Effects of polyphenols of Cocos nucifera husk fibre on selected indices of cardiovascular diseases in mice

Joseph Oluwatope Adebayo,Olumuyiwa Sunday Adewumi,Simbiat Titilayo Baruwa,Elizabeth Abidemi Balogun,Sylvia Orume Malomo,Lawrence Aderemi Olatunji,Ayodele Olufemi Soladoye 셀메드 세포교정의약학회 2016 셀메드 (CellMed) Vol.6 No.2

Cocos nucifera (C. nucifera) oil is indigenously used to treat cardiovascular diseases. However, coconut husk fibre (which is rich in polyphenols) has not been screened for this property. Based on the ethnomedicinal use of polyphenols in treating cardiovascular diseases, this study was carried out to evaluate the effects of polyphenols of C. nucifera husk fibre on selected cardiovascular disease indices in mice. Fifty adult male Swiss albino mice were assigned randomly into five groups (A-E). Mice in groups B, C, D and E were administered 31.25, 62.5, 125, and 250 mg/kg body weight polyphenols of ethyl acetate extract of C. nucifera husk fibre respectively while the control group (A) mice received 5% DMSO for seven days. The mice were sacrificed twenty four hours after the last administration of polyphenols. Heart and plasma lactate dehydrogenase (LDH), alanine aminotransferase (ALT), aspartate aminotransferase (AST) and alkaline phosphatase (ALP) activities and plasma lipid profile were determined. Results revealed significant reduction (*p < 0.05) in plasma levels of total cholesterol and LDL-cholesterol with no significant change (*p > 0.05) in HDL-cholesterol, triglyceride and VLDL levels in the plasma at all doses of polyphenols administered compared to controls. There was significant reduction (*p < 0.05) in the activities of heart AST and LDH while plasma ALT, AST, and ALP activities were not significantly altered (*p > 0.05) at all doses of polyphenols administered compared to controls. These results suggest that the polyphenols of C. nucifera husk fibre possess cardio-protective properties and also indicate their possible use in the treatment of cardiovascular diseases.

Cancer Chemoprevention by Tea Polyphenols Through Modulating Signal Transduction Pathways

Lin, Jen-Kun The Pharmaceutical Society of Korea 2002 Archives of Pharmacal Research Vol.25 No.5

The action mechanisms of several chemopreventive agents derived from herbal medicine and edible plants have become attractive issues in cancer research. Tea is the most widely consumed beverage worldwide. Recently, the cancer chemopreventive actions of tea have been intensively investigated. It have been demonstrated that the active principles of tea were attributed to their tea polyphenols. Recently, tremendous progress has been made in elucidating the molecular mechanisms of cancer chemoprevention by tea and tea polyphenols. The suppression of various tumor biomarkers including growth factor receptor tyrosine kinases, cytokine receptor kinases, P13K, phosphatases, ras, raf, MAPK cascades, NㆍFB, IㆍB kinase, PKA, PKB, PKC, c-jun, c-fos, c-myc, cdks, cyclins, and related transducing proteins by tea polyphenols has been studied in our laboratory and others. The IㆍB kinase (IKK) activity in LPS-activated murine macrophages (RAW 264.7 cells) was found to be inhibited by various tea polyphenols including (-) epigallocatechin-3-gallate (EGCG), theaflavin (TF-1), theaflavin-3-gal-late (TF-2) and theaflavin-3,3'-digallate (TF-3). TF-3 inhibited IKK activity in activated macrophages more strongly than did the other tea polyphenols. TF-3 inhibited both IKK1 and IKK2 activity and prevented the degradation of IㆍBㆍand IㆍBㆍin activated macrophage cells. The results suggested that the inhibition of IKK activity by TF-3 and other tea polyphenols could occur by a direct effect on IKKs or on upstream events in the signal transduction pathway. TF-3 and other tea polyphenols blocked phosphorylation of IB from the cytosolic fraction, inhibited NFB activity and inhibited increases in inducible nitric oxide synthase levels in activated macrophage. TF-3 and other tea polyphenols also inhibited strongly the activities of xanthine oxidase, cyclooxygenase, EGF-receptor tyrosine kinase and protein kinase C. These results suggest that TF-3 and other tea polyphenols may exert their cancer chemoprevention through suppressing tumor promotion and inflammation by blocking signal transduction. The mechanisms of this inhibition may be due to the blockade of the mitogenic and differentiating signals through modulating EGFR function, MAPK cascades, NFkB activation as wll as c-myc, c-jun and c-fos expression.

