TheprofessionalEnglishofpharmaceuticalengineeringWangXinliangEastChinauniversityofscienceandtechnology13.02.2012FinalexaminationTwoparts:gradeofdailystudy(30%)attendanceratehomeworkothers(exercise,middleexamination)gradeoffinalexamination(70%)ThecontentofexaminationThecontentofexaminationDegreetest

50%basicEnglish

50%professionalEnglish

word:translationfromEnglishtoChinese(5points)translationfromChinesetoEnglish(5points)Translation:(40points)4paragraphswhichincludeabout250wordsineachofthem.payattentiontoonly125to150wordsineachparagraphneedtobetranslated.These4paragraphsarenotsimplesentence.HowtolearntheprofessionalEnglishMastersomeskillsMasterthenecessaryknowledgeWhatisthemostimportantthingmorereading,morespeaking,morewritingWhatistheimportantthinginthiscourseremembertheword?translatesentencebysentence?learnmoreprofessionalknowledge?YoudaoDict有道詞典HowtoteachtheprofessionalEnglishCrocinyellow（藏花素）,whichisextractedfromGardeniajasminoidesEllis（梔子）,iswidelyusedasanaturalfoodcolorantinAsiancountries,whileGardeniaextracthasbeenusedinChinesetraditionalmedicine(CTM)forcuringanumberofailments[3].Thesecrocetin（藏紅花酸）derivatives,whicharedifferentfrommostfamiliesofcarotenoids（類胡蘿卜素）,areknownfortheircoloringpropertiesowingtotheirpeculiarwater-solublebehavior[4].Numerousstudieshavedealtwiththecomponentstructuresofyellowpigmentextractsisolatedfromgardeniafruits[4–8],theirspectroscopiccharacterizationandradical-scavengingactivity[4,9],dataconcerningtheconcentrationofmajorcomponentsforthedeterminationofoptimaltimeofharvestandextractionprocess[10,11].ThecontentofthiscourseIntroducesomeskillsoftranslationanddosomeexerciseintheclassroom.SummarizesomeregulationsintheprofessionalEnglish.Learnthetext.Discusssometopics.Part1MedicinalchemistryUnit1ProductionofDrugsThewholeconceptoftheproductionofdrugsTheclassificationofthedrugsTheintroductionofeachgroupofdrugs

Thefirstquestion:howtoclassifythedrugDependingonthekindsofdisease:CardiovasculardrugsDigestivesystemdrugsRespiratorysystemdrugsAntiviraldrugsProprietarydrugsorGenericdrugsDependingontheproductionororigin:藥品的生產依據其生產或來源，藥物制劑可以分為三類：I.完全的合成材料（人工合成材料），II.天然產物，和III.源自部分合成的產品（半合成產品）。

Dependingontheirproductionororiginpharmaceuticalagentscanbesplitintothreegroups:I.Totallysyntheticmaterials(synthetics)，II.Naturalproducts，andIII.Productsfrompartialsyntheses(semi-syntheticproducts).Unit1ProductsofDrugsWordssyntheticsglycoside(s)hydrolysatedextrantargetedmodificationEpinephrineLevodopaProstaglandinsD-PenicillamineVincamineEukaryontProkaryontLeuconostocmesenteroidesCorynebacteriumglutamicumBrevibacteriumflavumPropionibacteriumshermaniipurinanucleotidecitricacidmonosodiumL-glutamatechromatinn.[用作復]人工合成(絕緣)材料n.配醣；配糖體；糖苷n.水解液；水解產物n.葡萄聚糖；右旋糖酐定向（或靶向）修飾n.腎上腺素n.[藥]左旋多巴（等于L-dopa）n.前列腺素（prostaglandin的復數形式）n.D-青霉胺n.長春胺n.真核細胞n.原核細胞腸膜狀明串珠菌谷氨酸棒桿菌黃色短桿菌謝氏丙酸桿菌嘌呤核苷（酸）檸檬酸谷氨酸鈉（味精）n.核染色質；核染質AlkalimetalLilithiumNasodiumKpotassiumRbrubidiumCscaesiumFrfranciumHhydrogen本書的重點是在于Ⅰ和Ⅲ類中最重要的化合物——藥物合成。但是，這并不意味著，天然產品或其他制劑并不太重要。它們可以作為有價值的先導結構，他們常常作為重要的合成產品的起始原料或中間體產品。

