Studies On The Chemical Composition And Bioactivitics Of The Representative Species From Zingiberaceae

Many plants in Zingiberaceae family have both flavoring and medicinal properties, such as Amomumvillosum Lour, Amomum tsao-ko Crevoster Lemarie, Alpinia oxyphylla Miq, Zingiber officinale Rosc,Curcuma longa L., Curcuna phaeocaulis Val, Curcuma wenyujin Y.H. Chen et C. Ling, et al., and werewidely used.Firstly, fourteen Zingiberaceae species, widely used in China both for food and medicine, wereselected to evaluate and compare their antioxidant, antimicrobial and anti-tumor activities by radicalscavenging assay, reducing power measurement experiment, plate diffusion method and MTT assay,respectively. Results of antioxidant activity indicated that A. galangal, A. tsao-ko, A. villosum and C.longa displayed significant activity in DPPH radical scavenging and reducing power assays, while A.galangal, A. officinarum, A. oxyphylla, A. tsao-ko, A. villosum, C. longa and Z. officinale showedsignificant hydroxyl radical scavenging capacity. Antimicrobial active results showed that A. galangal,A. katsumadai, A. officinarum, A. oxyphylla, A. villosum and C. wenyujin have different degreesantimicrobial activities （MICs were between2.00to40.00μg/ml）. A. kravanh and C. longa exhibitedsignificant cytotoxicity against SMMC-7721cell line. A. galangal, A. katsumadai, A. officinarumand andA. oxyphylla showed moderate inhibition.Secondly, further radical scavenging capacity, anti-inflammatory, chem-protective and anti-tumoractivities of A. tsao-ko, A. galangal, and C. phaeocaulis and their fractions （petroleum ether,ethyl acetate water-soluble fractions） were evaluated. The ethanol extract of A. tsao-kodisplayed broader activities in four models. In particular, it displayed significant free radicalscavenging and anti-inflammatory activities, and its ethyl acetate fraction could berecognized as the antioxidant and anti-inflammatory fraction. In addition, its ethyl acetatefraction also shows the chem-protective effect and anti-tumor activity, and the petroleumether fraction showed moderate anti-tumor activity. The ethanol extract of A. galangaldisplayed significant anti-tumor activity and moderate radical scavenging activity. Itspetroleum ether fraction and ethyl acetate fraction were its anti-tumor active fractions.However, it displayed no significant anti-inflammatory or chem-protective effect. Theethanol extract of C. phaeocaulis showed significant chemical protective effect, and its ethylacetate fraction was the active fraction.By various chromatographic separation methods,12compounds （including fourflavonoids, four diphenylheptane, two steroidal, a polyphenols and an aldehyde） were isolatedfrom the ethyl acetate fraction of the A. tsao-ko. Among of them, two was newdiphenylheptane and tree constituents were first isolated from this plant. From the ethylacetate fraction of the A. galangal,7compounds were isolated, one of them was new diterpene and one was obtained for the first time from A. galangal. A new diphenylheptanol,together with two known diphenylheptanols were isolated from the ethyl acetate fraction of C.phaeocaulis.The anti-oxidant, anti-inflammatory, chem-protection and anti-tumor activities of theisolated compounds were assayed, respectively. The results of anti-oxidant activity indicatedthat the quercetin, epicatechin, catechol and diphenylheptanols were the active ingredient of A.tsao-ko, wherein, the quercetin and Vc showed considerable radical scavenging capacity. Andp-acrolein hydroxybenzaldehyde and benzebeacrolein derivatives were the anti-oxidant activeingredients of A. galangal, however, sesquiterpene or diterpenoids displayed no significantantioxidant activity.The anti-inflammatory results showed that the epicatechin and CG-5were the majoranti-inflammatory active ingredients of A. tsao-ko. More than40%NO release could besuppressed by epicatechin or CG-5at dose≥80μg·ml^-1.CG^-1,5and11, isolated from A. tsao-ko, showed significant chemical protective effects,at dose≥80μg·ml^-1, they could significantly improve the survival rate of the PC^-12cells（≥60%）. EZ-3, isolated from C. phaeocaulis, was also displayed significant chemicalprotective effect, at concentrations≥20μg·ml^-1, the survival rate of PC^-12cells was more then54.7%. At dose≥30μg·ml^-1, EZ^-1 and2also showed significant protective effect, viability ofthe pretreatmented cell increased to54.5-78.6%and56.3-70.6%, respectively.CG-8isolated from A. tsao-ko showed a selective inhibition to Hela cell line, whenconcentrations≥20μg·ml^-1, the inhibition rate to Hela cells>50%, but to other three celllines were less then50%. CG-6showed better inhibition to SMMC-7721cells. Atconcentration≥40μg·ml^-1, the inhibition rate of CG-6to SMMC-7721cell line was morethan50%, while at the highest experimental concentration, the inhibition rate was more than80%. Seven compounds from A. galangal displayed a different degree anti-tumor activity in adose-dependent manner. The HDK^-1,2,4and5showed higher inhibition then the HDK-3,6an7. At concentration of100μg·ml^-1the inhibition rates of HDK^-1,2,4and5were>60%.While the concentration≥25μg·ml^-1, the inhibition rates of HDK-2and4were49.6%and47.9%, respectively.