Protective Effects of Green Tea Polyphenol Against Renal Injury Through ROS-Mediated JNK-MAPK Pathway in Lead Exposed Rats

Wei Li,Haidong Wang,Deyuan Li,Zhongze Hu,Siming Zhao,Zhejun Zheng 한국분자세포생물학회 2016 Molecules and cells Vol.39 No.6

To investigate the potential therapeutic effects of polyphenols in treating Pb induced renal dysfunction and intoxication and to explore the detailed underlying mechanisms. Wistar rats were divided into four groups: control groups (CT), Pb exposure groups (Pb), Pb plus Polyphenols groups (Pb+PP) and Polyphenols groups (PP). Animals were kept for 60 days and sacrificed for tests of urea, serum blood urea nitrogen (BUN) and creatinine. Histological evaluations were then performed. In vitro studies were performed using primary kidney mesangial cells to reveal detailed mechanisms. Cell counting kit-8 (CCK-8) was used to evaluate cell viability. Pb induced cell apoptosis was measured by flow cytometry. Reactive oxygen species (ROS) generation and scavenging were tested by DCFH-DA. Expression level of tumor necrosis factor- (TNF-), interleukin-1- (IL-1-) and IL-6 were assayed by ELISA. Western blot and qPCR were used to measure the expression of ERK1/2, JNK1/2 and p38. Polyphenols have obvious protective effects on Pb induced renal dysfunction and intoxication both in vivo and in vitro. Polyphenols reduced Pb concentration and accumulation in kidney. Polyphenols also protected kidney mesangial cells from Pb induced apoptosis. Polyphenols scavenged Pb in-duced ROS generation and suppressed ROS-mediated ERK/JNK/p38 pathway. Downstream pro-inflammatory cytokines were inhibited in consistency. Polyphenol is protective in Pb induced renal intoxication and inflammatory responses. The underlying mechanisms lie on the antioxidant activity and ROS scavenging activity of polyphenols.

Protective Effects of Green Tea Polyphenol Against Renal Injury Through ROS-Mediated JNK-MAPK Pathway in Lead Exposed Rats

Wang, Haidong,Li, Deyuan,Hu, Zhongze,Zhao, Siming,Zheng, Zhejun,Li, Wei Korean Society for Molecular and Cellular Biology 2016 Molecules and cells Vol.39 No.6

To investigate the potential therapeutic effects of polyphenols in treating Pb induced renal dysfunction and intoxication and to explore the detailed underlying mechanisms. Wistar rats were divided into four groups: control groups (CT), Pb exposure groups (Pb), Pb plus Polyphenols groups (Pb+PP) and Polyphenols groups (PP). Animals were kept for 60 days and sacrificed for tests of urea, serum blood urea nitrogen (BUN) and creatinine. Histological evaluations were then performed. In vitro studies were performed using primary kidney mesangial cells to reveal detailed mechanisms. Cell counting kit-8 (CCK-8) was used to evaluate cell viability. Pb induced cell apoptosis was measured by flow cytometry. Reactive oxygen species (ROS) generation and scavenging were tested by DCFH-DA. Expression level of tumor necrosis factor-${\alpha}$ (TNF-${\alpha}$), interleukin-1-${\beta}$ (IL-1-${\beta}$) and IL-6 were assayed by ELISA. Western blot and qPCR were used to measure the expression of ERK1/2, JNK1/2 and p38. Polyphenols have obvious protective effects on Pb induced renal dysfunction and intoxication both in vivo and in vitro. Polyphenols reduced Pb concentration and accumulation in kidney. Polyphenols also protected kidney mesangial cells from Pb induced apoptosis. Polyphenols scavenged Pb induced ROS generation and suppressed ROS-mediated ERK/JNK/p38 pathway. Downstream pro-inflammatory cytokines were inhibited in consistency. Polyphenol is protective in Pb induced renal intoxication and inflammatory responses. The underlying mechanisms lie on the antioxidant activity and ROS scavenging activity of polyphenols.

