丝穗金粟兰根中的一个新倍半萜

目的：研究丝穗金粟兰根的化学成分。方法：采用硅胶、MCI和RP-18等多种层析柱分离手段,运用NMR和MS等波谱技术鉴定化合物的结构。结果：从丝穗金粟兰根中分离并鉴定了5个倍半萜化合物：chloranthatone（1）,atractylenolactam（2）,chloranthalactone C（3）,atractylenolid Ⅲ（4）和shizuka-acoradienol（5）。结论：化合物1为新的吉马烷型倍半萜,化合物2为首次从该属植物中分离得到。     

Studies on the chemical constituents of Valeriana fauriei Briq

Nine compounds were isolated from the roots of Valeriana fauriei Briq, of which one is a new germacrane-type sesquiterpenoid named as valerianin E and its structure was elucidated as bicyclo[8, 1, 0] 5β-hydroxyl-7β-acetoxyl-5α,11, 11′-trimethyl-E-1(10)–ene-4α, 15-olide (1). In addition, two were first reported from this genus and the others were isolated for the first time from the title plant.     

刺南蛇藤倍半萜的研究

从刺南蛇藤(Celastrus flagelaris Rupr.)种子油中分离到八个β-二氢沉香呋喃倍半萜,经红外、紫外、质谱及核磁共振谱确定它们的结构是1α-乙酰氧基-2α,9β-二肉桂酰氧基-β-二氢沉香呋喃(1),1α,6β,13-三乙酰氧基-9β-苯甲酰氧基-β-二氢沉香呋喃-(2),triptogelinG-1(3),1α,6β-二乙酰氧基-9β-苯甲酰氧基-β-二氢沉香呋喃(4),triptogelinF-2(5),1α,2α-二乙酰氧基-9β-肉桂酰氧基-β-二氢沉香呋喃(6),celaforlinB-3(7),1α,6β-二乙酰氧基-8α-肉桂酰氧基-9α-苯酰氧基-β-二氢沉香呋喃(8)。其中1是新化合物,命名为celastrine B。     

用分子轨道法对倍半萜类抗癌剂构效关系的研究

本文列举35种倍半萜类抗癌剂的结构和活性,从中归纳出有强抗癌活性的必要条件是分子中必须具有含共轭π键的活性基团。采用CNDO分子轨道法模拟地计算了这些活性基团的E_LUMO,发现其E_LUMO愈低,其母体的抗癌活性就愈高,并且这些E_LUMO与RNA、DNA分子中碱基的E_LUMO的差值较小。作者据此提出了倍半萜类抗癌剂的两个亲电活性基团分别与RNA或DNA的双股核苷酸链上的碱基发生电荷转移络合的抗癌机理。     

倍半萜类2—甲基—6—苯基—2—庚烯—4—酮及其衍生物的合成

本文叙述了三个倍半萜类衍生物—2-甲基-6-苯基-2-庚烯-4-酮(Ⅱ),2-甲基-6-苯基-4-乙烯基-2-庚烯-4-醇(Ⅳ)及2-甲基-6-苯基-4-乙烯基-2,4-庚=烯(Ⅴ)的合成。初步药理筛选结果表明,(Ⅲ)有一定的抗生育活性。化合物(Ⅲ)、(Ⅳ)、(Ⅴ)均未见文献报道,测定了它们的结构并得到了证实。     

Terpenoids and bisbibenzyls from Chinese liverworts Conocephalum conicum and Dumortiera hirsuta

Four new monoterpene esters, 2α,5β-dihydroxybornane-2-cinnamate (1), 2α,5β-dihydroxybornane-5-acetyl-2-cinnamate (2), 2α,5β-dihydroxybornane-2-p-hydroxycinnamate (3) and 2α,5β-dihydroxy-bornane-2-cis-p-hydroxycinnamate (4), together with a known compound 3,4-dimethoxystyrene (5) were isolated from Chinese liverwort Conocephalum conicum and six known compounds, 5,7-dihydroxycalamenene (6), 7-hydroxycalamenene (7), lunularin (8), riccardin C (9), marchantin C (10) and riccardin D (11) were isolated from Dumortiera hirsuta. Their structures were elucidated by extensive spectral analysis and chemical correlations. Compounds 1 and 8 showed moderate cytotoxicity against human HepG2 cells with IC₅₀ 4.5 μg/ml and 7.4 μg/ml, respectively, while compound 8 also showed antimicrobacterial activity against Pseudomonas aeruginosa with minimum inhibitory concentration at 64 μg/ml.     

