Itiye lingesinye seziphuzo ezintathu ezinkulu emhlabeni, ezinothe ngama-polyphenols, ane-antioxidant, anti-cancer, anti-virus, hypoglycemic, hypolipidemic kanye neminye imisebenzi yebhayoloji nemisebenzi yokunakekelwa kwezempilo.Itiye lingahlukaniswa libe yitiye elingavutshiwe, itiye elivutshiwe kanye netiye elivutshelwe ngokobuchwepheshe balo bokucubungula kanye nezinga lokuvutshelwa.Itiye langemva kokuvutshelwa lisho itiye elinokuhlanganyela kwe-microbial ekuvubeleni, njengetiye eliphekiwe le-Pu 'er, itiye le-Fu Brick, itiye le-Liubao elikhiqizwa e-China, kanye ne-Kippukucha, i-Saryusoso, i-Yamabukinadeshiko, i-Suraribijin ne-Kuroyamecha ekhiqizwa e-Japan.Lawa tiye avutshelwe ngama-microbial athandwa abantu ngemiphumela yawo yokunakekelwa kwezempilo njengokwehlisa amafutha egazi, ushukela egazini kanye ne-cholesterol.

Ngemuva kokuvutshelwa kwe-microbial, i-polyphenols yetiye itiye iguqulwa ngama-enzyme futhi ama-polyphenol amaningi anezakhiwo ezintsha ayakhiwa.I-Teadenol A ne-Teadenol B yizinto eziphuma ku-polyphenol ezihlukanisiwe netiye elivutshiwe eline-Aspergillus sp (PK-1, FARM AP-21280).Ocwaningweni olwalandela, kutholwe ngobuningi betiye elivutshiwe.Ama-Teadenols anama-stereoisomers amabili, i-cis-Teadenol A kanye ne-trans-Teadenol B. Ifomula ye-Molecular C14H12O6, isisindo samangqamuzana angu-276.06, [MH] -275.0562, ifomula yesakhiwo iboniswa kuMfanekiso 1. Ama-teadenol anamaqembu amabhayisikili futhi afana ne-C- a izindandatho ze-flavane 3-alcohol futhi ziyi-b-ring fission catechins derivatives.I-Teadenol A ne-Teadenol B ingenziwa nge-biosynthesized kusuka ku-EGCG ne-GCG ngokulandelanayo.

Ezifundweni ezalandela, kwatholakala ukuthi i-Teadenols yayinemisebenzi yebhayoloji efana nokukhuthaza ukugcinwa kwe-adiponectin, ukuvimbela inkulumo ye-protein tyrosine phosphatase 1B (PTP1B) nokuba mhlophe, okudonse ukunaka kwabacwaningi abaningi.I-Adiponectin iyi-polypeptide ethize kakhulu kuzicubu ze-adipose, ezinganciphisa kakhulu izehlakalo zokuphazamiseka kwe-metabolic ohlotsheni lwesifo sikashukela sohlobo II.I-PTP1B okwamanje ibonwa njengethagethi yokwelapha yesifo sikashukela nokukhuluphala, okubonisa ukuthi i-Teadenols inemiphumela engaba khona ye-hypoglycemic kanye nokuncipha kwesisindo.

Kuleli phepha, ukutholwa kokuqukethwe, i-biosynthesis, ukuhlanganiswa okuphelele kanye nokusebenza kwe-bioactivity kwe-Teadenols etiyeni elivutshelwe yi-microbial kwabuyekezwa, ukuze kuhlinzekwe isisekelo sesayensi kanye nereferensi yethiyori ekuthuthukisweni nasekusetshenzisweni kwe-Teadenols.

▲ TA isithombe esibonakalayo

01

Ukutholwa kwe-Teadenols etiyeni elivutshelwe yi-microbial

Ngemva kokuba ama-Teadenols etholwe etiyeni elivutshiwe i-Aspergillus SP (PK-1, FARM AP-21280) okokuqala ngqa, amasu e-HPLC kanye ne-LC-MS/MS asetshenziswa ukutadisha ama-Teadenols ngezinhlobo ezahlukene zetiye.Ucwaningo luye lwabonisa ukuthi ama-Teadenols atholakala kakhulu etiyeni elivutshelwe yi-microbial.

