Polyphenolic profile and antioxidant properties of Momordica charantia L. 'Enaja' cultivar grown in Romania.

This is the first study describing phenolics of Momordica charantia L. 'Enaja' cultivar (bitter melon) produced in Romania. Total polyphenol content, total tannin content, total flavonoid content, and antioxidant activity of bitter melon stems and leaves, young fruits, and ripe fruits grown in Romania were analysed, along with fruits imported from India. The UPLC-DAD analysis led to the identification of (+)-catechin, (-)-epicatechin, luteolin-3',7-di-O-glucoside, luteolin-7-O-glucoside and vanillic acid. (-)-Epicatechin (859 µg/g) and (+)-catechin (1677 µg/g) were the most abundant compounds in stems and leaves, while in the ripe fruits, luteolin-7-O-glucoside (310 µg/g) was the main phenolic. Stems and leaves were the most active for capturing free DPPH radicals (IC50 = 216.9 ± 11.91 µg/ml); the scavenging activity strongly correlated with the flavonoid content (r = 0.8806, r2 = 0.7754). Momordica charantia fruits from Romania, both young and ripe, are a source of polyphenols as valuable as those imported from India.

Fennel Essential Oil as a Complementary Therapy in the Management of Diabetes.

Diabetes is a serious pathology that affects a significant number of people worldwide. Its progression is rapid and leads to serious complications if glycemic control is missing. The micro and macrovascular complications of diabetes produce disabilities over time that affect the daily lives of patients. The major challenge of diabetes therapy is to reach a stable glycemic state and to delay the onset of specific complications. Aromatherapy is considered an alternative or complementary therapy, but in recent years, there has been a tendency to overuse essential oils. The present study was designed to evaluate and compare the effects produced by the topical and oral administration of fennel essential oil to diabetic rats. Eighteen compounds in fennel essential oil were identified by gas chromatography-mass spectrometry (GC-MS) analysis. The major compounds were trans-anethole (64.6%) and fenchone (24.5%). The in vivo study revealed that after a four-week treatment with fennel essential oil, the rats' glycemic levels were significantly reduced (p ≤ 0.05). Furthermore, there were no differences between the two routes of administration. In addition, an ex vivo study underlined the potential effect of this essential oil in the prevention of cataract formation.

Isolation of compounds from the roots of Ambrosia artemisiifolia and their effects on human cancer cell lines.

Common ragweed (Ambrosia artemisiifolia L.) is an invasive plant in Europe with spreading use in the contemporary folk medicine. The chemical composition of the above-ground parts is extensively studied, however, the metabolites of the roots are less discovered. By multiple chromatographic purification of the root extracts, we isolated thiophene A (1), n-dodecene (2), taraxerol-3-O-acetate (3), α-linoleic acid (4), (+)-pinoresinol (5), and thiophene E (7,10-epithio-7,9-tridecadiene-3,5,11-triyne-1,2-diol) (6). The 1H NMR data published earlier for 1 were supplemented together with the assignment of 13C NMR data. Thiophene E (6), which is reported for the first time from this species, exerted cytotoxic and antiproliferative effects on A-431 epidermoid skin cancer cells, whereas taraxerol-3-O-acetate (3) and α-linoleic acid (4) had slight antiproliferative effect on gynecological cancer cell lines. Thiophene E (6) and taraxerol-3-O-acetate (3) displayed antiproliferative and cytotoxic effects on MRC-5 fibroblast cells. Thiophene E (6) exerted weak antibacterial activity (MIC 25 µg/mL) on MRSA ATCC 43300, on Staphylococcus aureus ATCC 25923, Escherichia coli AG100 and E. coli ATCC 25922 both thiophenes were inactive. Although the isolated compounds exerted no remarkable cytotoxic or antiproliferative activities, the effects on MRC-5 fibroblast cells highlight the necessity of further studies to support the safety of ragweed root.

The metabolic effect of Momordica charantia cannot be determined based on the available clinical evidence: a systematic review and meta-analysis of randomized clinical trials.