表1列出了獲取藥物制劑的不同方法的概述。

TheemphasisofthepresentbookisonthemostimportantcompoundsofgroupsIandⅢ-thusDrugsynthesis.Thisdoesnotmean，however，thatnaturalproductsorotheragentsarelessimportant.Theycanserveasvaluableleadstructures，andtheyarefrequentlyneededasstartingmaterialsorasintermediatesforimportantsyntheticproducts.Table1givesanoverviewofthedifferentmethodsforobtainingpharmaceuticalagents.

最初從天然資源庫獲得的幾個重要治療作用的天然產品，今天可以通過全合成更有效地，例如更經濟地被制備出來。這樣的例子包括L-氨基酸、氯霉素、咖啡因、多巴胺、腎上腺素、左旋多巴、肽類激素、前列腺素、D-青霉胺、長春胺，以及幾乎所有的維生素。

Severaltherapeuticallysignificantnaturalproductswhichwereoriginallyobtainedfromnaturalsourcesaretodaymoreeffectively-i.e.moreeconomically-preparedbytotalsynthesis.SuchexamplesincludeL-aminoacids,Chloramphenicol,Caffeine,Dopamine,

Epinephrine,Levodopa,peptidehormones,Prostaglandins,D-Penicillamine,Vincamine,

andpracticallyallvitamins.

在過去的幾年里，發酵，即微生物過程，變得極其重要。通過現代技術和基因選擇導致的微生物的高性能突異變種的結果，發酵已成為選擇寬范圍物質的方法。真核細胞（酵母菌和霉菌）和原核細胞（單細胞細菌，放線菌）都可用作微生物。可以得到下列產品類型：

Overthelastfewyearsfermentation-i.e.microbiologicalprocesseshasbecomeextremelyimportant.Throughmoderntechnologyandresultsfromgeneticselectionleadingtothecreationofhighperformancemutantsofmicroorganisms,fermentationhasalreadybecomethemethodofchoiceforawiderangeofsubstances.BothEukaryonts(yeastsandmoulds)andProkaryonts(singlebacterialcells,andactinomycetes)areusedmicroorganisms.Thefollowingproducttypescanbeobtained:

盡管從諸如腸膜狀明串球菌的某些微生物的黏膜可以生產葡萄聚糖，但第2和3類產品類型只與藥品生產的有關。葡聚糖自身的分子量5萬?10萬，可用作血漿代用品。而來自谷氨酸棒桿菌和黃色短桿菌突變體的初級代謝產物中，L-氨基酸尤其令人感興趣。從這些生物體中，可以生產約35萬噸L-谷氨酸單鈉鹽（味精，食品添加劑）和約70,000噸L-賴氨酸（用于植物蛋白補充物質）。此外，重要的初級代謝產物還有嘌呤核苷酸、有機酸、乳酸、檸檬酸和維生素，例如源自謝氏丙酸桿菌的維生素B12。

Disregardingtheproductionofdextranfromthemucousmembranesofcertainmicroorganisms，e.g.Leuconostocmesenteroides,classes2and3

are

therelevantonesforthepreparationofdrugs.Dextranitself,withamolecularweightof50,000~100,000,isusedasabloodplasmasubstitute.AmongtheprimarymetabolitestheL-aminoacidsfrommutantsofCorynebacteriumglutamicum

andBrevibacteriumflavum

areespeciallyinteresting.Fromtheseorganismssome350,000tonesofmonosodiumL-glutamate(foodadditive)andsome70,000tonesofL-lysine(supplementforvegetableproteins)areproduced.Furtherimportantprimarymetabolitesarethepurinanucleotides,organicacids,

lacticacid,citricacid,andvitamins,forexamplevitaminB12fromPropionibacteriumshermanii.

