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Discovery of Potent of New 4-oxothia.olidin-2-ylidene Deriva.ives Conta.ning Piperidinyl Moiety a.a.nsta.dose Reducta.e

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材料科学与工程（中英文a.） 2012年第2期2卷 220-231页

作者： areal a. farrag a.i.Kha.il Sha.a. Ibra.im Moha.ed a.med a. EI-Hena.a. Ga.eel a.a.ed Moha.ed El-Ha. a.il Yuosry a.med a.ma. Chemistry Depa.tment Faculty of Science AI-Azhar University Nasr City（Girls） Cairo Egypt Chemistry Depa.tment Faculty of Science Ain Shams University Cairo Egypt Technology Engineering Institute Tamoh Giza Egypt Chemistry Depa.tment Faculty of Science Al-Azhar University Nasr City Cairo（boys） Egypt Chemistry Depa.tment Faculty of Science King Khaled University Saudi Arabia Abha

2-(2-Oxo-2-(piperidin-1-yl)ethylidene)thia.olidin-4-one (1) wa. used a. a.key intermedia.e for the synthesis of ma.y thia.olo[3,2-a. pyridine deriva.ives. Thus, 4-thia.olidinine (1) wa. refluxed with a.oma.ic a.dehydes where the corresponding 4-thia.olidinone deriva.ives (2a. b) were a.forded. Cycliza.ion of (2a. b) with ma.ononitrile a.d a.dehydes ga.e the corresponding thia.olo[3,2-a. pyridines (5a. b). Thia.olo[3,2-a. na.hthyridine deriva.ives (6a. b) were obta.ned from the rea.tion of compounds (5a. b) with formic a.id. a.yla.ion of (5a. b) with a.etic a.hydride or benzoyl chloride for 2 h produced the corresponding a.ide deriva.ives (7,8). While, upon trea.ment of (5b) with a.etic a.hydride for 5 h furnished tricyclic structure (9). Furthermore, compounds (5a. b) were refluxed with either chloroa.etonitrile to give thia.olo[3,2-a. pyrrolo [2,3-c] pyridines (10a. b) or with ma.ononitrile to a.ford the corresponding thia.olo[3,2-a. na.hthyridine deriva.ives (14a. b). In a.dition, the corresponding thiourea.a.d Pyra.olo [3,4:4",5] thia.olo deriva.ives (15) a.d (16) were produced via.the rea.tion of 5 ethyl with ethylisothiocya.a.e a.d phenyl hydra.ine. Molecula. docking simula.ions into the a.tive site of a.R2 were performed, a.d showed tha., some of the synthesized compounds more suita.le inhibitor a.a.nst a.R2 with fa.ther modifica.ion in future.

关键词：吡啶衍生物哌啶基还原酶亚基萘衍生物噻唑啉酰胺衍生物噻唑衍生物

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Prelimina.y eva.ua.ion of the ra.iothera.eutic effica.y of 131I-a.orva.ta.in in ra.s with hepa.ocellula. ca.cinoma

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Nuclea. Science a.d Techniques 2020年第11期31卷 1-11页

作者： Nouriha. S.farrag a.eer M.a.in La.eled Compounds Depa.tment Hot Laboratories CentreEgyptian Atomic Energy Authority(EAEA)P.O.Box 13759CairoEgypt

a. one of the most critica. types of ca.cer,hepa.ocellula. ca.cinoma.HCC)a.fects ma.y people *** study demonstra.ed the prospective use of a.orva.ta.in,a.drug tha. inhibits the meva.ona.e pa.hwa.,ca.sing hypolipidemia.a. a.ca.rier to deliver the iodine-131(131I)isotope to liver tissues for HCC *** a.orva.ta.in ra.ioiodina.ion method wa. optimized for utilizing the131I *** ra.iochemica. qua.ity a.d the in vitro sta.ility of the genera.ed[131I]a.orva.ta.in were *** a.dition,the biodistribution experiments of[131I]a.orva.ta.in were eva.ua.ed in both norma. a.d HCC-induced ra. models.[131I]a.orva.ta.in wa. produced a. a.ma.imum ra.iochemica. yield of 86.7±0.49%.The[131I]a.orva.ta.in solution purified via.high-performa.ce liquid chroma.ogra.hy showed good in vitro sta.ility for 12 h a.ter *** a.a.yses revea.ed rema.ka.le liver ta.geting ca.a.ity of[131I]a.orva.ta.in a.d good loca.iza.ion of131I in liver ***,the encoura.ing biochemica. profile a.d histopa.hologica.findings ha.e been reported,a.d prelimina.y investiga.ions on the possible use of[131I]a.orva.ta.in a. a.ra.iotra.er a.d its impa.t on HCC ra.iothera.y in ra.s show promise.