Several studies have shown that Momordica charantia L. (Cucurbitaceae, bitter melon) has beneficial effects on metabolic syndrome (MetS) parameters and exerts antidiabetic, anti-hyperlipidemic, and anti-obesity activities. Since the findings of these studies are contradictory, the goal of this systematic review and meta-analysis was to assess the efficacy of bitter melon in the treatment of metabolic syndrome, with special emphasis on the anti-diabetic effect. Embase, Cochrane, PubMed, and Web of Science databases were searched for randomized controlled human trials (RCTs). The meta-analysis was reported according to the PRISMA statement. The primary outcomes of the review are body weight, BMI, fasting blood glucose, glycated hemoglobin A1c, systolic blood pressure, diastolic blood pressure, serum triglyceride, HDL, LDL, and total cholesterol levels. Nine studies were included in the meta-analysis with 414 patients in total and 4-16 weeks of follow-up. In case of the meta-analysis of change scores, no significant effect could be observed for bitter melon treatment over placebo on fasting blood glucose level (MD = -0.03; 95% CI: -0.38 to 0.31; I2 = 34%), HbA1c level (MD = -0.12; 95% CI: -0.35 to 0.11; I2 = 56%), HDL (MD = -0.04; 95% CI: -0.17 to 0.09; I2 = 66%), LDL (MD = -0.10; 95% CI: -0.28 to 0.08; I2 = 37%), total cholesterol (MD = -0.04; 95% CI: -0.17 to 0.09; I2 = 66%,), body weight (MD = -1.00; 95% CI: -2.59-0.59; I2 = 97%), BMI (MD = -0.42; 95% CI: -0.99-0.14; I2 = 95%), systolic blood pressure (MD = 1.01; 95% CI: -1.07-3.09; I2 = 0%) and diastolic blood pressure levels (MD = 0.24; 95% CI: -1.04-1.53; I2 = 0%). Momordica treatment was not associated with a notable change in ALT, AST, and creatinine levels compared to the placebo, which supports the safety of this plant. However, the power was overall low and the meta-analyzed studies were also too short to reliably detect long-term metabolic effects. This highlights the need for additional research into this plant in carefully planned clinical trials of longer duration.

An Updated Systematic Review of Vaccinium myrtillus Leaves: Phytochemistry and Pharmacology.

Bilberry leaves are used in many countries in traditional medicine for treating a wide variety of diseases. Due to the high therapeutic potential of Vaccinium myrtillus (VM) leaves, this review aims to present the latest knowledge on the phytochemical profile, as well as the therapeutic effects of this herbal drug. The review was conducted according to the Prisma guidelines, and the scientific databases were searched using combinations of the following keywords: "Vaccinium myrtillus", "leaves", "bilberry". Recent research was focused on the influence of abiotic factors on the phytochemical composition, and it seems that there are significant differences between the herbal drugs collected from different countries. The phytochemical composition is correlated with the broad spectrum of pharmacological effects. The paper outlines the potent antimicrobial activity of VM extracts against multidrug-resistant bacterial strains, and also the pathways that are modulated by the unique "cocktail" of phytoconstituents in different metabolic alterations. Reviewing the research articles published in the last 10 years, it seems that bilberry leaves have been slightly forgotten, although their phytochemical and pharmacological characteristics are unique.

Effects of alpha-lipoic acid treatment on serum progranulin levels and inflammatory markers in diabetic neuropathy.

OBJECTIVES: Progranulin (PGRN) is a secreted growth factor that helps to regulate neuronal survival by blocking tumor necrosis factor-alpha (TNFα) receptors. The antioxidant alpha-lipoic acid (ALA) is used in diabetic neuropathy to improve nerve conduction and relieve neuropathic pain, but its effects on PGRN levels have not yet been elucidated. METHODS: In this prospective study, 54 patients with type 2 diabetes and peripheral neuropathy received 600 mg of ALA daily for 6 months. Twenty-four patients with diabetes without neuropathy were also included in the study. Serum PGRN and TNFα levels were determined using enzyme-linked immunosorbent assays. In addition, current perception threshold (CPT) testing was used to assess sensory neuropathy. RESULTS: After ALA treatment, serum PGRN levels were significantly increased and CPT values were significantly improved. Furthermore, there were significant positive correlations among TNFα, ICAM-1, and PGRN levels both before and after ALA treatment. A significant negative correlation was observed between the improvements in CPT and the PGRN levels. Furthermore, ICAM-1 levels were an independent predictor of PGRN levels. CONCLUSIONS: Changes in serum PGRN levels indicate that ALA treatment may have beneficial effects on endothelial function and neuronal inflammation.

