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Friday, 8 November 2013

Phytochemicals - 13 Health Benefits of Apigenin

Apigenin (4’,5,7-trihydroxyflavone) is a flavone or citrus bioflavonoids found in high amounts in fruits, vegetables red wine and tomato sauce and several herbs including parsley, thyme, and peppermint.

Health Benefits
1. Promyelocytic leukemia HL-60 cells
In the study of non-mutagenic flavonoid apigenin 7-glucoside and its effect in cancer prevention through cancer cell differentiation, found that Apigenin 7-glucoside inhibited HL-60 cell growth, dose- and time-dependently, but did not cause apoptosis. The distribution of cells at different stages in the cell cycle indicated an accumulation of treated cells in G(2)/M phase. Moreover, apigenin 7-glucoside induced granulocytic differentiation of HL-60 cells, according to "Proteomic study of granulocytic differentiation induced by apigenin 7-glucoside in human promyelocytic leukemia HL-60 cells" by Nakazaki E, Tsolmon S, Han J, Isoda H.(1)

2. Anti-adipogenic Effect
In the investigation of apigenin, a plant flavonoid, on adipogenesis and its effect in adipogenesis found that Apigenin suppressed adipocyte differentiation of mouse adipocytic 3T3-L1 cells and reduced the accumulation of intracellular lipids.Thus, dietary apigenin may contribute to lower body-fat content and body-weight gain through the activation of 5'-adenosine monophosphate-activated protein kinase (AMPK), according to "Anti-adipogenic Effect of Dietary Apigenin through Activation of AMPK in 3T3-L1 Cells" by Ono M, Fujimori K.(2)

3. Cancer prevention
In the study of apigenin, a naturally occurring plant flavone, abundantly present in common fruits and vegetables and it anti oxidative process indicated that human clinical trials examining the effect of supplementation of apigenin on disease prevention have not been conducted, although there is considerable potential for apigenin to be developed as a cancer chemopreventive agent, according to "Apigenin: a promising molecule for cancer prevention" by Shukla S, Gupta S.(3)

4. Colon cancer
In the investigation of dietary apigenin and naringenin and their effect against colon cancer found that the ability of dietary apigenin and naringenin to reduce HMACF, lower proliferation (naringenin only) and increase apoptosis may contribute toward colon cancer prevention. However, these effects were not due to mitigation of iNOS and COX-2 protein levels at the ACF stage of colon cancer, according to "Apigenin and naringenin suppress colon carcinogenesis through the aberrant crypt stage in azoxymethane-treated rats" by Leonardi T, Vanamala J, Taddeo SS, Davidson LA, Murphy ME, Patil BS, Wang N, Carroll RJ, Chapkin RS, Lupton JR, Turner ND.(4)

5. Leukemia
In the evaluation of apigenin and it effects human leukemia cells and anti-leukemic activity found that constitutively active myristolated Akt prevented apigenin-induced JNK, caspases activation, and apoptosis. Conversely, LY294002 and a dominant negative construct of Akt potentiated apigenin-induced apoptosis in leukemia cells, according to "Apigenin induces apoptosis in human leukemia cells and exhibits anti-leukemic activity in vivo via inactivation of Akt and activation of JNK" by Budhraja A, Gao N, Zhang Z, Son YO, Cheng S, Wang X, Ding S, Hitron A, Chen G, Luo J, Shi X.(5)

(6) Antioxidant Activity
In the observation of supercritical carbon dioxide (SC-CO(2)) extraction of bioactive compounds including flavonoids and phenolics from Ampelopsis grossedentata stems found that flavonoids and phenolics were found to be mainly responsible for the 2,2-diphenyl-1-picrylhydrazyl (DPPH) scavenging activity of the extracts, but not for the chelating activity on ferrous ion according to Pearson correlation analysis. Furthermore, several unreported flavonoids such as apigenin, vitexin, luteolin, etc., have been detected in the extracts from A. grossedentata stems, according to "Supercritical Carbon Dioxide Extraction of Bioactive Compounds from Ampelopsis grossedentata Stems: Process Optimization and Antioxidant Activity" by Wang Y, Ying L, Sun D, Zhang S, Zhu Y, Xu P.(6)

7. Apoptotic Effects
In the analyzing the molecular mechanism of these compounds (genistein, biochanin-A and apigenin) in PC-3 (hormone-independent/p53 mutant type) and their anti prostate cancer effect
found that apoptosis of prostate cancer cells was associated with p21 up-regulation and PLK-1 suppression. Exposure of genistein, biochanin-A and apigenin on LNCaP (hormone-dependent/p53 wild type) and PC-3 (hormone-independent/p53 mutant type) prostate cancer cells resulted in same pattern of cell cycle arrest and apoptosis, according to "Apoptotic Effects of Genistein, Biochanin-A and Apigenin on LNCaP and PC-3 Cells by p21 through Transcriptional Inhibition of Polo-like Kinase-1" by Seo YJ, Kim BS, Chun SY, Park YK, Kang KS, Kwon TG.(7)