在次生代謝產物中首先必須提到的是抗生素。以下五組藥品代表了全球每年價值170億美元：

青霉素類（產黃青霉），

頭孢菌素類（頂頭孢霉菌），

四環素類（金霉素鏈霉菌），

紅霉素類（紅霉素鏈霉菌），

氨基糖苷（如來自灰色鏈霉菌的鏈霉素）。

Amongthesecondarymetabolitestheantibioticsmustbementionedfirst.ThefollowingfivegroupsrepresentayearlyworldwidevalueofUS-$17billion:penicillins(Penicilliumchrysogenum)，cephalosporins(Cephalosporiumacremonium)，tetracyclines(Streptomycesaureofaciens)，erythromycins(Streptomyceserythreus)，aminoglycosides(e.g.streptomycinfromStreptomycesgriseus).Dextranisapolymerofglucose.Itisawhitepowderanditissolubleinwaterandinsolubleinethanol.Dextrancanincreasetheplasmavolumeandmaintainthebloodpressure,soitcanbeusedforasabloodplasmasubstitute.Itcanbeproducedbyfermentationofsucroseinleuconostocmesenteroides.Certainly,thefermentationonlyproducetherawmaterialandthesomepurificationisnecessary.

ThesimpleintroductionofdextranMolecularformula:（C6H10O5）nglucose葡萄糖fructose果糖

mono-,di-,tri-,polymer單體，二聚體，三聚體，聚合體(物)sucrosen.蔗糖

從微生物中已分離出約5000種抗生素，但其中只有不到100種有治療用途。但是，必須記住，許多衍生物已通過部分合成法來修飾以獲得治療用途；在過去的十年里，采用半合成方法已從?-內酰胺獲得了約50,000種制劑。發酵是在體積高達400m3的不銹鋼發酵罐中進行。為了避免受到噬菌體等微生物的污染，（發酵）全過程都必須在無菌條件下進行。由于更重要的是，發酵只在有氧條件下才能發生；因此，需要提供有足夠量的（無菌）氧氣或空氣。二氧化碳的來源包括糖類（碳水化合物），如廢糖漿、低聚糖類和葡萄糖。

About5000antibioticshavealreadybeenisolatedfrommicroorganisms,butoftheseonlysomewhatfewerthan100areintherapeuticuse.Itmustberemembered，however，thatmanyderivativeshavebeenmodifiedbypartialsynthesisfortherapeuticuse;some50,000agentshavebeensemisyntheticallyobtainedfrom?-lactamsaloneinthelastdecade.Fermentationsarecarriedoutinstainlesssteelfermentorswithvolumesupto400m3.Toavoidcontaminationofthemicroorganismswithphagesetc.thewholeprocesshastobeperformedundersterileconditions.Sincethemoreimportantfermentationsoccurexclusivelyunderaerobicconditions,agoodsupplyofoxygenorair(sterile)isneeded.Carbondioxidesourcesincludecarbohydrates,e.g.molasses,saccharides,andglucose.Wordsammonium（ammonia）aminesodiumbicarbonatesodiumhydroxidehydrochloric/sulfuric/nitricacidhypochloritechloritechlorate

perchloratenitritenitratesulfidesulfitesulfate

persulfatephosphitehypophosphite

phosphatedihydrogenphosphatehydrogenphosphate銨；銨鹽（氨；氨水）胺碳酸氫鈉；小蘇打、NaHCO3氫氧化鈉、NaOH鹽酸；硫酸；硝酸次氯酸鹽（酯）亞氯酸鹽（酯）氯酸鹽（酯）高氯酸鹽（酯）亞硝酸鹽（酯）硝酸鹽（酯）硫化物；硫醚亞硫酸鹽（酯）硫酸鹽（酯）過硫酸鹽（酯）亞磷酸鹽（酯）次磷酸鹽（酯）磷酸鹽（酯）磷酸二氫鹽磷酸一氫鹽Prefix----------Parent-----------SuffixNomenclatureofparentpart:NomenclatureofalkanesandalkylsubstituentsStraight-chainalkanes