Bidirectional Interactions between Green Tea (GT) Polyphenols and Human Gut Bacteria

Choi Se Rin,Lee Hyunji,Singh Digar,Cho Donghyun,Chung Jin-Oh,Roh Jong-Hwa,Kim Wan-Gi,Lee Choong Hwan 한국미생물·생명공학회 2023 Journal of microbiology and biotechnology Vol.33 No.10

Green tea (GT) polyphenols undergo extensive metabolism within gastrointestinal tract (GIT), where their derivatives compounds potentially modulate the gut microbiome. This biotransformation process involves a cascade of exclusive gut microbial enzymes which chemically modify the GT polyphenols influencing both their bioactivity and bioavailability in host. Herein, we examined the in vitro interactions between 37 different human gut microbiota and the GT polyphenols. UHPLCLTQ-Orbitrap-MS/MS analysis of the culture broth extracts unravel that genera Adlercreutzia, Eggerthella and Lactiplantibacillus plantarum KACC11451 promoted C-ring opening reaction in GT catechins. In addition, L. plantarum also hydrolyzed catechin galloyl esters to produce gallic acid and pyrogallol, and also converted flavonoid glycosides to their aglycone derivatives. Biotransformation of GT polyphenols into derivative compounds enhanced their antioxidant bioactivities in culture broth extracts. Considering the effects of GT polyphenols on specific growth rates of gut bacteria, we noted that GT polyphenols and their derivate compounds inhibited most species in phylum Actinobacteria, Bacteroides, and Firmicutes except genus Lactobacillus. The present study delineates the likely mechanisms involved in the metabolism and bioavailability of GT polyphenols upon exposure to gut microbiota. Further, widening this workflow to understand the metabolism of various other dietary polyphenols can unravel their biotransformation mechanisms and associated functions in human GIT.

Development of Origanum vulgare Cell Suspension Culture to Produce Polyphenols and the Stimulation Effect of Salicylic Acid Elicitation and Phenylalanine Feeding

Yan-Ping Li,Dao-Bang Tang,Xiao-Qiang Wang,Meng Wang,Qing-Feng Zhang,Yuan Liu,Bei-Yun Shen,Jiguang Chen,Zhongping Yin 한국생물공학회 2021 Biotechnology and Bioprocess Engineering Vol.26 No.3

Three types of calli were induced from Origanum vulgare (O. vulgare) aseptic seedlings, and the friable calli with white appearance and high growth rate were further screened and used to develop cell suspension culture to produce polyphenols. Murashige and Skoog (MS) medium with 3.0 mg/L Kinetin (KT) and 0.5 mg/L 2,4-dichlorophenoxy acetic acid (2,4-D) was suitable for both O. vulgare cells growth and polyphenols accumulation. To further enhance the polyphenols accumulation, O. vulgare cells were treated by phenylalanine (Phe) feeding and salicylic acid (SA) elicitation. Compared with the individual Phe feeding and SA elicitation, SA elicitation combined with Phe feeding showed a much better promotion effect on the polyphenols synthesis in O. vulgare cells, especially rosmarinic acid (RosA) accumulation. With the combined treatment of 200 μM SA and 100 μM Phe, total polyphenols content and yield were 41.36 mg/g and 752.93 mg/L, respectively. RosA content and yield reached 31.25 mg/g and 570.37 mg/L, which were 5.44 and 5.47 times that of the control. Furthermore, the total polyphenols extracted from the cultured cells treated by SA elicitation combined with Phe feeding displayed a much higher antioxidant capacity than that of untreated cells, meanwhile its 1,1-diphenyl-2- trinitrophenyl hydrazine (DPPH) and superoxide anion radical-scavenging activity were much stronger than that of vitamin C. What’s more, our results also showed that RosA was the principal contributor to the fine antioxidant capacity of the total polyphenols extracted from the SA and Phe treated cells. Our research indicated that SA elicitation combined with Phe feeding significantly improved the polyphenols yield and antioxidant capacity of the cultured O. vulgare cells, and therefore has a promising application prospect in natural polyphenols production.

