藥學(xué)專業(yè)畢業(yè)論文外文翻譯---姜黃素及其天然、合成的類似物的生物活性研究進(jìn)展（英文）

1、Biological activities of curcumin and its analogues(Congeners) made by man and Mother NaturePreetha Anand a, Sherin G. Thomas b, Ajaikumar B. Kunnumakkara a, Chitra Sundaram a, Kuzhuvelil B. Harikumar a, Bokyung Sung a,

2、Sheeja T. Tharakan a, Krishna Misra c, Indira K. Priyadarsini d, Kallikat N. Rajasekharan b, Bharat B. Aggarwal a,*a Cytokine Research Laboratory, Department of Experimental Therapeutics, Unit 143, The University of Texa

3、s M.D. Anderson Cancer Center,1515 Holcombe Boulevard, Houston, TX 77030, USAb Department of Chemistry, University of Kerala, Thiruvananthapuram, Indiac Bio-informatics division, Indian Institute of Information Technolog

4、y, Allahabad, Indiad Radiation and Photochemistry Division, Bhabha Atomic Research Centre, Mumbai-400085, India1. IntroductionCurcumin, commonly called diferuloyl methane, is a hydro-phobic polyphenol derived from the rh

5、izome (turmeric) of theherb Curcuma longa. Turmeric has been used traditionally formany ailments because of its wide spectrum of pharmacolo-gical activities. Curcumin has been identified as the activeprinciple of turmeri

6、c; chemically, it is a bis-a, b-unsaturatedb-diketone that exhibits keto-enol tautomerism. Curcuminhas been shown to exhibit antioxidant, anti-inflammatory,antimicrobial, and anticarcinogenic activities. It also hashepat

7、oprotective and nephroprotective activities, suppressesthrombosis, protects against myocardial infarction, and hashypoglycemic and antirheumatic properties. Moreover, cur-cumin has been shown in various animal models and

8、 humanstudies to be extremely safe even at very high doses [1–12]. Inb i o c h e m i c a l p h a r m a c o l o g y 7 6 ( 2 0 0 8 ) 1 5 9 0 – 1 6 1 1a r t i c l e i n f oArticle history:Received 27 June 2008Accepted 7 Aug

9、ust 2008Keywords:CurcuminSynthetic analoguesBioavailabilityLiposomesNanoparticlesa b s t r a c tCurcumin, a yellow pigment present in the Indian spice turmeric (associated with currypowder), has been linked with suppress

10、ion of inflammation; angiogenesis; tumorigenesis;diabetes; diseases of the cardiovascular, pulmonary, and neurological systems, of skin, andof liver; loss of bone and muscle; depression; chronic fatigue; and neuropathic

11、pain. Theutility of curcumin is limited by its color, lack of water solubility, and relatively low in vivobioavailability. Because of the multiple therapeutic activities attributed to curcumin, how-ever, there is an inte

12、nse search for a ‘‘super curcumin’’ without these problems. Multipleapproaches are being sought to overcome these limitations. These include discovery ofnatural curcumin analogues from turmeric; discovery of natural curc

13、umin analogues madeby Mother Nature; synthesis of ‘‘man-made’’ curcumin analogues; reformulation of curcu-min with various oils and with inhibitors of metabolism (e.g., piperine); development ofliposomal and nanoparticle

14、 formulations of curcumin; conjugation of curcumin prodrugs;and linking curcumin with polyethylene glycol. Curcumin is a homodimer of feruloyl-methane containing a methoxy group and a hydroxyl group, a heptadiene with tw

15、o Michaelacceptors, and an a,b-diketone. Structural homologues involving modification of all thesegroups are being considered. This review focuses on the status of all these approaches ingenerating a ‘‘super curcumin.’’.

16、# 2008 Elsevier Inc. All rights reserved.* Corresponding author. Tel.: +1 713 7921817; fax: +1 713 7456339.E-mail address: aggarwal@mdanderson.org (B.B. Aggarwal).available at www.sciencedirect.comjournal homepage: www.e

17、lsevier.com/locate/biochempharm0006-2952/$ – see front matter # 2008 Elsevier Inc. All rights reserved.doi:10.1016/j.bcp.2008.08.008diketone link. In this molecule, the a,b-unsaturated b-diketone moiety of curcumin is re

18、placed by an a,b-unsatu-rated dihydropyranone moiety. To date, not many biologicalstudies on cyclocurcumin have been reported; in one study,Simon et al. [14] reported that this analogue was ineffective ininhibiting MCF-7

19、 tumor cell proliferation and arrest of cellcycle progression.In the last few decades, efforts have been made to isolatecurcuminoids from different sources, including Curcuma longa,Curcuma zedoaria, and Curcuma aromatica

20、. Several researchgroups have investigated and compared their antioxidant,cardioprotective, neuroprotective, antidiabetic, antitumor,and chemopreventive activities, employing them eitherindividually or as mixtures. The c

21、urcuminoids have beenshown to be scavengers of free radicals and reactive oxygenspecies (ROS), such as hydroxyl radicals, superoxide radicals,singlet oxygen, peroxyl radicals, and peroxynitrite, whoseproduction is implic

22、ated in the induction of oxidative stressTable 1 – Activities of curcumin analogues derived from turmeric and of curcumin metabolites? BDMC is more active than DMC or curcumin for cytotoxicity against ovarian cancer cell