Straight-chainalkanesarenamedbycountingthenumberofcarbonatomsinthechainandaddingthefamilysuffix-ane.Thuspentaneisthefive-carbonalkane,andhexaneisthesix-carbonalkane.NomenclatureofOrganicCompounds1Analkylsubstituent(oranalkylgroup)isanalkanefromwhichasinglehydrogenhasbeenremoved.Alkylsubstituentsarenamedbyreplacingthe“ane”suffixofthealkanewith“yl”.Theletter“R”isusedtoindicateanyalkylgroup.ThusCH3-hasthenameofmethyl,whilethegroupofCH3CH2-wasnamedethyl.NumberMolecularNameNameinAlkylofcarbonsformulaChinesesubstituents1 CH4 Methane

甲烷

Methyl

2 C2H6 Ethane

乙烷

Ethyl3 C3H8 Propane

丙烷

Propyl4 C4H10 Butane

丁烷

Butyl5 C5H12 Pentane

戊烷

Pentyl6 C6H14 Hexane

己烷

Hexyl7C7H16 Heptane

庚烷

Heptyl8 C8H18 Octane

辛烷

Octyl9 C9H20 Nonane

壬烷

Nonyl10 C10H22 Decane

癸烷

Decyl11 C11H24Undecane

十一烷

Undecyl12 C12H26 Dodecane

十二烷

Dodecyl13 C13H28 Tridecane

十三烷

Tridecyl20 C20H42Icosane

二十烷

Icosyl

21 C21H44Heneicosane

二十一烷

Heneicosyl30 C30H62 Triacontane

三十烷

TriacontylBranched-chainalkanes3-ethyl-3-methylhexane

SomeusefulprefixesforindicatingthenumberofsubstituentgroupsMono-

單取代,一取代Di-

二取代Tri-

三取代Tetra-

四取代Pent(a)-

五取代Hex(a)-

六取代Hept(a)-

七取代Oct(a)-

八取代Nona-

九取代Deca-

十取代2,6-dimethyloctanenot2-ethyl-6-methylheptane3-ethyl-2-methylhexanenot3-isopropylhexaneSomeusefulprefixesusedtonamebranchedalkanes(Commonnames)(normal)n- 正(isomer)iso- 異neo- 新primary 伯，一級(secondary)sec-仲，二級(tertiary)tert- 叔，三級quaternary 季，四級

n-pentaneneopentaneisobutane正戊烷新戊烷異丁烷

Pentane2,2-dimethylpropane2-methylpropanetert-butanoliso-butanamine

sec-butanamine叔丁醇異丁胺仲丁胺2-methyl-2-propanol2-methylpropanamine1-methylpropanamine

Theunivalentradicalderivedfromacyclicalkeneoralkynehastheendings“-enyl”or“-ynyl”,(alkenealkenyl)(alkynealkynyl),andthepositionofthedoubleortriplebondisindicatedwherenecessary.(unlikealkanealkyl)e.g.

1-propenyl2-butenyl

ethynyl2-propynylThefollowingnon-systematicnamesareretainedEthylene(乙烯）Allene（丙二烯）Acetylene（乙炔）Isoprene（異戊二烯）Vinyl（乙烯基）Allyl（烯丙基）Isopropenyl（異丙烯基）NomenclatureofacyclichydrocarbonswithtwoormoredoubleortriplebondsTwoormoredoublebonds:theendingwillbe“-adiene”,“-atriene”etc.(alkadiene)Twoormoretriplebonds:theendingwillbe“-adiyne”,“-atriyne”etc.(alkadiyne)e.g.