Analysis of intravitreal bevacizumab treatment for macular oedema due to retinal vein occlusion.

PURPOSE: Our aim was to analyse the clinical effect of intravitreal bevacizumab treatment for macular oedema due to central/branch retinal vein occlusion (CRVO/BRVO). The end points were final best-corrected visual acuity (BCVA), BCVA improvement, final central 1-mm macular subfield thickness (CST) and change in CST. METHODS: Our study included 34 CRVO and 25 BRVO patients. Patients received intravitreal bevacizumab (IVB) treatment at our department. Our control group consisted of 50 CRVO and 30 BRVO patients, who had not received this treatment because their disease developed before the anti-VEGF treatment became available. For statistical analysis, two-sample t-test, Pearson's correlation, and ANOVA were used. The level of significance was defined at p < 0.05. RESULTS: With the two-sample t-test we found significant improvement of BCVA in the IVB-treated group (CRVO: 0.171 ± 0.270, p1 = 3.25×10-4; BRVO: 0.215 ± 0.282, p2 = 5.52×10-4). The difference in BCVA improvement was also significant compared to the control group (CRVO: p1 = 3.46×10-4; BRVO: p2 = 0.003). Significant decrease was observed in the CST in the treated group (CRVO: -345.114 ± 280.577, p1 = 6.94×10-9; BRVO: -151.875 ± 174.341, p2 = 1.67×10-4). In case of BRVO patients the final BCVA was significantly better in the treated group (0.617 ± 0.334) compared to the control group (0.406 ± 0.357), p = 0.016. CONCLUSION: IVB treatment results in significantly better final visual acuity and leads to significantly increased BCVA improvement compared to patients with RVO-induced macular oedema receiving no treatment.

Diabetic neuropathy and other diabetic complications at the Diabetic Neuropathy Center of the University of Debrecen / A diabeteses neuropathia és egyéb szövodmények elofordulása a Debreceni Egyetem Diabeteses Neuropathia Centrumában

INTRODUCTION: The prevalence of diabetes mellitus is significantly increasing worldwide. Distal sensorimotor neuropathy (DSPN) is the most common and the earliest detectable microvascular complication. Due to its diverse clinical appearance and atypical symptoms, DSPN is often recognized in an advanced stage. AIM AND METHOD: In our study, the data of 431 patients who were examined using the Neurometer® between 2011 and 2018 at the Diabetic Neuropathy Center of the University of Debrecen were processed and the correlations between cardiovascular and microvascular complications, laboratory parameters and the severity of DSPN were investigated. RESULTS: The average age of patients was 63.4 years, 62% of them were women, and 92% had type 2 diabetes mellitus. The average duration of diabetes was 13.7 years. Cardiovascular disease (CVD) was diagnosed in 42% of the patients. The incidence of retinopathy was 12%, persistent microalbuminuria was 16%. Despite DSNP complaints, neuronal damage could not be detected in 19%; in the examined patients 49% had mild, 19% moderate and 13% severe neuropathy. Diabetes-related neurological damage was more serious in the presence of both diabetic retinopathy (p<0.001) and microalbuminuria (p<0.001). The incidence of these microvascular complications and the severity of DSPN showed a significant positive correlation (p<0.001). There was no correlation between the severity of peripheral neuropathy and the development of CVD, and we did not find any correlations between the severity of DSPN and CVD. CONCLUSION: Based on our investigation, correlation between the progression of diabetic neuropathy and cardiovascular complications was not found, although the progression of diabetic neuropathy indicated the development of other microvascular diseases. Peripheral neurological examination using the Neurometer® is appropriate for controlling the DSPN status and the establishment of the severity of neuropathy determines the quality of life in diabetic patients. Among these patients, the risk of CVD can be assessed by Ewing's test for autonomic nervous system function. Orv Hetil. 2020; 161(30): 1243-1251.