关键词： Hepa.ocellula. ca.cinoma [131I]a.orva.ta.in Biodistribution Ra.iothera.y

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Decrea.ed a.optosis in a.va.ced-sta.e/high-gra.e hepa.ocellula. ca.cinoma.complica.ing chronic hepa.itis C is media.ed through the downregula.ion of p21 ra.

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Chinese Journa. of Ca.cer Resea.ch 2013年第3期25卷 281-288页

作者： Na.ed Ba.dour Ebteha. farrag a.med Zeid Essa. Bedewy Yousry Ta.er Depa.tments of Pa.hology Alexandria Egypt Depa.tments of Hepa.obilia.y Unit Internal MedicineAlexandria Egypt Depa.tments of Tropica. Medicine of the a.exa.dria.Fa.ulty of Medicine Alexandria Egypt

Objective a.d ba.kground： a.though p21 ra. ha. been reported to be upregula.ed in hepa.ocellula. ca.cinoma.complica.ing chronic hepa.itis C type I, p21 ra. ha. a.different role in a.va.ced sta.es, a. it ha. been found to be downregula.ed. The goa. of this study wa. to investiga.e the sta.us of p21 ra. in ea.ly-sta.e/low-gra.e a.d la.e-sta.e/high-gra.e hepa.ocellula. ca.cinoma.a.d its possible link to a.optosis. Ma.eria. a.d methods： Thirty-five ca.es ea.h of chronic HCV hepa.itis type 4 （group I） a.d cirrhosis with hepa.ocellula. ca.cinoma.（HCC） complica.ing chronic HCV hepa.itis （groups Ⅱ a.d Ⅲ） were immunohistochemica.ly eva.ua.ed using a.p21 ra. polyclona. a.tibody. The a.optotic index wa. determined in histologic sections using the termina. deoxynncleotidyl tra.sfera.e-media.ed d-UTP biotin nick end la.eling （TUNEL） a.sa.. Results： Significa.t differences （P=0.001） were detected in p21 ra. protein expression between the three groups. a.nea. 2-fold increa.e in p21 ra. sta.ning wa. observed in the cirrhotic ca.es compa.ed to the hepa.itis ca.es, a.d p21 ra. expression wa. decrea.ed in the HCC group, p21 ra. expression correla.ed with sta.e （r=0.64, P--0.001） a.d gra.e （r=-0.65, P=0.001） in the HCC group a.d gra.e in the HCV group （r=0.44, P=0.008）. Both p21 ra. expression a.d TUNEL-LI were significa.tly lower in la.ge HCCs compa.ed to sma.l HCCs （P=0.01 ea.h）. The TUNEL va.ues were nega.ively correla.ed with sta.e in the HCC group （r=-0.85, P=0.001）. The TUNEL va.ues were a.so nega.ively correla.ed with gra.e in both the HCV a.d HCC groups （r=0.89, P=0.001 a.d r=0.53, P=0.001, respectively）. The p21 ra. scores were significa.tly correla.ed with the TUNEL-LI va.ues in the HCC group （r=0.63, P=0.001） a.d HCV group （r=0.88, P=0.001）. Conclusions： p21 ra. a.ts a. a. initia.or in HCC complica.ing type 4 chronic HCV a.d is downregula.ed with HCC progression, which most likely promotes tumor cell surviva. beca.se it fa.ilita.es the downregula.ion of a.optosis with tumor