2-methyl-1,3-butadienepropadiene2,5-dimethyl-2,4,6-octatriene

3-ethyl-4-methyl-1,6-heptadiyneNomenclatureofmonocyclicaromatichydrocarbons

苯甲苯二甲苯苯乙烯異丙苯均三甲苯benzenetoluenexylenestyrenecumenemesitylene苯基甲苯基二甲苯基苯乙烯基異丙苯基均三甲苯基芐基PhenyltolylxylylstyrylcumenylmesitylbenzylCommonnamesretainedforthedisubstitutedbenzeneortho-,o- 鄰meta-,m- 間para-,p- 對

m-methylbenzylm-tolyl3,4-dimethylphenyl3-methylbenzyl

3-tolyl

o-styrylp-cumenyl3,5-dimethyl-4-ethylphenyl

2-styryl4-cumenyl

SomeimportantFamiliesoforganicmoleculesSaturatedhydrocarbons:suchas:Alkanes;cycloalkanes;Un-saturatedhydrocarbons:suchas:alkenes;alkynes;cycloalkenes;cycloalkynes;cycloalkadienes;cycloalkadiynes;Aromaticcompouds:benzene;biphenyl;naphthaleneandotherfusedandpolycyclicaromatichydrocarbons;Compoundswithfunctionalgroups:alkylhalides（鹵代烴）;alcohols（醇）;phenols（酚）;ethers（醚）;amines（胺）;Compoundswithfunctionalgroups:aldehydes（醛）;ketones（酮）;quinones（醌）;carboxylicacids（羧酸）;esters（酯）;acylhalides（酰鹵）;acidanhydrides（酸酐）amides（酰胺）;imides（亞胺）;

Compoundswithfunctionalgroups:

alkylhalides（鹵代烴）;alcohols（醇）;phenols（酚）;ethers（醚）;amines（胺）etc.alkylhalides R-X halogen(-halo)(-Cl,-Br,-F,-I)Alcohols R-OH hydroxygroup(-OH)Phenols Ar-OH hydroxygroup(-OH)Ethers R-O-R’ Alkoxygroup(O-R’)Amines R-NH2 aminogroup(NH2)

Alkylhalides(haloalkaneoralkyl

halide)Alkylhalidesareclassifiedasprimary,secondary,ortertiarydependingonthecarbontowhichthehalogenisattached.

Thecommonnamesofthealkylhalidesareobtainedbycitingthenameofthealkylgroupfollowedbythenameofthehalogen.(alkyl

halide)

IntheIUPACsystem,alkylhalidesarenamedassubstitutedalkanes.Thesubstitutedprefixnamesforthehalogensendin“o”(fluoro,chloro,bromo,iodo).(haloalkane)Alcohols

Thecommonnames,similartoalkylhalides,areobtainedbycitingthenameofthealkylgrouptowhichtheOHgroupisattached,followedbytheword“alcohol”.(alkyl

alcohol)

TheIUPACnameforanalcoholisobtainedbyremovingthe“e”fromthenameofthealkaneandaddingthesuffix“ol”.(alkanol)NomenclatureofalcoholsAminesarecompoundsinwhichoneormorehydrogenofammoniahavebeenreplacedbyalkylgroups.Thereareprimary,secondary,andtertiaryamines.Thisclassificationdependsonhowmanyalkylgroupsarebondedtothenitrogen.

(!!!notcarbon)NomenclatureofaminesThecommonnameofaamineisobtainedbycitingthenamesofthealkylgroupsbondedtothenitrogeninalphabeticalorder.Theentirenameiswrittenasoneword.

(alkylamine)e.g.TherearetwoIUPACapprovedwaytonameanamine.Itcanbenamedasasubstitutedalkaneusingtheprefix“amino”todesignatetheaminesubstituent.(???aminoalkane)Italsocanbeennamedwithafunctionalgroupsuffix----“amine”.The“e”attheendofthealkanenameisreplacedby“amine”.ThenamesofsubstituentsbondedtothenitrogenareprecededbyanN

(initalic)toindicatethatthesubstituentisbondedtoanitrogenratherthantoacarbon.[(N-alkyl)alkanamine]Amineswithfouralkylgroupsbondedtothenitrogen-andthereforeapositivechargeonthenitrogen-arecalledquaternaryammonium

salts.Theirnamesareobtainedbycitingthenamesofthealkylgroupsinalphabeticalorderasaprefixto“ammonium”,followedbythenameofthe

counterion.

