DrugDiscoveryandNaturalProductsItmaybearguedthatdrugdiscoveryisarecentconceptthatevolvedfrommodernscienceduringthe20thcentury,butthisconceptinrealitydatesbackmanycenturies,andhasitsoriginsinnature.Onmanyoccasions,humanshaveturnedtoMotherNatureforcures,anddiscovereduniquedrugmolecules.Thus,thetermnaturalproducthasbecomealmostsynonymouswiththeconceptofdrugdiscovery.Inmodemdrugdiscoveryanddevelopmentprocesses,naturalproductsplayanimportantroleattheearlystageof"lead"discovery,i.e.discoveryoftheactive(determinedbyvariousbioassays)naturalmolecule,whichitselforitsstructuralanaloguescouldbeanidealdrugcandidate.1.origin[5rid3in]n・起点，端点；来源；出身，血统2.Synonymous[si'nonms]adj.同义的，类义的.3.i.e.[,ai'i:]＜拉〉abbr.(=idest)即，换言之.4.candidate['k&ndidit]n・申请求职者，候选人；报考者；候选物.有人可能认为药物发现是一个 20 世纪才出现的、来源于现代科学的新概念,但是事实上这个概念是源于自然界的，可以追溯到许多个世纪以前。过去，人们常常向自然母亲寻求帮助，并且找到了分子结构独特的药物。在那时，天然产物几乎是药物发现的同义词。天然产物在现代药物发现和开发过程中也发挥着重要的作用，即作为天然活性化合物(通过各种生物检定方法)的来源，而天然活性化合物或者其结构类似物可能是很好的候选药物。Naturalproductshavebeenenormoussourceofdrugsanddrugleads.Itisestimatedthat61percentofthe877small-molecularnewchemicalentitiesintroducedasdrugsworldwideduring1981-2002canbetracedbacktoorweredevelopedfromnaturalproducts.Theseincludenaturalproducts(6percent),naturalproductderivatives(27percent),andsyntheticcompoundswithnatural-product-derivedpharmacophores(5percent)andsyntheticcompoundsdesignedonthebasisofknowledgegainedfromanaturalproduct,i.e.anaturalproductmimic(23percent).Insometherapeuticareas,thecontributionofnaturalproductsisevengreater,e.g.about78percentofantibacterialsand74percentofanticancerdrugcandidatesarenaturalproductsorstructuralanaloguesofnaturalproducts.In2000,approximately60percentofalldrugsinclinicaltrialsforthemultiplicityofcancerswereofnaturalorigins.In2001,eight(simvastatin,...
