Agasti 26, 2015 / Kyushu University / Imibiko Yesayensi

Umbhalo/Wu Tingyao

Ithimba labacwaningi likaKuniyoshi Shimizu, uprofesa ohlangene e-Institute of Agricultural Sciences of Kyushu University eJapane, ukuqinisekisile ukuthi i-31 triterpenoids ehlukanisiwe ne-fruiting body ye-Ganoderma ivimbela i-neuraminidase yamagciwane amahlanu omkhuhlane A ngamazinga ahlukene, phakathi kwawo kukhona amabili. ama-triterpenoids alungele ngisho nokuthuthukiswa njengemithi elwa nomkhuhlane.Imiphumela yocwaningo yashicilelwa kokuthi “Imibiko Yesayensi” ngaphansi kweqembu lokushicilela elithi “Imvelo” ekupheleni kuka-Agasti 2015.

I-Neuraminidase ingelinye lamaprotheni amabili aphumela ngaphandle kwamagciwane omkhuhlane A.Igciwane lomkhuhlane ngalinye linama-protease acishe abe yikhulu.Lapho igciwane lihlasela ingqamuzana futhi lisebenzisa izinto ezisengqamuzaneni ukuze liphindaphinde izinhlayiya zegciwane elisha, i-neuraminidase iyadingeka ukuze izinhlayiya zegciwane elisha zihlukane nengqamuzana futhi ziqhubeke nokuthelela amanye amangqamuzana.Ngakho-ke, lapho i-neuraminidase ilahlekelwa umsebenzi wayo, igciwane elisha liyovaleleka esitokisini futhi lingakwazi ukuphunyuka, usongo kumninikhaya luzoncipha, futhi isifo singalawulwa.I-oseltamivir (Tamiflu) evame ukusetshenziswa emtholampilo iwukusebenzisa lesi simiso ukuvimbela ukwanda nokusabalala kwegciwane.

Ngokocwaningo olwenziwa u-Kuniyoshi Shimizu, ekuhlanganiseni okungu-200 μM, lawa ma-Ganoderma triterpenoid avimbele umsebenzi we-H1N1, H5N1, H7N9 kanye nezinhlobo ezimbili eziguquguqukayo ezimelana ne-NA (H1N1, N295S) kanye ne-NA (H3N2, E119V) kuya kumadigri ahlukahlukene.Sekukonke, umphumela wokuvimbela i-neuraminidase yohlobo lwe-N1 (ikakhulukazi i-H5N1) yiwo ongcono kakhulu, futhi umphumela ovimbelayo ku-neuraminidase we-H7N9 mubi kakhulu.Phakathi kwalawa ma-triterpenoids, i-ganoderic acid TQ kanye ne-ganoderic acid TR ibonise amazinga aphezulu kakhulu okuvimbela, futhi imiphumela yalezi zinhlanganisela ezimbili isukela ku-55.4% kuya ku-96.5% ukuvinjelwa kwezinhlobo ezihlukene ze-NA.

Ukuhlaziywa okwengeziwe kobudlelwane bomsebenzi wesakhiwo salawa ma-triterpenoid kwembula ukuthi ama-triterpenoid, anomphumela ongcono wokuvinjwa kwe-N1 neuraminidase, anesakhiwo esiyinhloko “se-tetracyclic triterpenoids enamabhondi amabili aphindwe kabili, igatsha njengeqembu le-carboxylic, kanye ne-oxygen- eliqukethe iqembu esizeni sika-R5” (Umgogodla A esithombeni esingezansi).Uma isakhiwo esiyinhloko singezinye ezimbili (Umgogodla B no-C esithombeni esingezansi), umphumela uzoba mubi.

(Umthombo/Sci Rep. 2015 Aug 26;5:13194.)

