鱼藤的三个新三萜化合物

从民间杀虫植物鱼藤（Derris eriocarpa How)的根中分离得到5个三萜化合物,经波谱和化学分析确定了这些化合物的化学结构,其中化合物1（3β,15α-dihydroxy-olean-12(13)-en-16-one),2(3β,15α,23-trihydroxy-olean-12(13)en-16-one),3(15α-hydroxyl-16-oxo-olean-12(13)-en-3-O-β-glucuronopyranoside)为新化合物,命名为鱼藤三萜素A,B,C。两个已知三萜为2β,3β,28-三羟基-12（13）-烯-齐墩果烷和β-香树脂素（β-amyrin)。另外还得到了二十七碳脂肪酸单甘油酯和β-谷甾醇。     

Nitric oxide-donating derivatives of hederacolchiside A1: Synthesis and biological evaluation in vitro and in vivo as potential anticancer agents

A series of nitric oxide (NO) donating derivatives of hederacolchiside A₁ bearing triterpenoid saponin motif were designed, synthesized and evaluated for their anticancer activity. All of the tested furoxan-based NO releasing compounds showed significant proliferation inhibitory activities. Especially compound 6a exhibited strong cytotoxicity (IC₅₀ = 1.6–6.5 μM) against four human tumor cell lines (SMMC-7721, NCI-H460, U251, HCT-116) in vitro and the highest level of NO releasing. Furthermore, compound 6a was revealed low acute toxicity to mice and weak haemolytic activity with potent tumor growth inhibition against mice H22 hepatocellular cells in vivo (51.5%).     

齿叶黄皮的化学成分研究

从药用植物齿叶黄皮（clausena dunniana)叶中分离了6个化合物。通过化学方法和波谱分析已知物数据对照,分别鉴定为：β－谷甾醇（β－sitosterol,1),谷甾醇（stigmasterol,2）,硬脂酸（steraric acid,30,桦木酸(betulinic acid,4),pomolic acid(5),熊果醇（uvaol,6),上述化合物在该植物中均为首次获得。     

Study on the Triterpenoids of Tripterygium regeli

Ten triterpenoids were isolated from the ethanol extract of the roots of Tripteryglum regeli collected from Jilin Province, north-eastern China. They were identified as wilforlide A(1), wilforlide B(2), regelide (3) 3β-hydroxy-olean-ll,13(18)-diene (4), orthosphenic acid (5), salaspermic acid (6), 3-epikatonic acid(7), maytenfolic acid (8), 3β-acetyl-oleanolic acid (9), and celastrol (19), by spectroscopic analyses and chemical correlations. Compound 3—10 were isolated from T. regeli for the first time, among them regelide 3 was a new comound and its structure was elucidated to be 3-keto-22α-hydroxy-olean-ll,13(18)-dien-29-oic acid(29, 22α)-lactone. 3-epikatonic acid(7)showed obvious spermicidal effect, while cealstrol (10)revealed significant immunosuppressive activity.     

Saponins of the Rhizome of Panax japonicus C. A. Meyer var. major (Burk.)Wu et Feng Collected in Qinling Mountain (Shaanxi)

From the rhizome of Panax japonicus C. A. Meyer var major (Burk.) Wu et Feng, collected in Qinling Mountain (Shaanxi), seven saponins were isolated. By means of 13C NMR, FAB-MS and comparison with authentic samples, six of them were identified with chikusetsusaponin Ⅴ (=ginsenoside Ro), Ⅳa, oleanolic acid 28-O-β-D-glucoside, ginsenoside Re, Rg2 and notoginsenoside R2. Another saponin was proved to be chikusetsusaponin Ⅳa methylester, and its structure was elucidated to be oleanolic acid (3-O-β-D-glucorunopyranosyl-methylate)-28-O-β-D-glucopyranoside. A comparison of sapoinin constituents of this variety collected in Qinling Mountain (Shaanxi) and Hengduan Mountains (Yunnan) was provided. As a common characteristic of both rhizome, it has been proved that the saponins of oleanane type were main constituents and the saponins of dammarane type were minor constituents. But some differences also has been found in both materials (Tab. 1). From the relationship between the biosynthesis pathway of triterpenoids and plant phytogenetics, this is a phenomenon of chemical polymorphism in a variety, which followed in the train of geographical distribution, ledto appearance of a che- mical evolution in the process of evolution and of spread of this variety.     