Extractability of polyphenols from black currant, red currant and gooseberry and their antioxidant activity.

In this study, we analyzed extracts of Ribes (black currant, red currant and gooseberry) fruits obtained with methanol, methanol 50% and water. For each extract total polyphenol content, total flavonoid content and total anthocyanin content was assessed. The antioxidant activity of extracts was evaluated by 1,1-Diphenyl-2-picrylhydrazyl (DPPH) and 2,2'-azino-bis(3-ethylbenzothiazoline-6-sulphonic acid) (ABTS) radical scavenging capacity and by the photo-chemiluminescence (PCL) method. Identification and quantification of individual phenolic compounds was performed by means of high performance liquid chromatograph coupled with diode array detector (HPLC-DAD) analyses. From each fruit, best extraction of polyphenols was obtained with methanol 50%. In case of red currants and gooseberry there was no significant difference in flavonoids and anthocyanins extraction rate by the different extraction solvents. For black currants the methanol and methanol 50% extract presented the highest antioxidant activity. For red currants extracts with methanol 50% showed stronger antioxidant activity (IC50 = 5.71 mg/ml for DPPH, IC50 = 1.17 mg/ml for ABTS) than those with methanol or water. In case of gooseberry by the DPPH test the water extract proved to be the most active (IC50 = 5.9 mg/ml). In the PCL test black currants methanol 50% extract was over 6 times more powerful as the ones from red currants. In case of gooseberries, water extract presented the highest antioxidant activity (41.84 µmol AAE/g). In black currant cyanidin-3-glucoside was the major compound. Quercetin 3-O-glucoside was identified in each sample. From cinnamic acid derivatives neochlorogenic acid was present in black currants in the highest amount (356.33 µg/g).

Vaccinium Extracts as Modulators in Experimental Type 1 Diabetes.

Antihyperglycemic effects of four extracts obtained from leaves and fruits of Vaccinium myrtillus and Vaccinium corymbosum were assessed in diabetic rats. In addition, the effects of extracts on diabetic-related complications such as the development of diabetic cataract and oxidative stress were evaluated. Type 1 diabetes was induced with a single dose of streptozotocin in Wistar rats. The rats were randomly divided into seven equal groups: NC-normal control, DC-diabetic control, PC-positive control treated with metformin, VML-received V. myrtillus leaf extract, VMLF-received VML and fruit extract, VCL-received V. corymbosum leaf extract, and VCLF-received VCL and fruit extract. Body weight and glucose levels were monitored every second week. After 8 weeks of treatment, serum glucose, insulin, and malondialdehyde were measured. Lenses were removed after sacrifice and eight lenses from each group were randomly selected for evaluation of cataract development. A decrease in body weight was observed in all diabetic groups in the first weeks. In the VML group, no significant decrease was observed. Glucose levels during the experiment were high in DC, PC, and VCL groups, with no improvement during the 8 weeks. In VML, VMLF, and VCLF groups, a decrease in blood glucose levels was observed. Similar results regarding serum insulin and glucose levels at the end of the experiment were observed within groups. V. myrtillus extracts prevented the development of cataract compared with the DC group (P < .05).

Isolation and quantitative analysis of physalin D in the fruit and calyx of Physalis alkekengi L.

Physalin D was isolated from the methanol extract of Physalis alkekengi L. fruits by combination of different chromatographic methods (CPC, TLC, HPLC). The structure was elucidated based on 1H and 13C NMR spectral analysis with the aid of 2D-correlation spectroscopy (1H, 1H-COSY, HSQC and HMBC) and comparison with literature data. The quantity of physalin D in mature and immature fruits and calyces was determined by RP-HPLC-UV method. Among the studied samples, immature calyx showed the highest content of physalin D (0.7880 ± 0.0612%), while mature calyx contained 4 times less amount (0.2028 ± 0.016%). The physalin D content of the fruit was much lower; immature fruits contained 0.0992 ± 0.0083% physalin D and mature fruits 0.0259 ± 0.0021%. The antiproliferative activity of the CHCl3 extract and its fractions was tested on three cancer cell lines (HeLa, MCF-7 and A431). The antiproliferative activity of physalin D is discussed with regard the published data.