[alkylammoniumhalide

(orhydroxideetc)]Nomenclatureofetherssymmetricaletherandasymmetricalether.e.g.Thecommonnameofanetherisobtainedbycitingthenamesofthetwoalkylsubstituents(inalphabeticalorder)followedbytheword“ether”.Thesmallestethersarealmostalwaysnamedbytheircommonnames.(alkylalkyl

ether)

TheIUPACsystemnamesanetherasanalkanethatbearsanalkoxysubstituent.Alkoxysubstituentsarenamedbyremovingthe“yl”fromthenameofthealkylsubstituentandadding“oxy”.(alkoxyalkane)methoxyethoxy1-methylethoxy1,1-dimethylpropoxy

Acarbonylgroup（羰基）

isacarbondoublybondedtoanoxygenandanacylgroup（酰基）

isacarbonylgroupattachedtoanalkylsubstituent.Abenzoylgroup（苯甲酰基）

isacarbonylgroupattachedtoabenzenering.Thecommonnameofanaldehydeisthesameascarboxylicacid(derivedfromsomeLatinwords).(Latin+aldehyde)TheIUPACnameofanaldehydeisobtainedbyremovingthe“e”fromthealkanenameandadding“-al”.(alkanal)NomenclatureofaldehydesandketonesIfthealdehydegroupisattachedtoaring,thealdehydeisnamedbyadding“carbaldehyde”tothenameofthering.(cycloalkanecarbaldehyde)phenylmethanalCommonname:Onlyafewketonshavecommonnames,suchasacetone(likealdehyde).Commonnamesarealsousedforphenyl-substitutedketones.Theyarecalledphenones.(+one)IUPACname:KetonesarenamedintheIUPACsystembyremovingthe“e”fromthealkanenameandadding“-one”.(alkanone)Derivedname:Likeethers,R-CO-R’canbenamedbycitingthenamesofthetwoalkylsubstituents(inalphabeticalorder)followedbytheword“ketone”.(alkylalkyl

ketone)NomenclatureofketonesCommonnameIUPACnameDerivednameNomenclatureofcarboxylicacidsanditsderivativesX=OH,acarboxylicacidX=halogen,anacylhalideX=OR',anesterX=OCOR',anacidanhydrideX=NRR',anamideNomenclatureofcarboxylicacids

acarboxylgroup

Thefunctionalgroupofacarboxylicacidiscalledacarboxylgroup.Long-chaincarboxylicacidsarecalled“fattyacids”.

Commonname:Carboxylicacids(<6)arefrequentlycalledbytheircommonnames.Theyarenamedbyadding“Latinprefix”before“acid”.?whatisα–carbon?

IUPACname:acarboxylicacidisnamedbyreplaceingthe“e”endingofthealkanenamewith“–oicacid”.(alkanoic

acid)Carboxylicacidsinwhichacarboxylgroupisattachedtoacycliccompoundcanbenamedbyadding“carboxylicacid”tothenameofthecycliccompound.benzoicacidNomenclatureofacylhalidesAcylhalidesarenamedbyusingtheacidnameandreplacingthe“–icacid”with“–ylhalide”(alkanoyl

halide),orbyreplacing“carboxylicacid

”with“carbonylhalide”(cycloalkanecarbonylhalide)benzoylchlorideNomenclatureofacidanhydrides?Doyouknowthemeaningof“anhydride”

R=R’,asymmetricalanhydride

R≠R’,amixedanhydrideSymmetricalanhydridesarenamedbyusingtheacidnameandreplacing“acid”with“anhydride”,mixedanhydridesarenamedbystatingthenameofbothacidgroupsinalphabeticalorderfollowedby“anhydride”.Innaminganester,thenameofthegroupattachedtothe“carboxyloxygen”isstatedfirst.Thisisfollowedbythenameoftheacidwith“-icacid”replacedby“-ate”.Saltsofcarboxylicacidsarenamedinthesameway.

