Immunosuppressive terpenoids from Tripterygium wilfordii

Two new terpenes,triptobenzene P（1）and wilforone（2）were isolated from Tripterygium wilfordii,as well as 10 known terpenes.Their structures were elucidated by spectroscopic methods.Compounds 2-4,8,10,and 11 showed significant immunosuppressive activities.

In vitro propagation of a medicinal plant: Tripterygium wilfordii Hook f.

In this study a reliable protocol was developed for the establishment of commercial in vitro cultures of Tripterygium wilfordii Hook f.. Juvenile shoots from one-year-old elite plants were used as the source of explants. New axillary shoots were obtained after 30 days of culture on a MS medium supplemented with BAP （2.0 mg.L^-1） and NAA （0.1 mg.L^-1）. The optimal multiplication medium was a modified MS medium supplemented with BAP （1.0 mg.L^-1） and NAA （0.1 mg.L^-1）. This yielded a multiplication rate of 2.4 for each subculture. Slightly more than 92% of shoots rooted when cultured on a modified MS medium containing IBA （0.2 mg.L^-1） and activated charcoal （0.5 mg.L^-1）. Activated charcoal promoted both a strong and a high rooting rate during the rooting phase. Plantlets were transferred to pots for a short acclimatization stage in a greenhouse where 95% of the plantlets survived. This highly reproducible procedure can be adopted for large-scale propagation of T. wilfordii.

A new triterpenoid from the roots of Tripterygium wilfordii

A new triterpenoid 3,4,6-trihydroxy-2-oxo-1(10),3,5,7-tetraen-23,24-nor-D:A-friedooleana-29-oic acid,as well as twelve known terpenes were isolated from the roots of Tripterygium wilfordii.Its structure was established on the basis of spectroscopic methods.

Two new terpenes from Tripterygium wilfordii

Two new terpenes,wilfornine H(1) and triptobenzene Q(2) were isolated from Tripterygium wilfordii,as well as 11 terpenes. Their structures were elucidated by spectroscopic methods.Compounds 5,9-13 showed significant immunosuppressive activities.

Three new sesquiterpene alkaloids from the root of Tripterygium wilfordii

三新 sesquiterpene 碱， 1-desacetylwilforgine (1 ) ， 1-desacetylwilforine (2 ) ，和 9 鈥 ? hydroxy-2-nicotinoylwilforine (3 ) 从 Tripterygium wilfordii 钩 f. 的根被孤立，与六已知的碱一起。他们的结构被建立根据光谱分析。

Isolation and Purification of Triptolide from the Leaves of Tripterygium wilfordii Hook F

Triptolide is an important active component of Tripterygium wilfordii Hook F (TWHF) and possesses anti-inflammatory, immunosuppressive, male anti-fertility, and anticancer properties. A new method combining different techniques, including solid-liquid extraction, liquid-liquid partition, column chromatography and high-speed counter-current chromatography (HSCCC) but avoiding the use of chloroform, was developed for the isolation and purification of triptolide from the leaves of TWHF. 48 mg of triptolide at 96.5% purity was obtained from 1 kg of air-dried leaves of TWHF.

Progress of Botanical Resources, Chemical Ingredients and Pharmacolo- gical Study of Tripterygium Wilfordii

Tripterygium Wilfordii Hooks. f (TW) also called yellow vine, yellow vine wood, yellow wax vine, breakgut herb etc., belongs to Galactia genus, its medicinal parts mostly belong to the wooden part of the double-layer decortical root. Traditional Chinese medicine (TCM) holds that it has the function of clearing Heat and removing toxin, dispelling Wind to fr- ee collateral, relaxing tendon to activate blood circulation, subsiding swelling and analgesia, insecticide and hemostasis. The studies on botanical resources, chemical ingredients and pharmacology of TW are briefly introduced as follows.

A Brief Review and Prospect of Treatment of Proteinuria by Tripterygium Wilfordii

Tripterygium wilfordii (TW) was reported by LI Lei-shi, et al in 1981 to have marked effect in reducing proteinuria when it was used to treat glomerular nephritis, and the conclusion they worked out has been now accepted by most of nephrologists in 20-year experimental studies and wide application in clinical practice. Its mechanism, adverse reaction and mutagenesis effects, and dosage in clinical application in the recent years are now briefly reviewed in this paper.