8. Atherosclerosis (AS)
In the identification of Twenty-three flavonoids categorized into flavones, flavonols, isoflavones, and flavanones, including apigenin and theirs vascular endothelial dysfunction effect found that the effective agents in inhibiting endothelial dysfunction include myricetin, quercetin, luteolin, apigenin, genistein and daidzein. Our work might provide some evidence for atherosclerosis (AS) prevention and a strategy for the design of novel AS preventive agents, according to "Chemical Structures of 4-Oxo-Flavonoids in Relation to Inhibition of Oxidized Low-Density Lipoprotein (LDL)-Induced Vascular Endothelial Dysfunction" by Yi L, Jin X, Chen CY, Fu YJ, Zhang T, Chang H, Zhou Y, Zhu JD, Zhang QY, Mi MT.(8)

9. Hepatoprotective activity
In the demonstratyion of four known flavonoids were isolated (scutellarein 6-methyl ether, dihydroquercetin, apigenin 7-O-glucoside, and apigenin-7-neohesperidoside), from the bulbs of P. michuacana and theirs hepatoprotective effect found that Compounds 1, 4, and 5 were found to exhibit good hepatoprotective effect. These effects were comparable to that of the standard drug silymarin, a well-known hepatoprotective agent according to "Effect of flavonoids from Prosthechea michuacana on carbon tetrachloride induced acute hepatotoxicity in mice" Perez Gutierrez RM, Anaya Sosa I, Hoyo Vadillo C, Victoria TC.(9)

10. Lung cancer
in the observation of Apigenin and its effect in significantly suppressed the proliferation of four types of human lung cancer cells found that apigenin widely inhibits cell proliferation of various lung cancer cell lines in a dose-dependent manner and the combination treatment of apigenin and antitumor drugs is very effective in human lung cancer cells, and Nrf2-ARE pathway may contribute to the mechanism, according to "[Anti-proliferation and chemo-sensitization effects of apigenin on human lung cancer cells].[Article in Chinese]' by Ren HY, Tang XW(10)

11. Oral cancer
In the evaluation of apigenin and it effect in hamster buccal pouch carcinogenesi found that that apigenin might have inhibited oral carcinogenesis by improving the status of antioxidant defense mechanism and modulated the activities of phase I and phase II detoxification cascade toward increased excretion of active metabolite of DMBA, during DMBA induced hamster buccal pouch carcinogenesis, according to "Chemopreventive potential of apigenin in 7,12-dimethylbenz(a)anthracene induced experimental oral carcinogenesis' by Silvan S, Manoharan S, Baskaran N, Anusuya C, Karthikeyan S, Prabhakar MM.(11)

12. Antiviral Activity
in the observation of C-glycosides, luteolin 6- C- α-L-arabinopyranosyl-7- O- β-D-glucopyranoside ( 1), apigenin 6- C- β-D-galactopyranosiduronic acid (1 → 2)- α-L-arabinopyranoside ( 2), luteolin 6- C- β-D-galactopyranosiduronic acid (1 → 2)- α-L-arabinopyranoside ( 3), and luteolin 6- C- β-D-glucopyranosiduronic acid (1 → 2)- α-L-arabinofuranoside ( 4) from the Leaves of Lophatherum gracile and their antiviral activity found that the flavone were screened for their IN VITRO antiviral activity against respiratory syncytial virus (RSV) with cytopathic effect (CPE) reduction assay, and several flavone 6- C-monoglycosides showed potent IN VITRO anti-RSV effect, according to "Flavone C-glycosides from the Leaves of Lophatherum gracile and Their In Vitro Antiviral Activity" by Wang Y, Chen M, Zhang J, Zhang XL, Huang XJ, Wu X, Zhang QW, Li YL, Ye WC.(12)

13. Haemostasis
In the evaluation of isolation of apigenin (1), apigenin-7-O-glucoside or cosmosiin (2), apigenin-7-O-apiosyl-(1 --> 2)-O-glucoside or apiin (3) and the coumarin 2",3"-dihydroxyfuranocoumarin or oxypeucedanin hydrate (4) of the aqueous extract (Pc) of Petroselinum crispum (Mill) leaves and theirs effect on haemostasis found that Pc, apigenin and cosmosiin interfere on haemostasis inhibiting platelet aggregation, according to "Phenolic chemical composition of Petroselinum crispum extract and its effect on haemostasis" by Chaves DS, Frattani FS, Assafim M, de Almeida AP, de Zingali RB, Costa SS.(13)

14. Etc.
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Sources
(1) http://www.ncbi.nlm.nih.gov/pubmed/22113421
(2) http://www.ncbi.nlm.nih.gov/pubmed/22098587
(3) http://www.ncbi.nlm.nih.gov/pmc/articles/PMC2874462/
(4) http://www.ncbi.nlm.nih.gov/pubmed/20511675
(5) http://www.ncbi.nlm.nih.gov/pubmed/22084167
(6) http://www.ncbi.nlm.nih.gov/pubmed/22072923
(7) http://www.ncbi.nlm.nih.gov/pubmed/22065906
(8) http://www.ncbi.nlm.nih.gov/pubmed/22016603
(9) http://www.ncbi.nlm.nih.gov/pubmed/22014261
(10) http://www.ncbi.nlm.nih.gov/pubmed/21984153
(11) http://www.ncbi.nlm.nih.gov/pubmed/21970806
(12) http://www.ncbi.nlm.nih.gov/pubmed/21870321
(13) http://www.ncbi.nlm.nih.gov/pubmed/21834233