Natural polyphenols antagonize the antimyeloma activity of proteasome inhibitor bortezomib by direct chemical interaction

Kim, Tae Young,Park, Jongmin,Oh, Bora,Min, Hyun Jung,Jeong, Tae-Sook,Lee, Jae Hoon,Suh, Cheolwon,Cheong, June-Won,Kim, Hyo Jung,Yoon, Sung-Soo,Park, Seung Bum,Lee, Dong Soon Blackwell Publishing Ltd 2009 British journal of haematology Vol.146 No.3

<P>Summary</P><P>Bortezomib is a therapeutic proteasome inhibitor with antimyeloma activity and polyphenols are well known compounds that exert antiproliferative effects against tumuors. We attempted to co-treat myeloma cells with bortezomib and polyphenols, anticipating a synergistic effect. However, the anticancer activity of bortezomib was blocked by the polyphenols. The structural features of the polyphenols correlated strikingly with their antagonistic effect; in particular, the presence or absence of a vicinal diol moiety was the key element for effective blockage of the anticancer function of bortezomib. We speculated that the vicinal diols in the polyphenols interact with the boronic acid of bortezomib and convert the active triangular boronic acid of bortezomib to an inactive tetrahedral boronate, thus abolishing the antimyeloma activity of bortezomib. We confirmed this hypothesis by <SUP>11</SUP>B nuclear magnetic resonance spectroscopy and an <I>in vitro</I> assay on multiple myeloma (MM) cell lines and primary myeloma cells from patients. Based on these findings, restriction of the intake of natural polyphenols in foods or vitamin supplements during bortezomib treatment in MM patients should be considered.</P>

Effects of a chitosan nanoparticles encapsulation on the properties of litchi polyphenols

Xingan Cheng,Qiwen Zou,Hanhui Zhang,Jianwei Zhu,Murtaza Hasan,Fangyun Dong,Xin Liu,Junjie Li,Yuehua Wu,Xiaojing Lv,Keqiang Wang,Xiangling Deng,Zhanmei Liu,Xuhong Jiang 한국식품과학회 2023 Food Science and Biotechnology Vol.32 No.13

Litchi polyphenols have very specific biological activities. Nevertheless, the low and inconsistent oral bioavailability and instability hinder the further application of litchi polyphenols in food systems. This work prepared litchi polyphenols loaded chitosan nanoparticles (LP-CSNPs) by ionic gelation method to enhance the encapsulation on the properties of litchi polyphenols. The optimum conditions of formation via single factors and the Box–Behnken design were chitosan (CS) concentration 1.065 mg/mL, sodium tripolyphosphate (TPP) concentration 0.975 mg/mL, and the mass ratios of polyphenols and CS 1:1 with encapsulation efficiency (EE%) of 45.53%. LP-CSNPs presented the nanosized range of particle size (mean 170 nm), excellent polydispersity index (PDI) (0.156 ± 0.025), and zeta potential values (+ 35.44 ± 0.59). The in vitro release in simulated gastric fluid (pH 1.2) and intestinal fluid (pH 6.8) during 100 h was 58.34% and 81.68%, respectively. LP-CSNPs could effectively improve the storage stability and had great antibacterial activity compared with unencapsulated litchi polyphenols.

