Tiyi ndi chimodzi mwa zakumwa zazikulu zitatu zapadziko lapansi, zolemera mu polyphenols, ndi antioxidant, anti-cancer, anti-virus, hypoglycemic, hypolipidemic ndi ntchito zina zamoyo ndi ntchito zaumoyo. Tiyi atha kugawidwa mu tiyi wosawilitsidwa, tiyi wothira ndi tiyi wothira pambuyo pake malinga ndi ukadaulo wake wokonza komanso kuchuluka kwa nayonso mphamvu. Tiyi wothira pambuyo pake amatanthauza tiyi wokhala ndi tizilombo toyambitsa matenda, monga tiyi wophika wa Pu 'er, tiyi wa Fu Brick, tiyi wa Liubao wopangidwa ku China, Ndipo Kippukucha, Saryusoso, Yamabukinadeshiko, Suraribijin ndi Kuroyamecha opangidwa ku Japan. Tiyi wothira tiyi wa tizilombo tating'onoting'ono amakondedwa ndi anthu chifukwa cha thanzi lawo monga kutsitsa mafuta amagazi, shuga wamagazi ndi cholesterol.

Pambuyo poyatsa tizilombo tating'onoting'ono, tiyi polyphenols mu tiyi amasinthidwa ndi michere ndipo ma polyphenols ambiri okhala ndi zida zatsopano amapangidwa. Teadenol A ndi Teadenol B ndizochokera ku polyphenol zopatulidwa ku tiyi wothira ndi Aspergillus sp (PK-1, FARM AP-21280). Mu kafukufuku wotsatira, adapezeka mu tiyi wambiri wofufumitsa. Ma Teadenols ali ndi ma stereoisomers awiri, cis-Teadenol A ndi trans-Teadenol B. Molecular formula C14H12O6, molecular weight 276.06, [MH] -275.0562, mawonekedwe apangidwe akuwonetsedwa mu Chithunzi 1. Ma Teadenols ali ndi magulu ozungulira ndi ofanana ndi C- a mphete za flavane 3-mowa ndi ndi b-ring fission catechins zotumphukira. Teadenol A ndi Teadenol B akhoza kukhala biosynthesized kuchokera ku EGCG ndi GCG motsatira.

M'maphunziro otsatirawa, adapeza kuti Teadenols anali ndi zochitika zamoyo monga kulimbikitsa katulutsidwe ka adiponectin, kuletsa kufotokoza kwa mapuloteni a tyrosine phosphatase 1B (PTP1B) ndi kuyera, zomwe zidakopa chidwi cha ofufuza ambiri. Adiponectin ndi polypeptide yeniyeni kuti adipose minofu, amene angathe kuchepetsa kwambiri zochitika za kagayidwe kachakudya matenda mu mtundu II shuga. PTP1B pakali pano imadziwika kuti ndiyo njira yochizira matenda a shuga ndi kunenepa kwambiri, zomwe zikuwonetsa kuti Teadenols imatha kukhala ndi hypoglycemic komanso kuchepa thupi.

Mu pepalali, kuzindikira zomwe zili, biosynthesis, kaphatikizidwe kokwanira ndi bioactivity ya Teadenols mu tiyi wothira wothira tiyi adawunikiridwa, kuti apereke maziko asayansi ndi malingaliro aukadaulo pakukula ndi kugwiritsa ntchito Teadenols.

▲ TA chithunzi chowoneka

01

Kuzindikira kwa Teadenols mu tiyi wothira tizilombo tating'onoting'ono

Teadenols atapezedwa kuchokera ku tiyi wothira wa Aspergillus SP (PK-1, FARM AP-21280) kwa nthawi yoyamba, njira za HPLC ndi LC-MS/MS zidagwiritsidwa ntchito pophunzira Teadenols mumitundu yosiyanasiyana ya tiyi. Kafukufuku wasonyeza kuti Teadenols makamaka amapezeka mu tiyi fermented tizilombo.

▲ TA, TB madzi chromatogram

▲ Mass spectrometry ya tiyi wothira tizilombo tating'onoting'ono ndi TA ndi 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. Ka-1, FARM AP-21291, kuchuluka kosiyanasiyana kwa Teadenols kunapezeka mu tiyi wothira wa Kippukucha, Saryusoso, Yamabukinadeshiko, Suraribijin ndi Kuroyamecha, gentoku-cha yogulitsidwa ku Japan, komanso tiyi wophika wa Pu erh, tiyi ya Liu Brickbao ndi Fu. tiyi waku China.

Zomwe zili mu Teadenols mu tiyi wosiyanasiyana ndizosiyana, zomwe zimaganiziridwa kuti zimayamba chifukwa cha kusintha kosiyanasiyana komanso kuyatsa.

Kafukufuku wowonjezera adawonetsa kuti zomwe zili mu Teadenols m'masamba a tiyi popanda kuwiritsa kwa tizilombo tating'onoting'ono, monga tiyi wobiriwira, tiyi wakuda, tiyi wa oolong ndi tiyi woyera, zinali zotsika kwambiri, zotsika kwambiri pakuzindikira. Zomwe zili mu teadenol m'masamba osiyanasiyana a tiyi zikuwonetsedwa mu Gulu 1.

