 and 60 °Brix. Samples of clarified, pre-concentrated, and concentrated juice were analyzed for their physico-chemical composition and in terms of the antioxidant activity and inhibitory activity against α-amylase and lipase. The results clearly confirmed the assumption of a mild fruit juice processing method, allowing us to preserve the original nutritional and functional properties of the fresh juice. In particular, the OD retentate at 60 °Brix resulted the most active sample against pancreatic lipase and α-amylase inhibitory activity with IC50 values of 44.36 and 214.65 µg/mL, respectively.

Santolina pinnata Viv. Exerts Promising Antitumor Activity against Breast Cancer Cells and Anti-Inflammatory Effects in LPS-Stimulated RAW 264.7 Cells.

Cancer is one of the largest causes of mortality in the world, and due to its incidence, the discovery of novel anticancer drugs is of great importance. Many successful anticancer drugs used in clinical practices are derived from natural products. The genus Santolina is a group of species distributed in the Mediterranean area and used in traditional medicine for their biological properties. The aim of this work was to investigate, for the first time, the multi-target biological potential of Italian Santolina pinnata in relation to their chemical profile, by which an interesting natural source of valuable phytochemicals endowed with anticancer and anti-inflammatory features could be assessed. n-Hexane (EHSP) and methanol (EMSP) extracts were investigated by gas chromatography (GC) and gas chromatography-mass spectrometry (GC-MS) and ultra-high-performance liquid chromatography (UHPLC), respectively. Anti-proliferative activity was analyzed on MCF-7 and MDA-MB-231 breast cancer cells, as well as on non-tumorigenic MCF-10A cells, by the 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyl-2H-tetrazolium bromide (MTT) assay. Apoptotic death was assessed by comet assay. Cell motility and invasive features were examined in highly invasive MDA-MB-231 by wound-healing scratches, while, in both breast cancer cell lines, by gel-zymography experiments. The anti-inflammatory potential was analyzed by nitric oxide (NO) production and the nuclear factor kappa-light-chain-enhancer of activated B cells (NF-κB) staining experiments in bacterial lipopolysaccharides (LPS) which stimulated RAW 264.7 cells. EHSP and EMSP extracts exhibited anticancer activity against breast cancer cells, promoting apoptotic death, as well as decreasing cell migration and invasive behaviours. The highest activity (IC50 of 15.91 µg/mL) was detected against MDA-MB-231 cells, a highly invasive breast cancer cell line. Both extracts were also able to promote anti-inflammatory effects (IC50 values ranging from 27.5 to 61.14 µg/mL), as well as to reduce NO levels by inducing inhibitory effects on NF-κB nuclear translocation in LPS-stimulated RAW 264.7 cells. The different biological behaviours found between the extracts could be related to their different chemical compositions. Herein, the multi-target biological potential of S. pinnata in inducing antitumor and anti-inflammatory effects was comprehensively demonstrated. These findings will provide important stepping-stones for further investigations and may lead to the development of highly effective S. pinnata extract-based treatments for breast cancer and inflammatory processes.

The potential of pumpkin seed oil as a functional food-A comprehensive review of chemical composition, health benefits, and safety.

The growing interest in foods that can be beneficial to human health is bringing into focus some products that have been used locally for centuries but have recently gained worldwide attention. One of these foods is pumpkin seed oil, which has been used in culinary and traditional medicine, but recent data also show its use in the pharmaceutical and cosmetic industries. In addition, some sources refer to it as a potential functional food, mainly because it is obtained from pumpkin seeds, which contain many functional components. However, the production process of the oil may affect the content of these components and consequently the biological activity of the oil. In this review, we have focused on summarizing scientific data that explore the potential of pumpkin seed oil as a functional food ingredient. We provide a comprehensive overview of pumpkin seed oil chemical composition, phytochemical content, biological activity, and safety, as well as the overview of production processes and contemporary use. The main phytochemicals in pumpkin seed oil with health-related properties are polyphenols, phytoestrogens, and fatty acids, but carotenoids, squalene, tocopherols, and minerals may also contribute to health benefits. Most studies have been conducted in vitro and support the claim that pumpkin seed oil has antioxidant and antimicrobial activities. Clinical studies have shown that pumpkin seed oil may be beneficial in the treatment of cardiovascular problems of menopausal women and ailments associated with imbalance of sex hormones.