Effect of the Multiglycoside of Tripterygium Wilfordii Hook f. (Tii) on Cornea Allograft Rejection Model in Rabbit

Purpose:Toexamine the effect of Tii treatment of cornea graft survival in a rab-bit model.Methods:Tii was administrated orally after eccentrical corneal transplantation.Survival times were determined by biomicroscopy.Cytotoxic T lymphocytes(CTL)and delayed-type hypersensitivity(DTH)responses to donor alloantigens were assessed at ady 16after heterotopic corneal grafts.Results:Administration of Tii reduced the incidence and prologed the graft sur-vival time.Both CTLand DTH responses to donor alloantigens were severely ed-pressed in hosts treated with Tii.However,combination of Tii and cyclosporine further enhanced the immunosuppressive effects described above.Conclusions:Tii is a potent immunosuppressant with the ability to prolong allo-graft survival in the rabbit penetrating keratoplasty model and may have coordi-native effects with CsA through different mechanisms.Further studies are neces-sary to define any potentially coordinative role in the prevention of allograft rejec-tion in human keratoplasty.Eye Science 1995;11:168-172.

A Novel Diterpenoid,11-O-β-D-glucopyranosylneo-triptophenolide, from Tripterygium wilfordii Hook. f

A new diterpenoid was isolated from the ethanolic extract of the dried root bark of Tripterygium wilfordii Hook.f. It is the first example of abietane diterpenoid glycoside isolated from Tripterygium wilfordii Hook.f. Its structure was identified to be 11-O-b-D-glucopyranosyl- neotriptophenolide based on spectral methods.

Tripterygium Wilfordii： Structure，Chemistry and Activityof Male Antifertility Constituents

ＴｒｉｐｔｅｒｙｇｉｕｍＷｉｌｆｏｒｄｉｉ：Ｓｔｒｕｃｔｕｒｅ，ＣｈｅｍｉｓｔｒｙａｎｄＡｃｔｉｖｉｔｙｏｆＭａｌｅＡｎｔｉｆｅｒｔｉｌｉｔｙＣｏｎｓｔｉｔｕｅｎｔｓＳＡＭａｔｌｉｎ；ＡＢｅｌｅｎｇｕｅｒ；ＶＥＳｔａｃｅｙ；ＳＺＱｉａｎ；ＹＸｕ；ＪＷ...

Identification of Genes Involved in Celastrol Biosynthesis by Comparative Transcriptome Analysis in Tripterygium wilfordii

Tripterygium wilfordii has been renowned mostly because of the anticancer effects of its root extracts,which is partly ascribed to the presence of celastrol,a pentacyclic triterpenoid,as one of the main active components.Celastrol also has recently been reported as an effective prodrug in the treatment of obesity.Despite the promising activities,the pathway leading to celastrol biosynthesis,especially cytochrome P450(CYP)enzyme(s)that occur in its downstream steps,are largely unknown.This study conducted a comparative analysis of the T.wilfordii transcriptome derived from its root and leaf tissues.Differential gene expression analysis identified a number of root-specific CYP genes.Further phylogenetic analysis suggested specific family members of CYPs that may participate in the late steps during celastrol biosynthesis.Root-specific transcription factors(TFs)that may play regulatory roles in celastrol biosynthesis were also discussed.This genetic resource will aid in isolating the celastrol biosynthetic genes as well as engineering the celastrol biosynthesis pathway.

The Effect of Tripterygium Wilfordii Monomer T4 on Rat Spermatid Nuclear Protein Transition

Rat testis elongating spermatids and epididymal sperms were collected after 7 weeks of treatment with Tripterygium wilfordii monomer T4.Total nuclear basic protein(TNBP)was extracted from the elongating spermatid nuclei and the sperm nuclei isolated by sonication.Polyacrylamide gel electrophoresis has been used to separate the TNBP and individual proteins were quantified by scanning microdensitometry.It was found that the content of protamine was reduced and the TH(Total Histones)/RP(Rat Protamine)ratios were increased following treatment in the testis elongating spermatids, and same result was found in the epididymal sperms.These results suggest that the interruption of nuclear protein transition of testis spermatids induced by T4 might cause aberrant epididymal sperm nuclear protein and lead to infertility.The relationship between protamine and fertility was discussed.

HISTOCHEMICAL EFFECT OF THE MULTIGLYCOSIDES OF TRIPTERYGIUM WILFORDII HOOK.F.(GTW)ON THE TESTIS AND EPIDIDYMIS OF RATS

SD Twenty adult male rats were equally divided into a contro1 and an experimcntal group.GTW,10 mg/kg per day,was given to the experimental rats through gastric gavage 6 days a week for 8 weeks.To the control rats,the same amount of vehicle was given The animals were sacrificed when they became infertile and the fol1owing parameters of the testis and epididymis were examined:l)DNA(Feulgen′s method),2)RNA(Brachet′s tech-uique),3)LDH-X(Lojda′s method),4)ATPase(Wachstein′s procedure),5)Succinate dehydrc-genase(SDH,Pearson's method),6)Non-specific esterase(NSE,Lojda's technique)and 7)PAS reaction.Routine examination of the epididymal spermatozoa was also carried out.