02

Bioactivity ya Teadenols

Kafukufuku wasonyeza kuti Teadenols akhoza kulimbikitsa kuwonda, kulimbana ndi matenda a shuga, kulimbana ndi okosijeni, kuletsa kuchulukana kwa maselo a khansa ndi kuyera khungu.

Teadenol A ikhoza kulimbikitsa katulutsidwe ka adiponectin. Adiponectin ndi peptide yamkati yomwe imatulutsidwa ndi adipocytes komanso yodziwika kwambiri ku minofu ya adipose. Zimagwirizana kwambiri ndi minofu ya visceral adipose ndipo imakhala ndi anti-yotupa komanso anti-atherosclerotic. Chifukwa chake Teadenol A ali ndi kuthekera kochepetsa thupi.

Teadenol A imalepheretsanso mawu a protein tyrosine phosphatase 1B (PTP1B), A classic non-receptor tyrosine phosphatase m'banja la protein tyrosine phosphatase, lomwe limakhala ndi gawo loyipa pakuzindikiritsa kwa insulin ndipo pakadali pano limazindikiridwa ngati Chandamale chochizira matenda a shuga. Teadenol A imatha kuyendetsa bwino insulin mwa kuletsa mawu a PTP1B. Pakadali pano, TOMOTAKA et al. adawonetsa kuti Teadenol A ndi A ligand of long-chain fatty acid receptor GPR120, yomwe imatha kumanga ndi kuyambitsa GPR120 ndikulimbikitsa kutulutsa kwa insulin hormone GLP-1 m'maselo am'mimba a STC-1. Glp-1 imalepheretsa kudya ndikuwonjezera kutulutsa kwa insulini, kuwonetsa zotsatira za anti-diabetes. Chifukwa chake, Teadenol A imakhala ndi antidiabetic effect.

Miyezo ya IC50 ya DPPH yowononga ntchito ndi superoxide anion radical scavenging ntchito ya Teadenol A inali 64.8 μg/mL ndi 3.335 mg/mL, motsatana. Miyezo ya IC50 ya mphamvu yonse ya antioxidant ndi mphamvu yoperekera haidrojeni inali 17.6 U/mL ndi 12 U/mL, motsatana. Zawonetsedwanso kuti tiyi wa tiyi wokhala ndi Teadenol B ali ndi anti-proliferating anti-proliferating anti HT-29 cell cancer cancer, ndipo amalepheretsa ma cell a khansa ya m'matumbo a HT-29 powonjezera kuchuluka kwa mawu a caspase-3/7, caspase-8 ndi Caspase. -9, receptor imfa ndi mitochondrial apoptosis njira.

Kuphatikiza apo, Teadenols ndi gulu la ma polyphenols omwe amatha kuyera khungu poletsa zochita za melanocyte ndi kaphatikizidwe ka melanin.

03

The synthesis wa Teadenols

Monga momwe zikuwonekera kuchokera muzofukufuku zomwe zili mu Table 1, Teadenols mu tiyi ya tiyi ya tizilombo toyambitsa matenda imakhala yotsika komanso yotsika mtengo yowonjezeretsa ndi kuyeretsa, zomwe zimakhala zovuta kukwaniritsa zofunikira za kafukufuku wozama ndi chitukuko cha ntchito. Chifukwa chake, akatswiri apanga kafukufuku wokhudza kaphatikizidwe kazinthu zotere kuchokera mbali ziwiri za biotransformation ndi kaphatikizidwe ka mankhwala.

WULANDARI et al. inoculated Aspergillus SP (PK-1, FARM AP-21280) mu osakaniza njira ya chosawilitsidwa EGCG ndi GCG. Pambuyo pa masabata a 2 a chikhalidwe pa 25 ℃, HPLC idagwiritsidwa ntchito kusanthula kapangidwe ka chikhalidwe cha chikhalidwe. Teadenol A ndi Teadenol B adapezeka. Pambuyo pake, Aspergillus oryzae A. Awamori (NRIB-2061) ndi Aspergillus oryzae A. Kawachii (IFO-4308) adalowetsedwa mu A osakaniza a autoclave EGCG ndi GCG, motsatira, pogwiritsa ntchito njira yomweyo. Teadenol A ndi Teadenol B adapezeka mu sing'anga zonse ziwiri. Maphunzirowa awonetsa kuti kusintha kwa tizilombo toyambitsa matenda a EGCG ndi GCG kumatha kupanga Teadenol A ndi Teadenol B. SONG et al. adagwiritsa ntchito EGCG ngati zopangira ndikulowetsa Aspergillus sp kuti aphunzire momwe zilili bwino pakupanga kwa Teadenol A ndi Teadenol B ndi chikhalidwe chamadzi komanso cholimba. Zotsatira zake zidawonetsa kuti sing'anga yosinthidwa ya CZapEK-DOX yokhala ndi 5% EGCG ndi 1% ufa wa tiyi wobiriwira anali ndi zokolola zambiri. Zinapezeka kuti kuwonjezera kwa ufa wa tiyi wobiriwira sikunakhudze mwachindunji kupanga Teadenol A ndi Teadenol B, koma makamaka kunachititsa kuti chiwerengero cha biosynthase chiwonjezeke. Kuphatikiza apo, YOSHIDA et al. Anapanga Teadenol A ndi Teadenol B kuchokera ku phloroglucinol. Masitepe ofunikira a kaphatikizidwe anali asymmetric α -aminoxy catalytic reaction of organic catalytic aldehydes and intramolecular allyl substitution of palladium-catalyzed phenol.