▲ TA, TB liquid chromatogram

▲ I-mass spectrometry yetiye elibiliswe yi-microbial kanye ne-TA ne-TB

Aspergillus oryzae SP.PK-1, FARM AP-21280, Aspergillus oryzae sp.AO-1, ​​NBRS 4214, Aspergillus awamori sp.SK-1, Aspergillus oryzae Sp.AO-1, ​​NBRS 4214, Aspergillus oryzae.SK-1 , NBRS 4122), Eurotium sp.I-Ka-1, FARM AP-21291, Ukugxila okuhlukile kwe-Teadenols kutholwe etiyeni elibilile i-Kippukucha, i-Saryusoso, i-Yamabukinadeshiko, i-Suraribijin ne-Kuroyamecha, i-gentoku-cha ethengiswa e-Japan, nasetiyeni eliphekiwe le-Pu erh, itiye le-Liuckbao ne-Fu Brick. itiye laseChina.

Okuqukethwe kwe-Teadenols kumatiye ahlukene kuhlukile, okucatshangwa ukuthi kubangelwa izimo ezihlukene zokucubungula kanye nezimo zokuvutshelwa.

Ucwaningo olwengeziwe lubonise ukuthi okuqukethwe kwe-Teadenols emaqabunga etiye ngaphandle kokucubungula ukuvutshelwa kwe-microbial, njengetiye eliluhlaza, itiye elimnyama, itiye le-oolong netiye elimhlophe, kwakuphansi kakhulu, ngokuyisisekelo kungaphansi komkhawulo wokutholwa.Okuqukethwe kwe-Teadenol emaqabunga etiye ahlukahlukene kuboniswa kuThebula 1.

02

I-Bioactivity ye-Teadenols

Ucwaningo luye lwabonisa ukuthi i-Teadenols ingakhuthaza ukwehla kwesisindo, ukulwa nesifo sikashukela, ukulwa ne-oxidation, ukuvimbela ukwanda kwamangqamuzana omdlavuza kanye nesikhumba sibe mhlophe.

I-Teadenol A ingakhuthaza ukukhiqizwa kwe-adiponectin.I-Adiponectin iyi-peptide engapheli ekhishwa ama-adipocyte futhi icace kakhulu kuzicubu ze-adipose.Ihlotshaniswa kabi kakhulu nezicubu ze-visceral adipose futhi inezindawo zokulwa nokuvuvukala kanye ne-anti-atherosclerotic.Ngakho-ke i-Teadenol A inamandla okwehlisa isisindo.

I-Teadenol A iphinde ivimbele ukuvezwa kwe-protein tyrosine phosphatase 1B (PTP1B), I-non-receptor tyrosine phosphatase yakudala emndenini we-protein tyrosine phosphatase, edlala indima ebalulekile engalungile ekuboniseni i-insulin futhi okwamanje eyaziwa njengethagethi yokwelapha yesifo sikashukela.I-Teadenol A ingalawula kahle i-insulin ngokuvimbela isisho se-PTP1B.Ngaleso sikhathi, u-TOMOTAKA et al.ibonise ukuthi i-Teadenol A iyi-Ligand ye-long-chain fatty acid receptor GPR120, engabopha ngokuqondile futhi yenze i-GPR120 isebenze futhi ikhuthaze ukukhishwa kwehomoni ye-insulin ye-GLP-1 kumaseli we-endocrine we-STC-1 wamathumbu.I-Glp-1 ivimbela isifiso sokudla futhi yandisa ukukhiqizwa kwe-insulin, ikhombisa imiphumela elwa nesifo sikashukela.Ngakho-ke, i-Teadenol A inomphumela we-antidiabetic ongaba khona.