Effect of Tea Polyphenols on Conversion of Nicotine to Cotinine

( Dong Hee Lee ),( Ha Won Kim ) 한국응용약물학회 2003 Biomolecules & Therapeutics(구 응용약물학회지) Vol.11 No.4

N/A Nicotine is one of the major hazardous components in cigarette smoke. Nicotine deals a harmful effect to smokers and passive smokers due to its rapid conversion to various carcinogenic metabolites. Nitro-samine-4-(methylnitrosamino)-1-(3-pyridyl)-1-butanone(NNK) is believed to cause lung cancers among the nicotine-derived carcinogens. Recent studies report that NNK synthesis can be inhibited by the metabolism pathway to produce a stable metabolite cotinine from nicotine. Tea polyphenols have been known to contain factors to prevent cancers and to retard progression of cancers. This study aims to correlate tea polyphenol`s potential for cancer prevention with an accelerated formation of cotinine. The conversion from nicotine to cotinine in the presence of tea extracts or three polyphenols (Catechin, epicatechin gallate, epigallocatechin gallate) was measured in established cell lines and in Xenopus oocytes. Among three lines of cell used, PLC/PRF5 and HEK293 cells showed a fast turnover from nicotine to cotinine while HepG2 cell line showed a marginal difference between groups treated and non-treated with tea polyphenols. When Xenopus oocytes were microinjected with nicotine, tea polyphenols appear to accelerate the conversion of nicotine to cotinine. Among the polyphenols tested in this study, (+)-catechin showed the best efficiency overall in accelerating conversion from nicotine to cotinine both in the cell lines and in the oocytes. In summary, the present study indicated that tea polyphenols have a positive effect on conversion of nicotine to cotinine.

A Comparison of Pectin, Polyphenols, and Phytosterols, Alone or in Combination, to Lovastatin for Reduction of Serum Lipids in Familial Hypercholesterolemic Swine

B.T. Metzger,D.M. Barnes,J.D. Reed 한국식품영양과학회 2009 Journal of medicinal food Vol.12 No.4

Greater than 50% of Americans use some form of a dietary supplement, and a diagnosis of coronary artery disease is associated with higher supplement use. The objective of this study was to compare nutritional supplements (pectin, polyphenols, and phytosterols) to lovastatin to reduce serum cholesterol. Familial hypercholesterolemic (FH) swine received the same amount of basal diet (control) in addition to pectin (30g/day), polyphenols (20g/day), phytosterols (6g/day), and all possible combinations in contrast to lovastatin (3mg/kg of body weight). The experimental design consisted of 4 weeks of basal diet followed by 4 weeks of basal diet plus the supplement treatment. All of the supplements, except pectin, reduced total cholesterol by an average of 71±19mg/dL in comparison to the control diet (53±20mg/dL) and lovastatin (143±21mg/dL) during the 5–8-week treatment period. Serum high-density lipoprotein-cholesterol remained unchanged, while serum triglycerides changed independent of diet. During the 5–8-week treatment period serum low-density lipoprotein (LDL)-cholesterol was reduced maximally 22%, 19%, 20%, 17%, 18%, and 17% by polyphenols, phytosterols, pectin+polyphenols, pectin+phytosterols, polyphenols+phytosterols, and pectin+polyphenols+phytosterols, respectively, compared to control (8%) and lovastatin (40%). Phytosterols was the most effective supplementation, while both phytosterol and polyphenol supplements enhanced the reduction in LDL-cholesterol of pectin-containing diets. Supplements effectively reduced cholesterol in FH swine by half compared to lovastatin. Results suggest that more research on the use of dietary supplements, alone or in combination with statins, to reduce LDL-cholesterol is justified.