(R’alkyl

R

alkanoate)Nomenclatureofestersethylacetate

AprimaryamideasecondaryamideatertiaryamideAmidesarenamedbyusingtheacidname,replacing“–oicacid”or“-icacid”with“amide”,orbyreplacing“carboxylicacid”with“carboxamide”.(alkanamide)or(cycloalkanecarboxamide)NomenclatureofamidesNomenclatureofnitrilesIncommonnomenclature,nitrilesarenamedbyreplacing“–icacid”with“-onitrile”,ortheyarenamedas“alkyl

cyanide”.(alkyl

cyanide)InIUPACnomenclature,nitrilesarenamedbyadding“-nitrile”tothealkanename.(alkanenitrile)Alkalineearths(堿土)Magnesium(鎂)Calcium(鈣)Aluminum

(鋁)Tin

(錫)Lead

(鉛)TransitionMetals:Titanium(鈦)Chromium(鉻)Manganese(錳)Iron(鐵)Cobalt(鈷)Nickle(鎳)Copper(銅)Zinc(鋅)Silver(銀)Platinum(鉑)Gold(金)Palladium(鈀)

另外必須提供微生物的生長介質必須含有諸如硫酸銨、氨水或尿素等含氮化合物，以及無機磷酸鹽。此外，必需有的恒定的最佳的pH值和溫度。以青霉素G為例，發酵過程在200小時后完成，細胞團塊經過濾而分離。從濾液中經吸收或提取工藝而分離出所需要的活性制劑。細胞團塊，如果并非目的產品，由于其高蛋白質含量，可進一步用作動物飼料。

Additionallythemicroorganismsmustbesuppliedinthegrowthmediumwithnitrogen-containingcompoundssuchasammonium

sulfate,ammonia,orurea,aswellaswithinorganicphosphates.Furthermore,constantoptimalpHandtemperaturearerequired.InthecaseofpenicillinG,thefermentationisfinishedafter200hours,andthecellmassisseparatedbyfiltration.Thedesiredactiveagentsareisolatedfromthefiltratebyabsorptionorextractionprocesses.Thecellmass,ifnotthedesiredproduct,canbefurtherusedasananimalfeedstuffowingtoitshighproteincontent.

利用現代重組技術，已獲得的微生物可以生產原始基因中并未編碼的多肽。修飾過的大腸桿菌使得產生人類胰島素或前胰島素原類似物的A-和B-鏈成為可能。經分離后再選擇性形成二硫鍵，其最終提純由色析（譜）工序來決定。通過這種方式，完全可以不受限制地從任意的動物胰腺原料獲得人類胰島素。

Bymodernrecombinanttechniquesmicroorganismshavebeenobtainedwhichalsoallowproductionofpeptideswhichwerenotencodedintheoriginalgenes.ModifiedE.colibacteriamakeitthuspossibletoproduceA-andB-chainsofhumaninsulinorproinsulinanalogs.Thedisulfidebridgesareformedselectivelyafterisolation，andthefinalpurificationiseffectedbychromatographicprocedures.Inthiswayhumaninsulinisobtainedtotallyindependentlyfromanypancreaticmaterialtakenfromanimals.

其他重要的肽，激素和酶，如人類生長激素（HGH），神經活性肽，生長抑素，干擾素，組織型纖溶酶原激活劑（TPA），淋巴因子，如鈣調蛋白的鈣調節劑，蛋白疫苗，以及作為診斷用單克隆抗體，也是應用這種方法合成的。

Otherimportantpeptides,hormones,andenzymes,suchashumangrowthhormone(HGH),neuroactivepeptides,somatostatin,interferons,tissueplasminogenactivator(TPA),lymphokines,calciumregulatorslikecalmodulin,proteinvaccines,aswellasmonoclonalantibodiesusedasdiagnostics,aresynthesizedinthisway.