Amanani e-IC50 omsebenzi wokukhukhula we-DPPH kanye nomsebenzi we-superoxide anion radical scavenging we-Teadenol A wawungu-64.8 μg/mL kanye no-3.335 mg/mL, ngokulandelana.Amanani e-IC50 omthamo we-antioxidant ophelele kanye namandla okuhlinzeka nge-hydrogen abengu-17.6 U/mL no-12 U/mL, ngokulandelana.Kubuye kwaboniswa ukuthi i-teadenol B ekhishwayo inomsebenzi ophezulu wokulwa nokwanda ngokumelene namaseli omdlavuza we-colon we-HT-29, futhi ivimbela amangqamuzana omdlavuza we-colon we-HT-29 ngokwandisa amazinga e-caspase-3/7, i-caspase-8 ne-Caspase. -9, ukufa kwe-receptor kanye nezindlela ze-apoptosis ze-mitochondrial.

Ngaphezu kwalokho, ama-Teadenols ayikilasi lama-polyphenols angenza isikhumba sibe mhlophe ngokuvimbela umsebenzi we-melanocyte kanye nokuhlanganiswa kwe-melanin.

03

Ukwakhiwa kwe-Teadenols

Njengoba kubonakala kudatha yocwaningo kuThebula 1, ama-Teadenols etiyeni lokuvutshelwa kwe-microbial anokuqukethwe okuphansi kanye nezindleko eziphakeme zokucebisa nokuhlanzwa, okunzima ukuhlangabezana nezidingo zocwaningo olujulile nokuthuthukiswa kwesicelo.Ngakho-ke, izazi zenze ucwaningo mayelana nokuhlanganiswa kwezinto ezinjalo kusuka ezinhlangothini ezimbili ze-biotransformation kanye ne-chemical synthesis.

WULANDARI et al.ifakwe i-Aspergillus SP (PK-1, FARM AP-21280) kusixazululo esixubile se-EGCG enziwe inzalo ne-GCG.Ngemuva kwamaviki ama-2 wesiko ku-25 ℃, i-HPLC yasetshenziswa ukuhlaziya ukwakheka kwendawo yesiko.Kutholwe i-Teadenol A ne-Teadenol B.Kamuva, i-Aspergillus oryzae A. Awamori (NRIB-2061) kanye no-Aspergillus oryzae A. Kawachii (IFO-4308) bagonyelwa ku-Autoclave EGCG ne-GCG, ngokulandelana, kusetshenziswa indlela efanayo.I-Teadenol A ne-Teadenol B zitholwe kukho kokubili okuphakathi.Lezi zifundo zibonise ukuthi ukuguqulwa kwe-microbial ye-EGCG ne-GCG kungakhiqiza i-Teadenol A ne-Teadenol B. SONG et al.wasebenzisa i-EGCG njengempahla eluhlaza futhi wajova i-Aspergillus sp ukutadisha izimo ezifanele zokukhiqizwa kwe-Teadenol A ne-Teadenol B ngesiko eliwuketshezi neliqinile.Imiphumela yabonisa ukuthi i-CZapEK-DOX medium eguquliwe equkethe i-5% EGCG kanye ne-1% ye-powder yetiye eluhlaza yayinesivuno esiphezulu.Kutholakale ukuthi ukungezwa kwe-green tea powder akuzange kuthinte ngokuqondile ukukhiqizwa kwe-Teadenol A ne-Teadenol B, kodwa ikakhulukazi kwabangela ukwanda kwenani le-biosynthase elihilelekile.Ngaphezu kwalokho, i-YOSHIDA et al.i-Teadenol A ne-Teadenol B ehlanganisiwe kusuka ku-phloroglucinol.Izinyathelo ezibalulekile zokuhlanganiswa kwakuyi-asymmetric α -aminoxy catalytic reaction of organic catalytic aldehydes kanye ne-intramolecular allyl substitution ye-palladium-catalyzed phenol.

▲ I-electron microscopy yenqubo yokuvutshelwa kwetiye

04

Isicelo sokufunda ngeTeadenols

Ngenxa yomsebenzi wayo obalulekile webhayoloji, ama-Teadenols asetshenziswe kwezemithi, ekudleni nasekuphakeleni, izimonyo, ama-reagents okuhlonza neminye imikhakha.