An Overview of Traditional Uses, Phytochemical Compositions and Biological Activities of Edible Fruits of European and Asian Cornus Species.

Cornus species are widely distributed in central and southern Europe, east Africa, southwest Asia, and America. Several species are known for edible fruits, especially Cornus mas and Cornus officinalis. These delicious fruits, characterized by their remarkable nutritional and biological values, are widely used in traditional medicine. In contrast to the other edible Cornus species, C. mas and C. officinalis are the most studied for which little information is available on the main phytochemicals and their biological activities. Fruits are characterised by several classes of secondary metabolites, such as flavonoids, phenolic acids, lignans, anthocyanins, tannins, triterpenoids, and iridoids. The available phytochemical data show that the different classes of metabolites have not been systematically studied. However, these edible species are all worthy of interest because similarities have been found. Thus, this review describes the traditional uses of Cornus species common in Europe and Asia, a detailed classification of the bioactive compounds that characterize the fruits, and their beneficial health effects. Cornus species are a rich source of phytochemicals with nutritional and functional properties that justify the growing interest in these berries, not only for applications in the food industry but also useful for their medicinal properties.

Mechanistic aspects of carotenoid health benefits - where are we now?

Dietary intake and tissue levels of carotenoids have been associated with a reduced risk of several chronic diseases, including cardiovascular diseases, type 2 diabetes, obesity, brain-related diseases and some types of cancer. However, intervention trials with isolated carotenoid supplements have mostly failed to confirm the postulated health benefits. It has thereby been speculated that dosing, matrix and synergistic effects, as well as underlying health and the individual nutritional status plus genetic background do play a role. It appears that our knowledge on carotenoid-mediated health benefits may still be incomplete, as the underlying mechanisms of action are poorly understood in relation to human relevance. Antioxidant mechanisms - direct or via transcription factors such as NRF2 and NF-κB - and activation of nuclear hormone receptor pathways such as of RAR, RXR or also PPARs, via carotenoid metabolites, are the basic principles which we try to connect with carotenoid-transmitted health benefits as exemplified with described common diseases including obesity/diabetes and cancer. Depending on the targeted diseases, single or multiple mechanisms of actions may play a role. In this review and position paper, we try to highlight our present knowledge on carotenoid metabolism and mechanisms translatable into health benefits related to several chronic diseases.

Systematics, Phytochemistry, Biological Activities and Health Promoting Effects of the Plants from the Subfamily Bombacoideae (Family Malvaceae).

Plants belonging to the subfamily Bombacoideae (family Malvaceae) consist of about 304 species, many of them having high economical and medicinal properties. In the past, this plant group was put under Bombacaceae; however, modern molecular and phytochemical findings supported the group as a subfamily of Malvaceae. A detailed search on the number of publications related to the Bombacoideae subfamily was carried out in databases like PubMed and Science Direct using various keywords. Most of the plants in the group are perennial tall trees usually with swollen tree trunks, brightly colored flowers, and large branches. Various plant parts ranging from leaves to seeds to stems of several species are also used as food and fibers in many countries. Members of Bombacoides are used as ornamentals and economic utilities, various plants are used in traditional medication systems for their anti-inflammatory, astringent, stimulant, antipyretic, microbial, analgesic, and diuretic effects. Several phytochemicals, both polar and non-polar compounds, have been detected in this plant group supporting evidence of their medicinal and nutritional uses. The present review provides comprehensive taxonomic, ethno-pharmacological, economic, food and phytochemical properties of the subfamily Bombacoideae.

LC-ESI/HRMS analysis of glucosinolates, oxylipins and phenols in Italian rocket salad (Diplotaxis erucoides subsp. erucoides (L.) DC.) and evaluation of its healthy potential.