关键词： p21 ra. termina. deoxynucleotidyl tra.sfera.e-media.ed d-UTP biotin nick end la.eling (TUNEL) a.optosis HCV type 4 hepa.ocellula. ca.cinoma

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Micro-computed tomogra.hy utility for estima.ion of intra.a.enchyma. spina. cord cystic lesions in sma.l a.ima.s

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Neura. Regenera.ion Resea.ch 2021年第11期16卷 2293-2298页

作者： Ma.moud farrag Dipa. D.Puka.e Nic D.Leipzig Integra.ed Bioscience Progra. The University of AkronAkronOHUSA Depa.tment of Chemica. Biomolecularand Corrosion EngineeringThe University of AkronAkronOHUSA Depa.tment of Chemica. Biomolecularand Corrosion EngineeringIntegrated Bioscience ProgramThe University of AkronAkronOHUSA

Precise a.sessment of spina. cord cystic lesions is crucia. to formula.e effective thera.eutic stra.egies,yet histologica. a.sessment of the lesion rema.ns the prima.y method despite numerous studies showing inconsistent results rega.ding estima.ion of lesion size via.*** the other ha.d,despite numerous a.va.ces in micro-computed tomogra.hy(micro-CT)ima.ing a.d a.a.ysis tha. ha.e a.lowed precise mea.urements of lesion size,there is not enough published da.a.on its a.plica.ion to estima.e intra.pina. lesion size in la.ora.ory a.ima. *** work a.tempts to show tha. micro-CT ca. be va.ua.le for spina. cord injury resea.ch by demonstra.ing a.cura.e estima.ion of syrinx size a.d compa.es between micro-CT a.d tra.itiona. histologica. *** used a.post-tra.ma.ic syringomyelia.ra. model to compa.e micro-CT a.a.ysis to conventiona. histologica. *** study showed tha. micro-CT ca. detect lesions within the spina. cord very simila. to ***,micro-CT a.pea.s to provide more a.cura.e estima.es of the lesions with more mea.ures(e.g.,surfa.e a.ea.,ca. detect compounds within the cord,a.d ca. be done with the tissue of interest(spina. cord)*** summa.y,the experimenta. work presented here provides one of the first investiga.ions of the use of micro-CT for estima.ing the size of intra.a.enchyma. cysts a.d detecting ma.eria.s within the spina. *** a.ima. procedures were a.proved by the University of a.ron Institutiona. a.ima. Ca.e a.d Use Committee(Ia.UC)(protocol#LRE 16-05-09 a.proved on Ma. 14,2016).

关键词： cyst size histology intra.a.enchyma. cysts lesion size estima.e micro-CT post-tra.ma.ic syringomyelia spina. cord ima.ing spina. cord injury spina. cystic lesion syrinx

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High Ga.n Predictions for Ni-Like Ta.Ions

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Chinese Physics Letters 2013年第11期30卷 80-83页

作者： Wessa.eldin S.a.dela.iz a.a.farrag H.M.Ha.ed Ma. E.a.med Na.iona. Institute of La.er Enha.ced Sciences Cairo UniversityGizaEgypt Fa.ulty of Science Cairo UniversityGizaEgypt Environmenta. a.fa.rs a.ency(EEa.) Egypt

a.omic structure da.a.a.d effective collision strengths for 1s^(2)2s^(2)2p^(6)3s^(2)3p^(6)3d^(10) a.d 54 fine-structure levels a.e conta.ned in the configura.ions 1s^(2)2s^(2)2p^(6)3s^(2)3p^(6)3d^(9)4l(l=s,p,d,f)for the nickel-like Ta.*** da.a.a.e used in the determina.ion of the reduced popula.ion for the 55 fine structure levels over a.wide ra.ge of electron densities(from 10^(21) to 10^(23))a.d a. va.ious electron pla.ma.*** ga.n coefficients for those tra.sitions with a.positive popula.ion inversion fa.tor a.e determined a.d plotted a.a.nst the electron density.

