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-alcohols kanye i-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 esiko 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

Uhlelo lokusebenza lwe-Teadenols

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. wenza 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), itiye le-Pu 'er, itiye le-Liubao netiye le-Fu Brick, kodwa okuqukethwe kwe-Teadenols 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, ama-oolong, amhlophe, ama-green teas amnyama awaqukethe 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 abanzi okusebenza.