BACKGROUND: This study investigated the chemical profile and biological activity of Diplotaxis erucoides subsp. erucoides (L.) DC. (Brassicaceae) collected in Sicily (Italy). RESULTS: Liquid chromatography coupled with electrospray ionization and high-resolution mass spectrometry (LC-ESI/HRMS) analysis of the ethanol extract revealed the presence of 42 compounds - glucosinolates, hydroxycinnamic acids, flavonoids, and oxylipins. The extract was tested for its antioxidant activity using 2,2-diphenyl-1-picrylhydrazyl (DPPH), 2,2'-azinobis(3-ethylbenzothiazoline-6-sulfonic) acid (ABTS), ferric reducing ability power (FRAP), and ß-carotene bleaching tests. Promising protection from lipid peroxidation was observed after 30 min of incubation in a ß-carotene bleaching test (IC50 of 3.32 µg mL-1 ). The inhibition of carbohydrates-hydrolyzing enzymes resulted in IC50 values of 85.18 and 92.36 µg mL-1 for α-amylase and α-glucosidase, respectively. Significant inhibition against lipase enzyme was observed (IC50 of 61.27 µg mL-1 ). CONCLUSION: Diplotaxis erucoides can be considered a potential source of antioxidant, hypoglycemic, and hypolipidemic bioactives. © 2021 Society of Chemical Industry.

In vitro and in vivo studies of Cucurbita pepo L. flowers: chemical profile and bioactivity.

Edible flowers consumption has increased in recent years due to their rich content of healthy phytochemicals. The aim of this study was to analyse the chemical profile of Cucurbita pepo L. flowers, and to explore their antioxidant and hypoglycaemic properties. Moreover, in order to assess in vivo effects, biochemical analysis, Reactive Oxygen Metabolites (d-ROMs) and Biological Antioxidant Potential (BAP) tests were performed on mice serum. High Performance Liquid Chromatography-Diode Array Detection (HPLC-DAD) analyses revealed the presence of (+)-catechin, (-)-epicatechin, rutin, and syringic acid as main constituents. 2,2'-Azino-bis (3-ethylbenzothiazoline-6-sulphonic acid) (ABTS) and Ferric Reducing Antioxidant Power (FRAP) tests showed interesting results. The extract exhibited the strongest inhibitory effect on α-glucosidase (IC50 of 144.77 µg/mL). In vivo results confirmed the hypoglycaemic effects, also affecting lipid metabolism but did not revealed benefits on ROS production. These results may add some information supporting the use of C. pepo flowers as functional foods and/or nutraceuticals.

In vitro anti-proliferative and anti-bacterial properties of new C7 benzoate derivatives of pinocembrin.

In the present work, the in vitro anti-proliferative and anti-bacterial activities of three semi-synthetic benzoate pinocembrin derivatives, isolated from the aerial parts of Glycyrrhiza glabra L., were investigated. As occurs in most natural compounds, the bioavailability of pinocembrin is very poor, therefore it should be improved by chemical strategies aimed to prolong its shelf life and, consequently, its activity. On this basis, three benzoate derivatives of pinocembrin (a1-a3) were synthesised and assayed in order to ascertain their biological value. Among them, compound a1 showed the highest anti-proliferative activity on a wide panel of cancer cell lines, as well as low toxic effects on non-malignant breast cells. The calculated IC50 values in HeLa and SKBR3 cells were 8.5 and 12.7 µM, respectively. Briefly, a1 treatment increased ROS levels, induced mitochondrial membrane damage leading to necrotic death of HeLa cells. Moreover, a1 displayed a promising anti-bacterial activity.

Salvia officinalis L. from Italy: A Comparative Chemical and Biological Study of Its Essential Oil in the Mediterranean Context.

Salvia officinalis L. (sage) is one of the most appreciated plants for its plethora of biologically active compounds. The objective of our research was a comparative study, in the Mediterranean context, of chemical composition, anticholinesterases, and antioxidant properties of essential oils (EOs) from sage collected in three areas (S1-S3) of Southern Italy. EOs were extracted by hydrodistillation and analyzed by gas chromatography (GC) and gas chromatography-mass spectrometry (GC-MS). Acetylcholinesterase (AChE) and butyrylcholinesterase (BChE) inhibitory properties were investigated by employing Ellman's method. Four in vitro assays, namely, 2,2-diphenyl-1-picrylhydrazyl (DPPH), 2,2'-azino-bis(3-ethylbenzothiazoline-6-sulfonic acid) (ABTS), ferric-reducing ability power (FRAP), and ß-carotene bleaching tests, were used to study the antioxidant effects. Camphor (16.16-18.92%), 1,8-cineole (8.80-9.86%), ß-pinene (3.08-9.14%), camphene (6.27-8.08%), and α-thujone (1.17-9.26%) are identified as the most abundant constituents. However, the content of these constituents varied depending on environmental factors and pedoclimatic conditions. Principal component analysis (PCA) was performed. Based on Relative Antioxidant Capacity Index (RACI), S2 essential oil exhibited the highest radical potential with an IC50 value of 20.64 µg/mL in ABTS test and presented the highest protection of lipid peroxidation with IC50 values of 38.06 and 46.32 µg/mL after 30 and 60 min of incubation, respectively. The most promising inhibitory activity against BChE was found for S3 sample (IC50 of 33.13 µg/mL).

