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1.
Antimicrobial flavonoids as a potential substitute for overcoming antimicrobial resistance.
Biharee, A, Sharma, A, Kumar, A, Jaitak, V
Fitoterapia. 2020;:104720
Abstract
BACKGROUND Infectious diseases are the leading cause of death in 21st century due to antimicrobial resistance and scarcity of new molecules to undertake rising infections. There could be a multiple reasons behind antimicrobial resistance whether it is increased drug metabolism or bacterial endotoxins. The demand of effective medication is increasing day by day to treat microbial infections and combat antimicrobial resistance. In recent years most of the synthetic antimicrobials developed resistance so natural products could provide better options to fulfill this demand. There has been increasing interest in the research on flavonoids because various flavonoids were found to be effective against pathogenic microorganisms. OBJECTIVE The objective of this article will be to explore antimicrobial activity of flavonoids with special focus on their possible mechanism of action. METHODS The article reviewed recent literature related to flavonoids with antimicrobial activity, which were isolated from various sources and the compounds showing fairly good activity against tested microbial species were discussed. RESULTS By throughout literature review it has been found that flavonoids show antimicrobial effect by inhibiting virulence factors, efflux pump, biofilm formation, membrane disruption, cell envelop synthesis, nucleic acid synthesis, and bacterial motility inhibition. CONCLUSION Most of the antimicrobial drugs available now a days are ineffective due to development of resistance to them. Flavonoids have the potential to overcome this emerging crisis as this class of natural products showed the antimicrobial activity by different mechanisms than those of conventional drugs, so flavonoid could be an effective treatment of pathogenic infections.
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2.
Keloidal penile fibrosis: improvements with Centellicum® (Centella asiatica) and Pycnogenol® supplementation: a pilot registry.
Ledda, A, Cornelli, U, Belcaro, G, Dugall, M, Feragalli, B, Cotellese, R, Hu, S, Corsi, M
Panminerva medica. 2020;(1):13-18
Abstract
BACKGROUND The aim of this pilot study was to evaluate the effects of Pycnogenol® and CA (Centellicum®) on penile fibrosis and on associated signs and symptoms. METHODS A group of 82 subjects with penile nodules and plaques was included in this registry study and followed up for 3 months; 32 were managed with standard management (SM) only. Twenty-four were managed with CA (Centellicum®: 3 capsules/day: 675 mg/day) in association with SM, and 26 subjects were managed with Pycnogenol® (150 mg/day) + CA (Centellicum® at the same dosage as in group 2) and SM. RESULTS Subjects in the 3 groups were comparable, including the distribution of plaques. The occurrence of any previous catheterizations was also comparable. Safety and tolerability were optimal, no subjects had to stop supplementation. The percentage of subjects with improved symptoms evaluated with a Visual Analogue Scale line was significantly higher with both supplements in comparison with SM (P<0.05). The combined management with Pycnogenol® and Centellicum® was superior to the other 2 managements (P<0.05). Erectile function assessed by the Index of Erectile Fuction questionnaire (IIEF) was significantly higher with the combination Pycnogenol®+Centellicum (P<0.05). The number of plaques and microplaques, the average total sectional area of the plaques in each subject and the grey scale median were all better improved with the combination. Both supplementations were superior to SM at 12 weeks (P<0.05). Oxidative stress resulted significantly better (P<0.05) with the combination. All blood tests were normal at inclusion and at 12 weeks. The minimal, penile curvature at baseline was reduced in both the supplement groups at 12 weeks more than in the SM group (P<0.05). CONCLUSIONS In conclusion Centellicum and Pycnogenol® appear to improve penile fibrosis reducing the keloidal aspects of penile plaques.
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3.
Broad-Spectrum Preclinical Antitumor Activity of Chrysin: Current Trends and Future Perspectives.