Observations on Therapeutic Effects of Huangdan Decoction and Tripterygium Wilfordii Compound Tablet on Membranous Glomerulon

The model of membranous glomerulonephritis(MGN)in rats was successfully established using self-made cationic bovine serum albumin(C-BSA)and treated with Huangdan Decoction (HDD) and Tripterygium Wilfordii Co.tablet(TW).Results indicated that the levels of urinary protein,blood urea nitrogen(BUN)and serum creatinine(Scr) in treated groups(groups A,B and C)were significantly decreased as compared with the control group(group D)(PM0.01).By light and electron microscope and immunofluorescent technique,the damage to kidney in groups A,B and C was found much milder than that in group D with lesion in group A being slightest.These findings suggest that HDD and TW may alleviate the pathological lesions of MGN,prevent or retard its progression,and have remarkable therapeutic effects on MGN.

United observation and analysis of the effect of tripterygium wilfordii on sex hormone levels, apoptosis in ovary and bone metabolism in female rats

Objective:To study the effect of tripterygium wilfordii on sex hormone levels, apoptosis in ovary and bone metabolism in female rats.Methods: Adult female SD rats were chosen as experimental animals and divided into model group and control group, model group were made into premature ovarian failure models through intragastric administration of tripterygium wilfordii, and control group were given intragastric administration of same dose of normal saline. Serum was collected 14 d after model making to determine the contents of sex hormones and bone metabolism markers, ovarian tissue was collected to determine the expression of apoptosis genes and tibial tissue was collected to determine the expression of bone metabolism marker genes.Results: FSH, LH,β-CTX and TRACP5b levels in serum of model group were significantly higher than those of control group whereas E2, PINP and N-MID levels were significantly lower than those of control group;Fas, FasL, APAF-1 and Caspase-3 mRNA expression in ovarian tissue of model group were significantly higher than those of control group whereas Bcl-2 and XIAP mRNA expression were significantly lower than those of control group;RUNX2, BAP and OPG mRNA expression in bone tissue of model group were significantly lower than those of control group whereas RANKL and RANK mRNA expression were significantly higher than those of control group.Conclusion:There are sex hormone changes, apoptosis aggravation in ovarian tissue and systemic bone metabolism disorder in rat model with tripterygium wilfordii-induced premature ovarian failure.

Comparative Potency of Seven Compounds Isolated from Tripterygium Wilfordii on Cultred Rat Leydig Cells and Sertoli Cells

The damaging effect of seven compounds isolated from Triplelygium Wilfordii Hook.F were tested on the rat Leydig cells and Sertoli cells in culture. The reslllts showed thai 10 μg/ ml orthosphenic acid (TW2), 10μg/ ml 39,22α -dihydroxy-△12 ursen- 30-oic acid(TW5), 5.0 μg/ ml 39,22a--dihydroxy-△12-oleallen--29-oic acid(TW6), 5.0 μg/ ml salaspermic acid(TW7), 0.5μg/ ml celastrol(TW27) alld 1.25μg/ ml polpunonic acid (TW28) Ivere all detrimental to Leydig cells. and Sertoli cells. Holvever, 30 μg/ ml wilforlide A (TW1) did not affect the viability of Leydig cells and Sertoli cells significantly.The most toxic compounds was TW27, and the leasl,TW1.These results suggested that the-COOH at the C-20 site of these triterpenoids may be the functional chemical group responsible for the damaging effect on the Leydig cells and Sertoli. cells.

Effects of Tripterygium wilfordii combined with viaminate capsules on psoriasis patients' immune indexes, endothelium, inflammatory reaction, sICAM-1 and NF-kB