23、s [32]? BDMC is less active than curcumin or DMC as an antioxidant and as an oxidative DNA cleaving agent [15]? BDMC is less active than curcumin or DMC as an inhibitor of peroxynitrite scavenger [16]? BDMC was most acti

24、ve when compared with DMC or curcumin for antimutagenic and anticarcinogenic activity [31]? BDMC is more active than curcumin or DMC for antitumor and antioxidant activity [24]? BDMC is more active than curcumin or DMC f

25、or suppression of carcinogenesis [31]? BDMC was more active than curcumin for reducing nicotine-induced oxidative stress [121]? BDMC improved innate immunity and transcription of MGAT-III and Toll-like receptors in AD pt

26、s [29]? BDMC is more active than curcumin for modulation of MDR1 gene [58]? BDMC is less active than curcumin or DMC in inhibiting singlet oxygen-induced DNA damage [18]? BDMC is less active than curcumin or DMC in bindi

27、ng and inhibiting Pgp and sensitizing cells to vinblastin [35]? BDMC is less active than curcumin or DMC in binding and inhibiting MRP1 and sensitizing cells to etoposide [37]? BDMC was more active than curcumin or DMC i

28、n protecting nerve and endothelial cells from beta amyloid-induced oxidative stress [27]? BDMC prevents DMH induced colon carcinogenesis [67]? BDMC is as active as curcumin in preventing DMH induced colon carcinogenesis

29、[36]? BDMC is more active than curcumin in preventing alcohol and PUFA-induced oxidative stress [99]? BDMC is more active than curcumin in preventing CCL4-induced hepatotoxicity in rats [122]? BDMC is more active than cu

30、rcumin in preventing alcohol and PUFA-induced cholesterol, TGs, PLs and FFA [104]? BDMC, curcumin, and DMC exhibit equivalent activity in suppression of blood glucose levels in diabetic mice through binding to PPAR-g [25

31、]? BDMC is less active than curcumin and DMC in protecting rats from lead-induced neurotoxicity [28]? BDMC is less active than curcumin and DMC in suppressing NF-kB activation [30]? BDMC is more active than DMC or curcum

32、in in inducing NRF2-mediated induction of heme oxygenase-1 [36]? BDMC is least active than DMC or curcumin in inducing p38 MAPK mediated induction of heme oxygenase-1 [23]? BDMC is least active than DMC or curcumin in in

33、hibiting H2O2-induced lipid peroxidation and hemolysis of eythrocytes [21]? BDMC is least active than DMC or curcumin in inhibiting the proliferation of VSMC induced by ox-LDL and induction of LDL-R [21]? BDMC is least a

34、ctive than DMC or curcumin in inhibiting the liposomal peroxidation; and of COX1 and COX2 activity [20]? DMC is more potent than curcumin, BDMC and cyclocurcumin in inhibiting proliferation of breast cancer cells [14]? D

35、MC is more potent than curcumin and BDMC in inducing nematocidal activity [13]? THC is less potent than curcumin in inhibiting the activity of 5-LOX; but more potent than curcumin in inhibiting COX-dependentarachidonic a

36、cid metabolism [60]? THC is more active than curcumin in preventing DMH-induced ACF formation in mice [61]? THC does not induces ROS production and membrane mobility coefficient but curcumin does [185]? THC is less activ

37、e than curcumin in preventing PMA-induced skin tumor promotion in mice [33]? THC is more active than curcumin as an antioxidant [39]THC is less active than curcumin as an antioxidant [186]? THC is less active under aerat

38、ed condition than curcumin but under N2O purged conditions, THC is more active than curcumin insuppressing radiation-induced lipid peroxidation [41]? THCwas less active than curcumin, DMC or BDMC in suppressing NF-kB act

39、ivation [30]? THC, HHC, OHC are less active than curcumin in suppressing NF-kB activation [59]? THC is more active than curcumin in suppressing nitrilotriacetate-induced oxidative renal damage [43]? THC is more active th

40、an curcumin in protecting from chloroquine-induced hepatotoxicity in rats [45]? THC is more active than curcumin in preventing brain lipid peroxidation in diabetic rats [51]? THC is more potent than curcumin for antioxid

41、ant and antidiabetic effects in rats [48]? THC is more potent than curcumin for modulation of renal and hepatic functional markers in diabetic rats [56]? THC is more potent than curcumin for modulation of blood glucose,

42、plasma insulin and erythrocyte TBARS in diabetic rats [55]? THC is more potent than curcumin in decreasing blood glucose and increasing plasma insulin in diabetic rats [50]? THC is less potent than curcumin in modulation

43、 of ABC drug transporters [58]? THC’s effect was comparable with curcumin on reduction of accummulation and cross-linking of collagen in diabetic rats [53]? THC exhibits stronger antioxidant activity than HHC OHC > cu

44、rcumin > DMC > BDMC [17]? THC was more potent than curcumin in suppressing LDL oxidation [42]? THC is more active than curcumin in suppressing lipid peroxidation of erythrocyte membrane ghosts [40]? Cyclocur exhibi

45、ts week anticancer activity [14]Note: BDMC, bisdemethoxycurcumin; COX, cyclooxygenase; DMC, demethoxycurcumin; HHC, hexahydrocurcumin; LDL, low-densitylipoproteins; NF-kB, nuclear factor kappa B; OHC, octahydrocurcumin;