Moghadam, ER, Ang, HL, Asnaf, SE, Zabolian, A, Saleki, H, Yavari, M, Esmaeili, H, Zarrabi, A, Ashrafizadeh, M, Kumar, AP
Biomolecules. 2020;(10)
Abstract
Pharmacological profile of phytochemicals has attracted much attention to their use in disease therapy. Since cancer is a major problem for public health with high mortality and morbidity worldwide, experiments have focused on revealing the anti-tumor activity of natural products. Flavonoids comprise a large family of natural products with different categories. Chrysin is a hydroxylated flavonoid belonging to the flavone category. Chrysin has demonstrated great potential in treating different disorders, due to possessing biological and therapeutic activities, such as antioxidant, anti-inflammatory, hepatoprotective, neuroprotective, etc. Over recent years, the anti-tumor activity of chrysin has been investigated, and in the present review, we provide a mechanistic discussion of the inhibitory effect of chrysin on proliferation and invasion of different cancer cells. Molecular pathways, such as Notch1, microRNAs, signal transducer and activator of transcription 3 (STAT3), nuclear factor-kappaB (NF-κB), PI3K/Akt, MAPK, etc., as targets of chrysin are discussed. The efficiency of chrysin in promoting anti-tumor activity of chemotherapeutic agents and suppressing drug resistance is described. Moreover, poor bioavailability, as one of the drawbacks of chrysin, is improved using various nanocarriers, such as micelles, polymeric nanoparticles, etc. This updated review will provide a direction for further studies in evaluating the anti-tumor activity of chrysin.
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4.
Effects of Cocoa-Rich Chocolate on Blood Pressure, Cardiovascular Risk Factors, and Arterial Stiffness in Postmenopausal Women: A Randomized Clinical Trial.
Garcia-Yu, IA, Garcia-Ortiz, L, Gomez-Marcos, MA, Rodriguez-Sanchez, E, Agudo-Conde, C, Gonzalez-Sanchez, J, Maderuelo-Fernandez, JA, Recio-Rodriguez, JI
Nutrients. 2020;(6)
Abstract
This study aimed to evaluate the effects of the intake of 10 g of cocoa-rich chocolate on blood pressure, other cardiovascular risk factors, and vascular structure and function in postmenopausal women. A total of 140 postmenopausal women participated in this randomized and controlled parallel clinical trial. For six months, the intervention group (IG; n = 73) consumed daily 10 g of chocolate (99% cocoa) added to their usual food intake, whereas the control group (CG; n = 67) did not receive any intervention. Blood pressure, pulse pressure (PP), cardio-ankle vascular index (CAVI), ankle-brachial index (ABI), brachial-ankle pulse wave velocity (baPWV), augmentation index, and laboratory variables were measured at baseline and six months. ANCOVA analyses adjusted for baseline values revealed no significant differences for systolic blood pressure (-1.45 mm Hg; 95% confidence interval (CI): -4.79, 1.88; p = 0.391) or baPWV (0.18 m/s; 95% CI: -0.14, 0.50; p = 0.263) between groups. A decrease in PP was observed in the IG compared to the CG (-2.05 mm Hg; 95% CI: -4.08, -0.02; p = 0.048). The rest of the vascular structure and function parameters and other measured variables remained unchanged. The daily intake of 10 g of cocoa-rich chocolate seems to provide little improvement to cardiovascular health, but neither does it cause any adverse effects on the parameters evaluated in postmenopausal women in the long term.
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Effect of Pycnogenol on Blood Pressure: Findings From a PRISMA Compliant Systematic Review and Meta-Analysis of Randomized, Double-Blind, Placebo-Controlled, Clinical Studies.
Fogacci, F, Tocci, G, Sahebkar, A, Presta, V, Banach, M, Cicero, AFG
Angiology. 2020;(3):217-225
Abstract
Results of previous clinical trials evaluating the effect of pycnogenol supplementation on blood pressure (BP) are controversial. Therefore, we aimed to assess the impact of pycnogenol on BP through a systematic review of literature and meta-analysis of available randomized, double-blind, placebo-controlled clinical studies (randomized clinical trials [RCTs]). Literature search included SCOPUS, PubMed-Medline, ISI Web of Science, and Google Scholar databases up to January 10, 2019 to identify RCTs investigating the impact of pycnogenol on BP. Two investigators independently extracted data on study characteristics, methods, and outcomes. This systematic review and meta-analysis is registered in International Prospective Register of Systematic Reviews (PROSPERO) under number CRD42018112172. Overall, the impact of pycnogenol on BP was reported in 7 trials involving 626 participants. Meta-analysis did not suggest any significant improvement in systolic BP (weighted mean difference [WMD]: -0.028 mm Hg; 95% confidence interval [CI]: -0.182 to 0.127; P = .726; I2 = 46%), diastolic BP (WMD: -0.144 mm Hg; 95% CI: -0.299 to 0.010; P = .067; I2 = 0%), mean arterial pressure (WMD: -0.091 mm Hg; 95% CI: -0.246 to 0.063; P = .246; I2 = 0%), and pulse pressure (WMD: -0.003 mm Hg; 95% CI: -0.151 to 0.158; P = .966; I2 = 0%) following pycnogenol treatment. Results persisted in the leave-one-out sensitivity analysis. Therefore, the present meta-analysis does not suggest any significant effect of pycnogenol on BP.