一個單一的微生物中所存在的酶或酶系統，可應用于控制的立體定向的和位置定向的化學反應。這個原理在類固醇化學尤其有用。在這里，我們只能提及黃體酮經微生物法的11-α-位羥基化反應制得11-α-羥基黃體酮，一個用于合成可的松（腎上腺皮質酮）的關鍵產品。今天，分離出的酶很重要，不僅因為淀粉的酶法糖化技術的重要性以及葡萄糖異構化成果糖，而且它們在用于診斷疾病的無數檢測程序和用于監測治療的酶法分析中也很重要。

Theenzymesorenzymaticsystemswhicharepresentinasinglemicroorganismcanbeusedfordirectedstereospecificandregiospecificchemicalreactions.Thisprincipleisespeciallyusefulinsteroidchemistry.Herewemayreferonlytothemicrobiological11-α-hydroxylationofprogesteroneto11-α-hydroxyprogesterone,akeyproductusedinthesynthesisofcortisone.Isolatedenzymesareimportanttodaynotonlybecauseofthetechnicalimportanceoftheenzymaticsaccharificationofstarch,andtheisomerizationofglucosetofructose,Theyarealsosignificantinthecountlesstestproceduresusedindiagnosingillness,andinenzymaticanalysiswhichisusedinthemonitoringoftherapy.

大量的酶本身可以作為活性成分。因此，含有蛋白酶（如糜蛋白酶，胃蛋白酶和胰蛋白酶），淀粉酶和脂肪酶的制劑產品，大多與合成的抗酸藥相配合，以促進消化。鏈激酶和尿激酶是重要的溶血栓劑，而天冬酰胺酶則用作治療白血病中的細胞生長抑劑。

Anumberofenzymesarethemselvesusedasactiveingredients.Thuspreparationscontainingproteases(e.g.chymotrypsin,pepsin,andtrypsin),amylasesandlipases,

mostlyincombinationwithsyntheticantacids,promotedigestion.Streptokinaseandurokinaseareimportantinthrombolytics,andasparaginaseisusedasacytostaticagentinthetreatmentofleukemia.

最后必須提到的是，酶作為生物催化劑在化學反應的重要應用，其中立體專一性和選擇性可以得到應用。著名例子有酶裂解N-乙酰基-D,L-氨基酸的外消旋體而生成L-氨基酸，從芐基青霉素經青霉素酰胺酶作用生產8-氨基青霉烷酸，以及天門冬氨酸酶催化氨對富馬酸立體專一性加成反應以生產L-天門冬氨酸。

在這些應用中，酶可以固載的形式—某種方式連接在載體上—使用，也可以雜相催化劑的形式來使用。這是有利的，因為它們可以很容易從反應介質中分離，并回收再利用。

Finallymentionmustbemadeoftheimportantuseofenzymesas‘biocatalysts’inchemicalreactionswheretheirstereospecificityandselectivitycanbeused.KnownexamplesaretheenzymaticcleavageofracematesofN-acetyl-D,L-aminoacidstogiveL-aminoacids,

theproductionof8-aminopenicillanicacidfrombenzylpenicillinbymeansofpenicillinamidaseandtheaspartase-catalysedstereospecificadditionofammoniatofumaricacidinordertoproduceL-asparticacid.Intheseapplicationstheenzymescanbeusedinimmobilizedforms-somehowboundtocarriers-andsousedasheterogeneouscatalysts.Thisisadvantageousbecausetheycantheneasilybeseparatedfromthereactionmediumandrecycledforfurtheruse.benzylpenicillinAminopenicillanicacidpenicillinamidaseFumaricacidaspartaseL-asparticacid

另一個基于蛋白酶專一性作用的重要工藝是應用于半合成人胰島素的生產。這從豬胰島素開始，其中在B鏈的30-位的丙氨酸由于胰蛋白酶選擇性作用被替換為蘇氨酸叔丁基酯。分離(生成的)胰島素酯，水解為人胰島素，最后經色析（譜）法程序而純化。

酶的來源不僅包括微生物，也包括植物的和動物的材料。

Anotherimportantprocessdependingonthespecificactionofproteasesisappliedfortheproductionofsemisynthetichumaninsulin.Thisstartswithpiginsulininwhichthealanineinthe30-positionoftheB-chainisreplacedbyathreoninetert-butylesterbytheselectiveactionoftrypsin.Theinsulinesterisseparated,hydrolyzedtohumaninsulinandfinallypurifiedbychromatographicprocedures.Sourcesforenzymesincludenotonlymicroorganismsbutalsovegetableandanimalmaterials