Pendulaosides A and B. Two acylated triterpenoid saponins from Harpullia pendula seed extract

Two new acylated triterpenoid saponins named pendulaosides A and B as well as the known phenolic compounds methyl gallate, gallic acid, 1,2,3,6-tera-O-galloyl-β-d-glucose and 1,2,3,4,6-penta-O-galloyl-β-d-glucose, were isolated from the seeds of Harpullia pendula. The structures of pendulaosides A and B were determined using extensive 1D and 2D NMR analysis and mass spectrometry as well as acid hydrolysis, as 3-O-β-d-glucopyranosyl-(1→2)-[α-L-arabinofuranosyl-(1→3)]-β-d-glucuronopyranosyl-22-O-angeloyl-3β,16α,22α,24β,28-pentahydroxylolean-12-ene and 3-O-β-d-glucopyranosyl-(1→2)-[α-L-arabinofuranosyl-(1→3)]-β-d-glucuronopyranosyl-16-O-(2-methylbutyroyl)-3β,16α,22α,24β,28-pentahydroxylolean-12-ene, respectively. To the best of our knowledge the two triterpene parts 22-O-angeloyl-3β,16α,22α,24β,28-pentahydroxylolean-12-ene and16-O-(2-methylbutyroyl)-3β,16α,22α,24β,28-pentahydroxylolean-12-ene have never been characterized before. The two isolated saponins were assayed for their in-vitro cytotoxic activity against the three human tumor cell lines HepG2, MCF7 and PC3. The results showed that pendulaoside A exhibited moderate activity on PC3 cell line with IC50value equal to 13.0 μM and weak activity on HepG2 cell line with IC50 value equal to 41.0 μM. Pendulaoside B proved to be inactive against the three used cell lines.     

New oleanane saponins from Schefflera kwangsiensis

Four new oleanane-type triterpenoid saponins, schefflesides I–L (1–4), were isolated from the aerial parts of Schefflera kwangsiensis. Their structures were established as oleanolic acid 3-O-β-d-glucopyranosyl (1 → 2) [α-l-arabinopyranosyl (1 → 4)]-β-d-(6-O-methyl) glucuronopyranoside (1), 22α-hydroxyoleanolic acid 3-O-α-l-arabinopyranosyl (1 → 4)-β-d-glucuronopyranoside (2), hederagenin 3-O-α-l-arabinopyranosyl (1 → 4)-β-d-glucuronopyranoside (3) and oleanolic acid 28-O-β-d-glucopyranosyl (1 → 2)-β-d-glucuronopyranosyl ester (4) by spectroscopic analyses (HRESIMS, 1D and 2D NMR) and chemical methods.     

Synthesis of triterpenoid triazine derivatives from allobetulone and betulonic acid with biological activities

The synthetic transformation and modification of natural products with the aim to improve the biological properties is an area of current interest. The triterpenoids betulin and betulinic acid are very abundant in nature and now are commercially available. In our study, starting from betulin and betulinic acid, we obtained allobetulone and betulonic acid in a few synthetic steps. The ketone function at the A-ring was used as the starting point for the synthesis of a series of 1,2,4-triazine-fused triterpenoids. The alkylation and Liebeskind–Srogl coupling were used for further substitution of 1,2,4-triazines, and the intramolecular hetero Diels–Alder reaction leads to interesting fused thienopyridine derivatives. All new compounds were tested for their cytostatic activities against murine leukemia L1210, human cervix carcinoma HeLa and human lymphoblast CEM tumor cells. The results show that some triterpenoid triazine betulonic acid derivatives have a promising cytostatic activity in vitro and could be used as potential leads for the development of new type of anti-cancer agents. Several compounds were also endowed with anti-HCMV activity in the low micromolar range.     

Constituents from the pseudofruits of Hovenia dulcis and their chemotaxonomic significance

Sixteen compounds, including six flavonoids (1–6), one lignan (7), three megastigmanes (8–10), three triterpenoids (11–13), and three benzoic acid derivatives (14–16) were isolated and structurally elucidated from the pseudo-fruits of Hovenia dulcis. Their structures were analyzed by NMR spectroscopic and data comparison. Among them, compounds 4, 7–11, 13, 15, and 16 were isolated from the Hovenia genus for the first time. The chemotaxonomic significance of the isolates was also described, which revealed a relationship between H. dulcis and H. acerbar as well as other species belonging to the Rhamnaceae family.     

Antifibrotic constituents of Alnus firma on hepatic stellate cells

Suppression of hepatic stellate cell (HSC) growth and activation have been proposed as therapeutic strategies for the treatment and prevention of liver fibrosis. In the course of screening antifibrotic activity of natural products, the methanolic extract of Alnus firma barks (Betulaceae) showed inhibitory activity of cell proliferation on HSC-T6 cells. A new triterpenoid characterized as lup-20(29) en-2,28-diol-3-yl caffeate (13) was isolated with 12 known diarylheptanoids (1-12) from the barks of A. firma using bioactivity-guided fractionation. Among these compounds, 2 and 13 significantly inhibited the proliferation of HSCs in dose- and time-dependent manners at concentrations from 10 to 100 μM. Taken together, antifibrotic activities of A. firma and its active constituents might suggest the therapeutic potentials against liver fibrosis.