关键词： density nickel structure

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Effica.y a.d Toxicity of Metronomic Ca.ecita.ine in a.va.ced Hepa.ocellula. Ca.cinoma

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Journa. of Ca.cer Thera.y 2012年第1期3卷 71-77页

作者： a.hra. farrag Clinica. Oncology Depa.tment Assiut University Hospital Assiut Egypt.

Ba.kground: Hepa.ocellula. ca.cinoma.(HCC) is a.hyperva.cula. tumor. Metronomic chemothera.y;the continuous a.ministra.ion of low-dose chemothera.y;ha. both cytotoxic a.d a.tia.giogenic effects with low toxicity profile. We eva.ua.ed the effica.y a.d toxicity of metronomic ca.ecita.ine (MC) in pa.ients with a.va.ced HCC. Pa.ients a.d Methods: From Ma. 2010, we enrolled pts with either meta.ta.ic or loca.ly a.va.ced disea.es not ca.dida.e for a.la.ive or locoregiona. trea.ment a.d ha.e a.cepta.le liver function. Pa.ients received ora. MC in dose of 1000 mg/m2 da.ly in a.21 da.s cycle without interruption till disea.e progression or toxicity. Results: The study cohort consisted of 22 pa.ients with a.media. a.e of 63 yea.s. The media. number of cycles received wa. 3 cycles (ra.ge 1 - 9). From 19 pa.ients were eva.ua.le for response we ha. 3 pa.tia. responders, 10 sta.le disea.es a.d disea.e progression in 6 pa.ients. Media. time to progression (TTP) wa. 2.2 months (95% CI 1.4 - 6.24) a.d media. surviva. time (OS) wa. 4.8 months (95% CI 1.8 - 7.9). For 20 pa.ients eva.ua.le for sa.ety: no gra.e III/IV hema.ologica. toxic effects were observed. Non-hema.ologica. toxic effects included gra.e III vomiting a.d dia.rhea.in one pa.ient a.d gra.e III ha.d-foot syndrome in one pa.ient. There wa. no trea.ment-rela.ed morta.ity. Conclusions: Ba.ed on the observed response ra.e, TTP a.d OS;MC ha. a.modest a.titumor effica.y in pts with a.va.ced HCC. However, due to its low toxicity profile it deserves further a.tention a. a.convenient, outpa.ient-ba.ed chemothera.y regimen.

关键词： Metronomic Chemothera.y Ca.ecita.ine Hepa.ocellula. Ca.cinoma

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Chronic intestina. fa.lure a.d short bowel syndrome in Crohn’s disea.e

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World Journa. of Ga.troenterology 2021年第24期27卷 3440-3465页

作者： a.segül a.sa. Ka.ima.farrag Irina.Blumenstein Oliver Schröder a.el U Digna.s Jürgen Stein Institute of Nutritiona. Sciences Justus-Liebig-UniversitätGiessen 35392Germany Depa.tment of Clinica. Resea.ch Interdisziplinäres Crohn Colitis Centrum Rhein-MainFrankfurt am Main 60594Germany Depa.tment of Ga.troenterology a.d Clinica. Nutrition DGD Kliniken SachsenhausenTeaching Hospital of the JW Goethe UniversityFrankfurt am Main 60594Germany Depa.tment of Ga.troenterology Hepatology and Clinical NutritionFirst Medical ClinicJW Goethe University HospitalFrankfurt am Main 60529Germany Depa.tment of MedicineⅠ Agaplesion Markus HospitalGoethe-UniversityFrankfurt am Main 60431Germany Institute of Pha.ma.eutica. Chemistry JW Goethe University60438 Frankfurt am MainGermany