Ceiba speciosa (A. St.-Hil.) Seeds Oil: Fatty Acids Profiling by GC-MS and NMR and Bioactivity.

This study aimed to evaluate the chemical composition by gas chromatography-mass spectrometry (GC-MS) and Nuclear Magnetic Resonance (NMR) analyses, the antioxidant activities evaluated by different in vitro assays namely 2,2-diphenyl-1-picrylhydrazyl (DPPH), 2,2'-azino-bis(3-ethylbenzothiazoline-6-sulphonic acid) (ABTS), Ferric Reducing Ability Power (FRAP), and ß-carotene bleaching tests, and the inhibitory effects of enzymes linked to obesity (lipase, α-amylase, and α-glucosidase) of fixed seed oil of Ceiba speciosa (A. St.-Hil.). Fourteen compounds were identified. Linoleic acid (28.22%) was the most abundant followed by palmitic acid (19.56%). Malvalic acid (16.15%), sterculic acid (11.11%), and dihydrosterculic acid (2.74%) were also detected. C. speciosa fixed oil exerted a promising ABTS radicals scavenging activity with an IC50 value of 10.21 µg/mL, whereas an IC50 of 77.44 µg/mL against DPPH+ radicals was found. C. speciosa fixed oil inhibited lipase with an IC50 value of 127.57 µg/mL. The present investigation confirmed the functional properties of C. speciosa fixed oil, and proposes its use as valuable source of bioactive constituents.

The Role of Anthocyanins in Drug Discovery: Recent Developments.

Natural compounds have always played a key role in drug discovery. Anthocyanins are secondary metabolites belonging to the flavonoids family responsible for the purple, blue, and red colour of many vegetables and fruits. These phytochemicals have attracted the interest of researchers for their important implications in human health and for their use as natural colorants. Many in vitro and in vivo studies demonstrated the potential effects of anthocyanins and anthocyanins-rich foods in the prevention and/or treatment of diabetes, cancer, and cardiovascular and neurodegenerative diseases. This review reports the recent literature data and focuses on the potential role of anthocyanins in drug discovery. Their biological activity, analysis of structure-activity relationships, bioavailability, metabolism, and future prospects of their uses are critically described.

High-Performance Liquid Chromatography/Electrospray Ionization Tandem Mass Spectrometry (HPLC-ESI-MSn) Analysis and Bioactivity Useful for Prevention of "Diabesity" of Allium commutatum Guss.

This study aimed at evaluating and comparing the chemical profile obtained by HPLC-ESI-MSn analysis, the inhibitory activity of enzymes linked to obesity (α-amylase, α-glucosidase, and lipase) and the antioxidant properties (DPPH, ABTS, FRAP, and ß-carotene bleaching tests) of ethanol extracts of bulbs (BE) and aerial parts (APE) from Allium commutatum Guss. (known in Italy as "aglio delle isole"). The chemical profile revealed alliin as the main abundant compound with values of 31.5 and 38.8 mg/g extract for BE and APE, respectively. APE is rich also in quercetin (38.5 mg/g extract) and luteolin (31.8 mg/g extract). Bulbs extract exhibited the highest activity as inhibitor of enzymes linked to obesity. Except for DPPH test, APE showed the highest antioxidant potential with IC50 of 7.6 and 56.6 µg/mL in ABTS and ß-carotene bleaching test after 60 min of incubation, respectively. In conclusion, the present investigation revealed A. commutatum bulbs and aerial parts as a promising source of inhibitors of enzyme linked to the obesity and of antioxidant compounds.

Impact of extraction processes on phytochemicals content and biological activity of Citrus × clementina Hort. Ex Tan. leaves: New opportunity for under-utilized food by-products.