Water-soluble constituents from aerial roots of Ficus microcarpa

Three new water-soluble constituents [ficuscarpanoside B (1), (7E,9Z)-dihydrophaseic acid 3-O-β-d-glucopyranoside (4) and ficuscarpanic acid (6)] and the natural product 2,2′-dihydroxyl ether (7) have been isolated, together with three known compounds [(7S,8R)-syringoylglycerol (2), (7S,8R)-syringoylglycerol-7-O-β-d-glucopyranoside (3) and icariside D₂ (5)] from the aerial roots of Ficus microcarpa. Identification of their structures was achieved by 1D and 2D NMR experiments, including ¹H–¹H COSY, NOESY, HMQC and HMBC methods and FAB mass spectral data.     

A novel sesquiterpene acid and an alkaloid from leaves of the Eastern Nigeria mistletoe,Loranthus micranthus with potent immunostimulatory activity on C57BL6 mice splenocytes and CD69 molecule

Context: The Eastern Nigeria mistletoe, Loranthus micranthus Linn. (Loranthaceae), is used in the treatment of several diseases including immune-modifying diseases and thus there is a need to identify the immunoactive constituents.

Objective: This research isolated and characterized the immunoactive constituents in the Eastern Nigeria mistletoe.

Materials and methods: Bioassay-guided fractionation was employed in the isolation and purification of the constituents. The characterized compounds were screened for immunostimulatory activities on isolated C57BL/6 mice splenocytes and early activation marker, CD69 at concentrations of 10, 25, and 100 µg/mL using flow cytometry techniques and compared to lipopolysaccharide (LPS; 10 µg/mL) and concanavalin A (ConA; 2 µg/mL) as standards.

Results: Two compounds, a novel sesquiterpene, 2, 3-dimethoxy-benzo [a, b] cyclopentenyl-3′,3′,5′-trimethyl pyran-4-carboxylic acid (1), and a known alkaloid, lupinine (2) were isolated and characterized. The compounds (25 µg/mL) showed statistically significantly (p?<?0.05) stimulatory activity on the splenocytes with values of 56.34?±?0.26% and 69.84?±?0.19%, respectively, compared to 7.58?±?0.42% recorded for the unstimulated control. Similarly, the CD69 expression assay showed immunostimulation with statistically significant values (p?<?0.05) of 2.31?±?0.07% and 2.71?±?0.03%, respectively, compared to 1.69?±?0.05% recorded for the nonstimulated control.

Discussion: These data suggest that the isolated compounds possess immunomodifying abilities. In addition, the activation of the CD69 molecule is possibly one of its mechanisms of action.

Conclusion: These compounds may be responsible in part, for the immunostimulatory activities already established for the Eastern Nigeria mistletoes.     

蜜环菌菌丝体化学成分的研究——Ⅵ.蜜环菌癸素(armillaripin)的分离与结构

从人工发酵培养的蜜环菌[Armillaria mellea(Vahl.ex Fr.)Quel.属白蘑科(Tricholometaceae)真菌]菌丝体的石油醚提取物中,经硅胶层析分离得到一新的倍半萜醇芳香酸酯类化合物,命名为蜜环菌癸素(armillaripin)。根据光谱(UV,IR,~1HNMR,~(13)CNMR和MS)分析推测其化学结构,并进一步用X-线衍射晶体解析法确证其结构和其相对构型。     

O-methyl nakafuran-8 lactone, a new sesquiterpenoid from a hainan marine sponge Dysidea sp

A new sesquiterpenoid, O-methyl nakafuran-8 lactone (1) has been isolated from a Hainan sponge Dysidea sp. and the structure of the new compound proposed by spectral data, was confirmed by X-ray diffraction analysis. The complete ¹H- and ¹³C-NMR assignments were made on the basis of detailed 2D NMR spectral analysis.

Compound 1 showed strong inhibitory bioactivity against PTP1B with IC₅₀ value of 1.58 μM.