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6.
A Double-Blind, Cross-Over Study to Examine the Effects of Maritime Pine Extract on Exercise Performance and Postexercise Inflammation, Oxidative Stress, Muscle Soreness, and Damage.
Aldret, RL, Bellar, D
Journal of dietary supplements. 2020;(3):309-320
Abstract
The purpose of the present study was to examine whether 14 days of supplementation with maritime pine extract leading up to and following an exercise test would increase performance and reduce biomarkers associated with muscle damage, inflammation, and oxidative stress. The study used a double-blind, placebo-controlled, cross-over design. Twenty apparently healthy young male participants ingested either 800 mg pine bark extract or placebo for 14 days prior to the first exercise trial and for 2 days postexercise. On the exercise day, participants submitted a pre-exercise blood sample then completed a VO2 peak test until volitional failure. A postexercise blood sample was collected 1 hour after completion of exercise. Participants returned at 24 and 48 hours after the exercise testing for measures of muscle pain in the lower body using an algometer. Participants then had a 7-day washout period before beginning to cross over to the alternate treatment. Analysis via ordinal regression demonstrated a significant difference in oxidative stress in the maritime pine extract group compared to placebo (ChiSq = 2.63; p = 0.045). Maritime pine extract was effective at affording protection from oxidative stress postexercise. Further work should be undertaken to evaluate the findings with other exercise modes or in participants with known metabolic syndrome.
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7.
Ampelopsin Induces DR5-Mediated Apoptotic Cell Death in EBV-Infected Cells through the p38 Pathway.
Yun, SM, Kim, YS, Kim, KH, Hur, DY
Nutrition and cancer. 2020;(3):489-494
Abstract
Ampelopsin (AMP) is a well-known flavonoid that exerts a number of biological and pharmacological effects including anticancer effects against several cancer cell lines. In this study, we investigated the anticancer activity of AMP against Epstein-Barr virus (EBV)-positive cells and its mechanism of action. Our results showed that AMP dose-dependently inhibited cell viability and induced apoptotic cell death in EBV-positive cells without cytotoxicity in EBV-negative cells. In particular, AMP induced caspase-8 dependent apoptosis via upregulation of tumor necrosis factor-related apoptosis-inducing ligand (TRAIL) and death receptor (DR5). Knockdown of DR5 by RNA interference blocked AMP-induced apoptosis. Furthermore, AMP dose-dependently activated p38 mitogen-activated protein kinases (MAPKs) in EBV-positive cells. Additionally, SB203580 (a p38-MAPK inhibitor) effectively inhibited apoptotic cell death. These results demonstrate that treatment with AMP induces the apoptosis of EBV-positive cells through upregulation of TRAIL/DR5 and activation of p38 signaling. Therefore, these results provide experimental information for developing AMP as a new therapeutic drug against EBV-positive cancer.
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8.
The impact of xenoestrogens on effectiveness of treatment for hormone-dependent breast cancer - current state of knowledge and perspectives for research.