Objective: To explore the effects of Tripterygium wilfordii combined with viaminate on psoriasis patients' immune indexes, endothelium, inflammatory reaction, sICAM-1 and NF-kB. Methods: A total of 112 patients with psoriasis admitted in our hospital from September 2015 to November 2017 were randomly divided into control group (n=56) and observation group (n=56). The control group was treated only by Viaminate Capsules, and the observation group was treated with Tripterygium wilfordii tablet on the basis of the control group, the immune function, endothelial, inflammatory response, soluble intercellular adhesion molecules-1 (sICAM-1) and nuclear transcription factor-kB (NF-kB) expression levels were compared before and after treatment in the two groups. Results: Before treatment, CD4+, CD8+, CD4+/CD8+, vascular endothelial growth factor (VEGF), nitric oxide (NO), endothelin-1 (ET-1), tumor necrosis factor-α (TNF-α), interferon-γ (IFN-γ), NF-kB, and sICAM-1 in two groups were no significant difference. After treatment, CD4+and CD4+/CD8+in both groups were significantly increased, while CD8+was significantly lower than before treatment, the CD4+and CD4+/CD8+in the observation group were significantly higher than those in the control group, and CD8+was obviously lower than that of the control group;The VEGF, NO and ET-1 in both groups were dramatically lower than those before treatment, and the VEGF, NO and ET-1 in the observation group were significantly lower than those in the control group;The TNF-α and IFN-γ in two groups were significantly lower than before treatment, and TNF-α and IFN-γ in the observation group were remarkably lower than those in the control group;The NF-kB and sICAM-1 in two groups were obviously decreased than those before treatment, and the NF-kB and sICAM-1 in the observation group were significantly lower than those in the control group. Conclusion: Tripterygium wilfordii combined with viaminate capsules in the treatment of psoriasis patients, can effectively correct their immune dysfunction, improve endothelial function, reduce inflammatory response and inhibit the expression of NF-kB and sICAM-1 expression.

Curative efficacy of vitamin D3 in combination with tripterygium wilfordii polyglycoside in patients with rheumatoid arthritis and its influences on indices of bone restoration

Objective: To investigate the curative efficacy of vitamin D3 in combination with tripterygium wilfordii polyglycoside in patients with rheumatoid arthritis (RA) and its influences on indices of bone restoration. Methods: A total of 320 patients with RA were collected as observation objects to be randomly divided into the control group and the observation group with 160 cases in each group. The control group was given treatment of tripterygium wilfordii polyglycoside, while the observation group was given treatment of vitamin D3 in combination with tripterygium wilfordii polyglycoside. All patients received a course treatment with 3 months. The curative efficacy, improvement of joint symptoms, changes of laboratory tests, indices of bone restoration and adverse reactions were compared. Results: After 3 months, assessment of curative efficacy showed that the observation group had a total curative efficiency ratio of 90.6%, which was significantly higher than that of 81.2% in the control group. Among the indices which reflect the improvement of joint symptoms, the joint pain index, joint tenderness index and joint swollenness index were statistically reduced in the observation group than those in the control group. And after treatment, in comparison with the control group, indices of laboratory tests of rheumatoid factor (RF), antistreptolyisn O antibody (ASO), c-reactive protein (CRP) were statistically lower respectively in the observation group. As to indices of bone restoration after treatment, the observation group had statistically lower serum level of receptor activator of nf-kb ligand (RNKL) and higher level of osteoprotegerin (OPG) than those in the control group. During the treatment, incidences of adverse reactions in the control group and the observation group were statistically same. Conclusion: Vitamin D3 in combination with tripterygium wilfordii polyglycoside has well curative efficacy in patients with RA, which can significantly improve joint symptoms, indices of laboratory tests and bone restoration.

CLINICAL STUDY ON EFFECT OF TRIPTERYGIUM WILFORDII HOOK. F. GLYCOSIDES ON UTERINE LEIOMYOMA

To observe the therapeutic effect and side reactions of Tripterygium wilfordii Hook.f (GTW) glycosides on patients with uterine leiomyomas. Methods 65 normally cycling women with symptomatic uterine leiomyomas received 40mg daily dose GTW for 3 to 6 months. Baseline ultrasound tests were obtained to evaluate the sizes of myomas and uterus, then repeated three and six months after treatment. Blood samples were collected to determine the hormonal levels of in the mid-follicular and mid-luteal phases of the menstrual cycles before GTW therapy and at 3～4 months and 5～6 months after treatment. Results Significant decrease in leiomyoma volume was shown in 39 of 65 (60%) and 28 of 40 ( 70% ) patients after 3～4 months and 5～6 months of treatment, respectively. The decrease of the volume of leiomyoma was time-dependent as while 27. 84% and 51.60% in 3～4 months and 5～6months, respectively. 25 of 65 patients had amenorrhea during the course of treatment. Tripterygium wilfordii glycosides treatment induced a significant increase in LH and FSH levels (P <0. O1 ) as compared with pretreatment values, hi contrary, a significant decrease in E2 and P levels ( P <0. 05) was found, but no changes were observed in T and PRL levels after treatment. Conclusion Tripterygium wilfordii might serve as an effective therapeutic agent for leiomyomas with fewer side effects. A reversible inhibitory, effect on the ovary by Tripterygium wilfordii glycosides may be one of the mechanisms of Tripterygium wilfordii in decreasing leiomyoma volume.