Chemical composition of essential oils of Grindelia squarrosa and G. hirsutula.

The essential oils of Grindelia squarrosa (Pursh) Dunal and G. hirsutula Hook. & Am. cultivated in Romania were isolated by hydrodistillation. The essential oils were analyzed by a combination of GC-FID and GC-MS. The identification of the constituents was achieved from their retention indices and comparison of their MS data with computer library database and literature data. The fifty-six identified constituents accounted for 72.1-81.3% of the oils. The oils were found to contain a-pinene, beta-pinene, limonene, borneol, bornyl acetate and germacrene D as main constituents. The oils obtained from the two species showed small differences in chemical composition. However, menthol, menthone and pulegone were detected only in the essential oil of G. hirsutula.

Anti-inflammatory activities of eleven Centaurea species occurring in the Carpathian Basin.

Our study aimed at the identification of anti-inflammatory activities of different fractions of C. sadleriana extract after per os administration in rats, the identification of the active compounds of the plant and the investigation of the in vitro anti-inflammatory activities of Centaurea species native to or cultivated in the Carpathian Basin. The aerial parts of Centaurea sadleriana Janka have been used in Hungarian folk medicine to treat the wounds of sheep. Methanol extract of C. sadleriana was fractioned by solvent-solvent partitioning. The n-hexane fraction was further fractionated and the anti-inflammatory activities of certain subfractions were confirmed in vivo in rats. The n-hexane and chloroform fraction of the methanol extract of C. sadleriana exhibited remarkable COX-1 and COX-2 inhibiting effects in vitro. Chromatographic separation of the fractions led to the identification of the active subfractions and 11 compounds (α-linolenic acid, γ-linolenic acid, stigmasterol, ß-sitosterol, campesterol, vanillin, pectolinarigenin, salvigenin, hispidulin, chrysoeriol and apigenin). The in vitro screening for anti-inflammatory activities of further Centaurea species occurring in the Carpathian Basin (C. adjarica, C. bracteata, C. cataonica, C. cynaroides, C. dealbata, C. indurata, C. macrocephala, C. melitensis, C. nigrescens, C. ruthenica) revealed considerable COX-1 and COX-2 inhibitory activities. Because C. sadleriana is an endangered species native only to the Carpathian Basin, the investigation of more prevalent species is reasonable.

[Antioxidant activity of the fruits and hydrophilic compounds of Physalis alkekengi]. / A Physalis alkekengi termésének és hidrofil anyagainak antioxidáns hatása.

Physalis alkekengi L. (bladder cherry, Chinese lantern, winter cherry) is an unusual species of the family Solanaceae. Although accumulation of alkaloids is characteristic to Solanaceae species, and accordingly the root and above ground parts of P. alkekengi are toxic, its fruits are in exceptionally edible. The present paper deals with the investigation of antioxidant hydrophilic compounds of the fruits in order to find correlation between the quantity of the constituents and antioxidant capacity of the extracts. Dried and fresh, freeze stored fruits were extracted with water, and the ascorbic acid and total polyphenol content of the fruits was determined. Furthermore, the antioxidant effect was investigated by DPPH test, and in vitro using the rat-brain homogenate method. The antioxidant activity measured by DPPH (fresh fruit: IC50 = 2.48 mg/ml; dried fruit: IC50 = 22.32 mg/ml) showed good correlation with the ascorbic acid content of the fruit (fresh fruit: 1.095%; dried fruit: 0.162%), and exhibited substantial decrease due the drying process. Lipid peroxidation inhibitory activity was found to be weaker as the DPPH radical scavenger capacity, however, also showed a decrease during the drying process of the fruit (fresh fruit: IC50 = 6.43 mg/ml; dried fruit: IC50 = 15.59 mg/ml). Our results clearly demonstrated the radical scavenger and lipid peroxidation inhibitory activity of aqueous extracts of bladder cherry, and indicate that the conservation and processing technology significantly influenced the antioxidant activity and the content of the active ingredients.