Plants are a rich source of natural bioactive compounds with a wide range of applications in the food and pharmaceutical industries. Citrus × clementina leaves extracts and essential oils may be a potential candidate for formulation of products characterized by hypoglycaemic, antioxidant and anti-browning properties. C. × clementina leaves collected in three different areas in Calabria (South Italy) were extracted by Soxhlet apparatus, maceration, Ultrasound assisted maceration, and hydrodistillation. Hesperidin, tangeritin, and sinensetin were identified by HPLC-DAD analysis as dominant constituents of the extracts. The absence of coumarins and furanocoumarins was demonstrated. GC-MS analyses of essential oils evidenced the presence of sabinene, linalool, and (E)-ß-ocimene as main compounds. Based on RACI and GAS values calculated by the integration of data obtained by DPPH, ABTS, FRAP and ß-carotene bleaching methods, hydroalcoholic extract obtained by Ultrasound assisted maceration of the leaves collected in Corigliano Calabro showed the highest antioxidant activity. Ultrasound assisted hydroalcoholic extract of Cetraro leaves revealed the highest α-amylase inhibitory activity (IC50 of 64.37 µg/ml). Promising results of C. × clementina extracts as tyrosinase inhibitors were also obtained. To evaluate the relationship between identified compounds and bioactivity PCA was performed. Taking into account results obtained by this study, C. × clementina leaves that were considered Citrus-by-products could be utilized for formulation of food additives, nutraceuticals and functional foods.

Gamma Irradiated Rhodiola sachalinensis Extract Ameliorates Testosterone-Induced Benign Prostatic Hyperplasia by Downregulating 5-Alpha Reductase and Restoring Testosterone in Rats.

The effect of Rhodiola sachalinensis Boriss extract irradiated with 50 kGy gamma rays (HKC) on benign prostatic hyperplasia (BPH) was investigated. Seven-week-old male SD rats received a subcutaneous injection of 20 mg/kg of testosterone propionate (TP) to induce BPH. Then, the testosterone only group received testosterone, the testosterone + finasteride group received testosterone and finasteride (5 mg/kg), the testosterone + HKC group received testosterone and HKC extract (500 mg/kg). Prostate weight and the dihydrotestosterone (DHT) levels in serum or prostate tissue were determined. The mRNA expressions of 5-alpha reductase (AR) in prostate tissue were also measured. Compared to the control group, prostate weight was significantly improved in the TP group and decreased in the HKC and finasteride-treated groups. Furthermore, the mRNA expression of 5-AR in the prostate was significantly reduced in the HKC and finasteride-treated groups. Similarly, the expression levels of α-smooth muscle actin (α-SMA) and cytokeratin, which are associated with prostatic enlargement in the HKC and finasteride groups, were much lower than in the TP group. HKC treatment showed similar efficacy to finasteride treatment on rats with testosterone-induced BPH. HKC may be explored as a potential new drug for BPH treatment.

Anchusa azurea Mill. (Boraginaceae) aerial parts methanol extract interfering with cytoskeleton organization induces programmed cancer cells death.

The present study aimed to determine the chemical composition, antioxidant effects and antitumor properties of a methanol extract of Anchusa azurea Mill. (Boraginaceae) aerial parts against four tumour cell lines (MCF-7, MDA-MB-231, RKO, and R2C). The antioxidant effects were assessed by using ß-carotene bleaching, 2,2'-azinobis(3-ethylbenzothiazoline-6-sulfonic acid) (ABTS), 2,2-diphenyl-1-picrylhydrazyl (DPPH), and ferric reducing ability power (FRAP) tests. HPLC analyses revealed chlorogenic acid, catechin, caffeic acid, and astragalin as the most abundant compounds. Interesting results were obtained in the ß-carotene bleaching test with IC50 values of 7.6 and 27.5 µg mL-1 after 30 and 60 min of incubation, respectively. Furthermore, the A. azurea extract protects 3T3-L1 mouse cells from oxidative stress induced by menadione and exhibits good antitumor activity, with very low toxicity. Our data indicate that the antitumor properties are due to the ability to induce programmed cancer cell death through caspase 3/7 and 9 activation and interference with the cytoskeleton dynamics.