Studies On The Chemical Constituents Of Picria Fel-terrae Lour. And Its Application

This thesis consists of four chapters altogether. The first chapter shows a review about theprogress of studies on Picria fel-terrae Lour. and reasons for the choice of this project. The secondchapter elaborates the identification of active fractions by pharmacological tests. The third chapterintroduces the isolation and verification of chemical constituents from Picria fel-terrae Lour. Inthe last chapter, the extraction and purification procedure of total triterpenoids from Picriafel-terrae Lour. is presented, and a TLCS for the determination of picfeltarraenins IA and IB and aspectrophotometry for the determination of triterpenoids are established. Chapter 1 Picria fel-terrae Lour., belonging to the genus Picria of the familyScrophulariaceae, has been used medically in the southern part of China against fever, cancer, andinflammation for more than 200 years. It was excavated and cultivated for the first time bybotanists of Guangxi Zhuang Autonomous region, where has become the main productive area ofthis plant. Chemical and pharmacological and clinical studies on Picria fel-terrae Lour. werecarried out subsequently, which led to the birth of at least five Traditional Chinese PatentMedicines. However, only triterpenoids and flavonoids from Picria fel-terrae have been reported so far,and its active constituents (or fraction) are still unidentifiable. Besides, the problems of massivedosage and rough standard of quality control exist in each Traditional Chinese Patent Medicinecontaining Picria fel-terrae. These facts mentioned above give the author a reason to investigate itfurther. Chapter 2 The ethanolic extract of Picria fel-terrae was fractioned with macroporous resin,and two fractions of which were proved to have pharmacological activities against inflammationand fungus. Moreover, the fraction of triterpenoids exhibited some promising response to immunetests, and its antitumor activity at the concentration of 0.25 mg·ml-1 was evaluated againstBEL-7402 liver cancer cell, A-549 lung cancer cell, P-388 and HL-60 leukaemia cell in vitro, withinhibiting rates of 74.3%, 94.3%, 67.8%, and 55.8%, respectively. Chapter 3 The investigations on the chemical constituents of Picria fel-terrae Lour. wereshown in this chapter. To search more bioactive constituents from this medical plant and to draw aclear face for the chemical studies on this plant which acts as the basis of the quality control ofrelational drugs, we systematically reinvestigated the chemical components of this plant collectedin Wuzhou city of Guangxi Zhuang Autonomous region of China, in October 2001. As a result, 30 compounds in all were isolated from this plant, and their structures wereelucidated on the basis of spectral evidences. Among them, 21 compounds were separated fromvi 苦玄参的化学成分研究及应用Picria fel-terrae Lour. for the first time, and 10 of which are new ones according to SCIFinder andBelstein.These compounds are listed below, and their structures and other messages in detail areshown in Table 1 of chapter 3. 1 Asperglaucide 2 1-hydroxy-7-hydroxymethyl-9,10-anthraquinone 3 1,2,5-trihydroxy-9,10-anthraquinone 4 5,7,4'-trihydroxy-flavone (apigenin) 5 9,16-dioxo-10,12,14-octadeca-trienoic acid 6 β-Sitosterol 7 Daucosterol 8 Picfeltarraenone I 9 PicfeltarraenoneII(new),2,11,22-trioxo-3α,16α-dihydroxy-(20S,25)-epoxy–cucurbit-5-ene 10 Picfeltarraegenin I 11 Picfeltarraegenin VI 12 Picfeltarraegenin VII (new), 11,22-dioxo-2β,3α,16α, 25-tetrahydroxy-(20S, 24)-epoxy-cucurbit-5-ene 13 Picfeltarraenin IA 14 Picfeltarraenin IB 15 Picfeltarraenin II 16 Picfeltarraenin IV 17 Picfeltarraenin VI 18 Picfeltarraenin VII 19 Picfeltarraenin X (new), picfeltarraegenin VI 2-O-β-D-glucopyranoside 20 Picfeltarraenin XI (new), 3,11,22-trioxo-16α-hydroxy-(20S,24)-epoxy-cucurbit-5,23-diene-2α-O-β-D-glucopyranoside...