Chronic intestina. fa.lure(CIF)is a.ra.e but fea.ed complica.ion of Crohn’s *** on the rema.ning length of the sma.l intestine,the a.fected intestina. segment,a.d the residua. bowel function,CIF ca. result in a.wide spectrum of symptoms,from single micronutrient ma.a.sorption to complete intestina. *** of CIF ha. improved significa.tly in recent *** in home-ba.ed pa.entera. nutrition,in pa.ticula.,ha.e tra.sla.ed into increa.ed surviva. a.d improved qua.ity of ***,60%of pa.ients a.e perma.ently relia.t on pa.entera. *** results with new drugs such a. teduglutide ha.e a.ded a.new dimension to CIF *** outcomes of pa.ients with CIF could be grea.ly improved by more effective prevention,understa.ding,a.d *** complex ca.es,the ca.e of pa.ients with CIF requires a.multidisciplina.y a.proa.h involving not only physicia.s but a.so dietitia.s a.d nurses to provide optima. intestina. reha.ilita.ion,nutritiona. support,a.d a. improved qua.ity of ***,we summa.ize current litera.ure on CIF a.d short bowel syndrome,encompa.sing epidemiology,pa.hophysiology,a.d a.va.ces in surgica. a.d medica. ma.a.ement,a.d elucida.e a.va.ces in the understa.ding a.d thera.y of CIF-rela.ed complica.ions such a. ca.heter-rela.ed bloodstrea. infections a.d intestina. fa.lure-a.socia.ed liver disea.e.

关键词： Chronic intestina. fa.lure Short bowel syndrome Crohn's disea.e Infla.ma.ory bowel disea.e Pa.entera. nutrition Intestina. fa.lure-a.socia.ed liver disea.e

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Percuta.eous Ba.loon Compression a.d Percuta.eous Ra.iofrequency a.la.ion in Pa.ients with Idiopa.hic Trigemina. Neura.gia. Ma.a.ement Outcome

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Open Journa. of Modern Neurosurgery 2019年第4期9卷 393-400页

作者： a.i R. Ha.da. Ra.wa. Nouby Ma.moud Moha.a. a. farrag Depa.tment of Neurosurgery South Valley University Qena Egypt Depa.tment of Neurosurgery Assuit University Assuit Egypt

Ba.kground: Trigemina. neura.gia.is a.chronic pa.n syndrome cha.a.terized by pa.oxysma., shock-like, sta.bing, recurrent episodes of pa.n loca.ized in the distribution a.ea.of one or more bra.ches of the trigemina. nerve. The Initia. a.proa.h for trea.ing trigemina. neura.gia.consists of pha.ma.ologica. thera.y. Ma.y pa.ients experience initia. pa.n relief with pha.ma.ologica. thera.y;however, most of those pa.ients eventua.ly undergo surgery. Pa.ients a.d Methods: In this descriptive prospective study, we eva.ua.e the efficiency a.d sa.ety of percuta.eous ba.loon compression (PBC) a.d percuta.eous ra.iofrequency a.la.ion (RFa. in trea.ing pa.ients with typica. idiopa.hic trigemina. neura.gia. This study includes 21 pa.ients (divided into two groups, PBC = 15 pa.ients a.d RFa.= six pa.ients) who met our inclusion a.d exclusion criteria. from Ma. 2018 to a.ril 2019, with a.follow-up period of six months. Results: a. one month postopera.ive follow-up, a.l pa.ients in both groups were pa.n-free. a. six months postopera.ive follow-up, in group 1 (PBC), 14 (95.24%) pa.ients were pa.n-free, while in group 2 (RFa. a.l pa.ients rema.ned pa.n-free. The most common encountered postopera.ive complica.ions a.e ma.tica.ory muscles wea.ness (Four pa.ients in PBC group, a.d one pa.ient in RFa.group) a.d fa.ia. hypothesia.(12 pa.ients in PBC group a.d four pa.ients in RFa.group). Conclusions: In our study, pa.ients with trigemina. neura.gia.were not controlled by drug trea.ment, but percuta.eous ba.loon compression a.d percuta.eous ra.iofrequency a.la.ion proved to be very effective trea.ment options, with no ma.or complica.ions.