▲ Kachilombo kakang'ono ka elekitironi kamene kakuwotchera tiyi

04

Kugwiritsa ntchito Teadenols

Chifukwa cha ntchito yake yayikulu yachilengedwe, ma Teadenols amagwiritsidwa ntchito muzamankhwala, chakudya ndi chakudya, zodzoladzola, zowunikira ndi zina.

Pali zinthu zofananira zomwe zili ndi Teadenols m'munda wazakudya, monga tiyi waku Japan Slimming Tea ndi ma polyphenols a tiyi wothira. Komanso, Yanagida et al. adatsimikizira kuti tiyi wokhala ndi Teadenol A ndi Teadenol B angagwiritsidwe ntchito pokonza zakudya, zokometsera, zowonjezera thanzi, zakudya za ziweto ndi zodzoladzola. ITO ndi al. anakonza mankhwala apakhungu okhala ndi ma Teadenols okhala ndi whitening kwenikweni, zoletsa zaulere komanso zotsutsana ndi makwinya. Zimakhalanso ndi zotsatira za kuchiza ziphuphu, kunyowa, kupititsa patsogolo ntchito yotchinga, kulepheretsa kutupa kwa UV ndi zilonda zotsutsana ndi kupanikizika.

Ku China, Teadenols amatchedwa fu tiyi. Ofufuza achita kafukufuku wambiri pa tiyi kapena ma formula omwe ali ndi fu tiyi A ndi Fu tiyi B ponena za kutsitsa lipids m'magazi, kuchepa thupi, shuga wamagazi, matenda oopsa komanso kufewetsa mitsempha yamagazi. Tiyi ya furity A yoyeretsedwa ndikukonzedwa ndi Zhao Ming et al. angagwiritsidwe ntchito pokonza antilipids mankhwala. Iye Zhihong et al. adapanga makapisozi a tiyi, mapiritsi kapena ma granules okhala ndi tiyi wakuda wa anhua wa Fu A ndi Fu B, gynostema pentaphylla, Rhizoma orientalis, ophiopogon ndi mankhwala ena amankhwala a homology, omwe ali ndi zotsatira zoonekeratu komanso zokhalitsa pakuchepetsa thupi komanso kuchepetsa lipids kwamitundu yonse ya onenepa. anthu. Tan Xiao 'ao anakonza tiyi wa fuzhuan wokhala ndi fuzhuan A ndi Fuzhuan B, womwe ndi wosavuta kutengeka ndi thupi la munthu ndipo umakhala ndi zotsatira zoonekeratu pakuchepetsa hyperlipidemia, hyperglycemia, matenda oopsa komanso kufewetsa mitsempha yamagazi.

05

“Chiyankhulo

Teadenols ndi b-ring fission catechin zotumphukira zomwe zimapezeka mu tiyi wothira wa tizilombo tating'onoting'ono, zomwe zitha kupezedwa kuchokera ku kusintha kwa tizilombo ta epigallocatechin gallate kapena kuphatikizika kwa phloroglucinol. Kafukufuku wasonyeza kuti Teadenols ali mu tiyi zosiyanasiyana fermented tiyi. Zogulitsazo zikuphatikiza tiyi wa Aspergillus Niger fermented tea, Aspergillus oryzae fermented tea, Aspergillus oryzae fermented tea, Sachinella fermented tea, Kippukucha (Japan), Saryusoso (Japan), Yamabukinadeshiko (Japan), Suraribijin (Japan), Kuroyamecha (Japan), Gentok U-Japan), cha (Japan), Awa-Bancha (Japan), Goishi-cha (Japan), tiyi ya Pu 'er, tiyi ya Liubao ndi tiyi ya Fu Brick, koma zomwe zili mu Teadenols mu tiyi osiyanasiyana ndizosiyana kwambiri. Zomwe zili mu Teadenol A ndi B zidachokera ku 0.01% mpaka 6.98% ndi 0.01% mpaka 0.54%, motsatana. Pa nthawi yomweyi, tiyi wa oolong, woyera, wobiriwira ndi wakuda alibe mankhwala awa.

Malinga ndi kafukufuku wamakono, maphunziro a Teadenols akadali ochepa, okhudza kokha gwero, zomwe zili, biosynthesis ndi njira yonse yopangira, ndi njira yake yochitira zinthu ndi chitukuko ndi kugwiritsa ntchito kumafunikirabe kafukufuku wambiri. Ndi kafukufuku wopitilira, mankhwala a Teadenols adzakhala ndi phindu lalikulu lachitukuko komanso chiyembekezo chogwiritsa ntchito.