Kunemikhiqizo ehlobene equkethe ama-Teadenols emkhakheni wokudla, njenge-Japanese Slimming Tea kanye nama-polyphenols etiye elibilile.Ngaphezu kwalokho, u-Yanagida et al.kuqinisekisile ukuthi izingcaphuno zetiye eziqukethe i-Teadenol A ne-Teadenol B zingasetshenziswa ekucubunguleni ukudla, izinongo, izithasiselo zezempilo, ukudla kwezilwane nezimonyo.ITO et al.ulungiselele i-ejenti ye-topical yesikhumba equkethe ama-Teadenols anomphumela omhlophe oqinile, ukuvimbela ama-radical mahhala kanye nomphumela wokulwa nokushwabana.Iphinde ibe nemiphumela yokwelapha induna, ukuthambisa, ukuqinisa umsebenzi wokuvimba, ukuvimbela ukuvuvukala okutholakala ku-UV kanye nezilonda ezilwa nokucindezela.

E-China, ama-Teadenols abizwa nge-fu tea.Abacwaningi benze ucwaningo oluningi mayelana netiye elikhishwe noma amafomula ayinhlanganisela aqukethe itiye i-fu A kanye netiye le-Fu mayelana nokwehlisa i-lipids yegazi, ukuncipha kwesisindo, ushukela wegazi, umfutho wegazi ophakeme kanye nokuthambisa imithambo yegazi.I-high-purity fu tea A ehlanziwe futhi yalungiswa ngu-Zhao Ming et al.ingasetshenziswa ekulungiseleleni imithi ye-antilipid.He Zhihong et al.yenza amaphilisi etiye, amaphilisi noma ama-granules aqukethe itiye elimnyama le-anhua le-Fu A ne-Fu B, i-gynostema pentaphylla, i-Rhizoma orientalis, i-ophiopogon neminye imikhiqizo ye-homology yokwelapha nokudla, enemiphumela esobala nehlala njalo ekunciphiseni isisindo kanye nokunciphisa i-lipid kuzo zonke izinhlobo zokukhuluphala. abantu.U-Tan Xiao 'ao ulungise itiye le-fuzhuan nge-fuzhuan A ne-Fuzhuan B, okulula ukumuncwa umzimba womuntu futhi linemiphumela esobala ekwehliseni i-hyperlipidemia, i-hyperglycemia, umfutho wegazi ophakeme kanye nokuthambisa imithambo yegazi.

05

“Ulimi

Ama-teadenols ama-b-ring fission catechin derivatives akhona etiyeni elivutshelwe yi-microbial, angatholakala ekuguqulweni kwamagciwane e-epigallocatechin gallate noma ekuhlanganiseni okuphelele kwe-phloroglucinol.Ucwaningo luye lwabonisa ukuthi ama-Teadenols aqukethwe kumatiye ahlukahlukene abilisiwe amagciwane.Imikhiqizo ihlanganisa itiye elivutshiwe i-Aspergillus Niger, itiye elibilile i-Aspergillus oryzae, itiye elibilile i-Aspergillus oryzae, itiye elibilile i-Sachinella, i-Kippukucha (eJapane), i-Saryusoso (eJapane), i-Yamabukinadeshiko (eJapane), i-Suraribijin (eJapane), i-Kuroyamecha (eJapane), i-Gentok cha (Japan), Awa-Bancha (Japan), Goishi-cha (Japan), Pu 'er tea, Liubao tea neFu Brick tea, kodwa okuqukethwe kweTeadenols kumatiye ahlukahlukene kuhluke kakhulu.Okuqukethwe kwe-Teadenol A no-B kusuka ku-0.01% kuya ku-6.98% no-0.01% kuya ku-0.54%, ngokulandelana.Ngesikhathi esifanayo, itiye le-oolong, elimhlophe, eliluhlaza kanye nelimnyama aliqukethe lezi zinhlanganisela.

Mayelana nocwaningo lwamanje, izifundo ze-Teadenols zisanqunyelwe, ezibandakanya kuphela umthombo, okuqukethwe, i-biosynthesis kanye nendlela yokwenziwa ephelele, kanye nendlela yayo yokusebenza nentuthuko kanye nokusetshenziswa kusadinga ucwaningo oluningi.Ngocwaningo olwengeziwe, izinhlanganisela zeTeadenols zizoba nenani elikhulu lokuthuthuka kanye namathemba okusebenza abanzi.