Boszkiewicz, K, Sawicka, E, Piwowar, A
Annals of agricultural and environmental medicine : AAEM. 2020;(4):526-534
Abstract
INTRODUCTION Breast cancer is the most common cancer occurring in women and causing the highest number of deaths among them. The role of xenoestrogens has been the subject of many studies in the pathogenesis of breast cancer. Less is known about the impact of xenoestrogens on the effectiveness of hormone therapy used to treat breast cancer, and thus possible drug-xenostrogen interactions. OBJECTIVE The aim of this review is to summarize the current state of knowledge and present perspectives for further research on the impact of xenoestrogens on the effectiveness of drugs used in the treatment of hormone-dependent breast cancer. CURRENT STATE OF KNOWLEDGE Phytoestrogens, in particular flavonoid genistein, are the best studied group of xenoestrogens in terms of interaction with drugs used in the treatment of breast cancer, due to their frequent use, including their use in alleviating the adverse effects of hormone therapy. Analyzing the current state of knowledge, it seems that phytoestrogens intake should be avoided during conventional anti-cancer treatment. Of the other xenoestrogens, bisphenol A (BPA) is one of the best-tested compounds for interactions with drugs used to treat breast cancer. It has been shown that bisphenol A could reduced therapeutic effect of active tamoxifen metabolite and cytostatics used in breast cancer treatment. CONCLUSIONS Confirmation in clinical trials of the results obtained in vitro and in vivo tests, would enable the creation of specific recommendations for patients undergoing breast cancer treatment, especially hormone therapy. An area requiring further research is the analysis of the effects of xenoestrogens other than phytoestrogens, e.g. metalloestrogens, on the effects of drugs used in the treatment of breast cancer.
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9.
Current Perspectives of the Applications of Polyphenols and Flavonoids in Cancer Therapy.
Montané, X, Kowalczyk, O, Reig-Vano, B, Bajek, A, Roszkowski, K, Tomczyk, R, Pawliszak, W, Giamberini, M, Mocek-Płóciniak, A, Tylkowski, B
Molecules (Basel, Switzerland). 2020;(15)
Abstract
The development of anticancer therapies that involve natural drugs has undergone exponential growth in recent years. Among the natural compounds that produce beneficial effects on human health, polyphenols have shown potential therapeutic applications in cancer due to their protective functions in plants, their use as food additives, and their excellent antioxidant properties. The possibility of combining conventional drugs-which are usually more aggressive than natural compounds-with polyphenols offers very valuable advantages such as the building of more efficient anticancer therapies with less side effects on human health. This review shows a wide range of trials in which polyphenolic compounds play a crucial role as anticancer medicines alone or in combination with other drugs at different stages of cancer: cancer initiation, promotion, and growth or progression. Moreover, the future directions in applications of various polyphenols in cancer therapy are emphasized.
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10.
Antitumor effect of baicalin from the Scutellaria baicalensis radix extract in B-acute lymphoblastic leukemia with different chromosomal rearrangements.
Orzechowska, BU, Wróbel, G, Turlej, E, Jatczak, B, Sochocka, M, Chaber, R
International immunopharmacology. 2020;:106114
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Abstract
Acute B-lymphoblastic leukemia (B-ALL) is the most common hematologic malignancy in children. Many cases of B-ALL harbor chromosomal translocations which are often critical determinants of prognosis. Most of them represent altered transcription factors that impact gene transcription or enhance signaling. B-ALLs harboring the mixed-lineage leukemia 1 (MLL1) gene rearrangements represent aggressive, high-risk type of early childhood leukemias that are usually associated with a very poor prognosis. Therefore, there is an urgent need for novel therapeutic agents as well as new treatment strategies. The objective was to examine the vitro inhibitory effects of Scutellaria baicalensis root extract (SBE) in B-ALL cell lines with different chromosomal rearrangements and in leukemic blasts derived from patients' bone marrow (BMCs). In this study we showed that baicalin which is the main component of the SBE possess antitumor activity against all leukemic cell lines especially those with MLL and PBX1 gene rearrangements. Baicalin inhibited cell proliferation, arrested the cell cycle at the G0/G1 phase, and induced cell death through caspase 3/7 activation. Moreover, baicalin treatment inhibited the glycogen synthase kinase-3β (GSK-3β) by suppressing its phosphorylation at Y216, and upregulated the downstream mediator of the cell cycle arrest - cyclin dependent kinase inhibitor p27Kip1. Bone marrow derived blasts from B-ALL patients also exhibited varied sensitivity towards baicalin with 72% patients sensitive to the SBE and baicalin treatment. Taken together, our findings provide new insights into the anti-cancer properties of baicalin by showing its diverse mode of action which might be related to the different genetic background.