关键词： Trigemina. Neura.gia Percuta.eous Ba.loon Compression Percuta.eous Ra.iofrequency a.la.ion

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Intra.ra.ia. a.herosclerosis: The Na.ura. History a.d Ma.a.ement Stra.egies

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World Journa. of Ca.diova.cula. Disea.es 2014年第7期4卷 350-360页

作者： Ossa.a.Ma.sour Ma.tin Schuma.her Moha.ma. a. farrag Foa. a.d-a.la. Freiburg Uniklinik Neurozentrium Neuroradiologie Abt. Freiburg Germany Neurology a.d Interventiona. Neurology Service Depa.tment Alexandria University Hospital Alexandria Egypt Neurology Depa.tment Cairo University Hospitals Cairo Egypt

Intra.ra.ia. a.herosclerotic disea.e (ICa.) represents a.ma.or ca.se of stroke a.d tra.sient ischemic a.ta.ks. The preva.ence a.d na.ura. course of ICa. a.e closely rela.ed to ra.e a.d ethnicity. The best trea.ment for ICa. is a.crucia. issue;da.a.from recent tria.s indica.e tha. a.gressive medica. ma.a.ement a.d life style modifica.ions a.e better tha. endova.cula. trea.ments for prevention of recurrent stroke in high-risk pa.ients with ICa.. Endova.cula. trea.ment is still a. option for subgroup of pa.ients who a.e not responded to optima. medica. thera.y.

关键词： Intra.ra.ia. a.herosclerosis Medica. Thera.y Endova.cula. Trea.ment

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Soft cora. Cespitula.ia.stolonifera.New cytotoxic cera.ides a.d ga.troprotective a.tivity

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Chinese Journa. of Na.ura. Medicines 2017年第2期15卷 105-114页

作者： a.delsa.ed I.Elsha.y Wa.a. a.El-Ka.ha. Heba.M.I.a.da.la. a.delra.ik H.farrag Ma.moud I.Na.sa. Na.ura. Compounds Chemistry Depa.tment National Research CentreGiza 12622Egypt Pha.ma.ology Depa.tment National Research CentreGiza 12622Egypt Pa.hology Depa.tment Na.iona. Resea.ch Centre Giza 12622Egypt

In the present study, a.new cera.ide, na.ely 2S, 3R-4E, 8E-2-(hepta.eca.oyla.ino)-hepta.eca.4, 8-diene-1, 3-diol(1), a.ong with four known steroids, including 24-methylcholesta.5, 24(28)-diene-3β-ol(2), 24-methylcholesta.5, 24(28)-diene-3β-a.eta.e(3), 4-methyl-24-methylcholesta. 22-ene-3-ol(4), a.d cholesterol, wa. isola.ed a.d cha.a.terized from CH2Cl2/Me OH extra.t of Cespitula.ia.stolonifera. a.new a.eta.e deriva.ive of compound 1, termed 2S, 3R-4E, 8E-2-(hepta.eca.oyla.ino)-hepta.eca.4, 8-diene-1, 3-dia.eta.e(1a., wa. a.so prepa.ed in the present study. a.l the structures were esta.lished on the ba.is of modern spectroscopic techniques, including FT-IR, 1D, 2D-NMR, HRESI-MS, a.d GC-MS, in a.dition of chemica. methods.(-)-a.loa.oma.endren, leda.e,(1)-a.loa.oma.endren oxide, isoa.oma.endrene epoxide a.d(-)-ca.yophellen oxide were identified from the n-hexa.e fra.tion using GC-MS. The extra.t a.d the two cera.ides(1) a.d(1a. exhibited significa.t cytotoxic a.tivity a.a.nst lung ca.cer a.49 cells, while the extra.t a.d the two steroids(2) a.d(3) exhibited significa.t cytotoxic a.tivity a.a.nst brea.t ca.cer MCF-7 cells. The CH_2Cl_2/MeOH extra.t exhibited significa.t a.tiulcer a.tivity in both etha.ol a.d a.etic a.id induced ulcer models in ra.s, a. evidenced by histopa.hologica., histochemica., a.d biochemica. exa.ina.ions.

关键词： Cespitula.ia.stolonifera Cera.ide Steroids a.tica.cer lea.ing constituents a.tiulcer a.tivity

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