Ku-silico docking isetshenziselwa ukulingisa ukusebenzisana kwe-ganoderic acid (TQ ne-TR) kanye ne-neuraminidases (H1N1 ne-H5N1).Ngenxa yalokho, kwatholakala ukuthi kokubili i-ganoderic acid kanye ne-Tamiflu bakwazi ukubopha ngokuqondile endaweni esebenzayo ye-neuraminidase.Le ndawo esebenzayo yakhiwe izinsalela eziningana ze-amino acid.I-Ganoderma acids TQ ne-TR izobophezela ezinsalela ezimbili ze-amino acid i-Arg292 ne-Glu119.I-Tamiflu inenye inketho kodwa futhi ingenza i-neuraminidase ingasebenzi.

Uma kuqhathaniswa nokuvimbela amanye amaprotheni egciwane le-influenza (njengeprotheni i-M2, evula igobolondo legciwane ngesikhathi igciwane libopha ingqamuzana eliphethe futhi lithumela izakhi zofuzo zegciwane engqamuzaneni), ama-neuraminidase inhibitors okwamanje aqashelwa njengasebenzayo futhi amancane. Imithi yokwelapha umkhuhlane engazweli.Ngakho-ke, abacwaningi bakholelwa ukuthi i-ganoderic acids i-TQ ne-TR, efana kodwa akufani nendlela ye-Tamiflu, inethuba lokusebenzisa njengesizukulwane esisha sezidakamizwa ezilwa nomkhuhlane noma izinkomba zokuklama.

Kodwa-ke, kunesidingo sokuthi umuthi usetshenziswe njengomuthi wokulwa nomkhuhlane, okungukuthi, umuthi kufanele uvimbele ngempumelelo ukukhiqizwa kwegciwane ngaphandle kokulimaza amaseli angenwe yigciwane.Kodwa-ke, ekuhlolweni kwamangqamuzana atheleleke ngamagciwane aphilayo kanye nemigqa yamaseli omdlavuza webele (MCF-7), kwatholakala ukuthi lapho abacwaningi besebenzisa lezi zinhlobo ezimbili zama-ganoderic acid kuphela, babenokungabaza nge-cytotoxicity ephezulu, kodwa bathola nolunye uhlobo. ye-Ganoderma triterpenoid, i-ganoderol B, inomphumela ovimbelayo ku-H5N1 (kodwa umphumela wokuvimbela mubi), kodwa awuyona i-cytotoxic.Ngakho-ke, abacwaningi bakholelwa ukuthi indlela yokuthuthukisa ukuphepha kwe-ganoderic acids TQ ne-TR ngokuguqulwa kwesakhiwo samakhemikhali ngenkathi kugcinwa ukuvinjelwa komsebenzi we-neuraminidase kufanele kucatshangelwe ngokucophelela.

[Umthombo] Zhu Q, et al.Ukuvinjelwa kwe-neuraminidase nge-Ganoderma triterpenoids kanye nemithelela yokwakheka kwe-neuraminidase inhibitor.Sci Rep. 2015 Aug 26;5:13194.doi: 10.1038/srep13194.

PHELA

Mayelana nombhali/ Nks. Wu Tingyao
UWu Tingyao ubelokhu ebika ngolwazi lwe-Ganoderma lokuqala kusukela ngo-1999. Ungumbhali wencwadiUkwelapha nge-Ganoderma(ishicilelwe ku-People's Medical Publishing House ngo-Ephreli 2017).
 
★ Lesi sihloko sishicilelwe ngaphansi kokugunyazwa okukhethekile kombhali.★ Le misebenzi engenhla ayinakuphinda ikhiqizwe, ikhishwe noma isetshenziswe ngezinye izindlela ngaphandle kwemvume yombhali.★ Ngokuphulwa kwesitatimende esingenhla, umbhali uzolandela izibopho ezingokomthetho ezifanele.★ Umbhalo wokuqala walesi sihloko ubhalwe ngesiShayina nguWu Tingyao futhi wahunyushelwa esiNgisini ngu-Alfred Liu.Uma kukhona ukungqubuzana phakathi kokuhumusha (isiNgisi) kanye nokwangempela (isiShayina), isiShayina sangempela siyonqoba.Uma abafundi benemibuzo, sicela uthinte umbhali wokuqala, uNksz. Wu Tingyao.