雪山芪的化学成分研究

目的 研究雪山芪He dysaram sikkimense Benth．ex Baker．var．rigidum Hand、-Mass．的化学成分。方法 采用反复硅胶柱层析分离纯化,通过理化常数测定和光谱分析鉴定化合物的结构。结果 从雪山芪干燥根中分离得到9个化合物。根据波谱分析和理化数据,鉴定出其中8个化合物分别为：羽扇豆醇(lupeol,1)、4′-羟基-7-甲氧基异黄酮(isoformononetein,Ⅱ)、4′-羟基-6,7-二甲氧基异黄酮(3-[4-hydroxyphenyl-6,7-dimetoxy-4H-1-benzopyran-4-one],Ⅲ)、熊果酸(ursolic acid,Ⅳ)、山嵛酸-α-单甘油酯(docosanooic acid-2,3-d．hydroxypropyl ester,Ⅴ)、二十四烷酸(lignoceric acid,Ⅵ)、β-谷甾醇(β-sitosterol,Ⅶ)及蔗糖。结论 以上化合物均为首次从该植物中分得。     

Anti-inflammatory pterocarpanoids from the roots of Pongamia pinnata

A phytochemical study on the roots of Pongamia pinnata afforded 11 pterocarpanoids, including three new compounds. The structures of the isolated compounds were determined by 1D and 2D NMR and HRESIMS data. The absolute configurations of the new compounds were assigned via analysis of the specific rotations and electronic circular dichroism (ECD) spectra. The isolates were evaluated for their inhibitory effects on nitric oxide (NO) production in LPS-stimulated BV-2 microglial cells. Six compounds exhibited inhibitory effects against NO production, and compound 5 showed the best activity with an IC₅₀ value at 12.0?μM.     

Fatty acids and other lipid composition of five Trifolium species with antioxidant activity

The contents of fatty acids and other lipids of Trifolium balansae Boiss, Trifolium stellatum Lin., Trifolium nigrescens Viv. subsp. petrisavi (Clem) Holmboe, Trifolium constantinopolitanum Ser., and Trifolium resupinatum L. var. resupinatum L. (Leguminosae) were determined by gas chromatography-mass spectrometry (GC-MS). The whole plant hexane extracts of five Trifolium species contained eight fatty acids consisting of linolenic (31.1%) and palmitic (18.9%) acids as the most abundant unsaturated and saturated fatty acids, respectively. The total unsaturation for the oils of five Trifolium species was 30.6–42.2%. In addition to fatty acids, some alkanes and phytol were also obtained. The antioxidant activity and contents of fatty acids and lipids of five Trifolium species T. balansae, T. stellatum, T. nigrescens subsp. petrisavi, T. constantinopolitanum, and T. resupinatum var. resupinatum are presented for the first time in this study.     

NMR确定鸡血藤中1个新的降倍半萜类化合物布卢门醇A-6-O-反式-对羟基肉桂酸酯

目的:研究鸡血藤水提取物中的化学成分。方法:采用硅胶、高效液相等柱色谱方法进行分离纯化,通过化合物的核磁共振(NMR)数据鉴定其结构。结果:从鸡血藤水提取物中分离出1个降倍半萜类化合物,根据其NMR数据鉴定其化学结构为布卢门醇A-6-O-反式-对羟基肉桂酸酯。结论:布卢门醇A-6-O-反式-对羟基肉桂酸酯为1个新的化合物。     

波叶山蚂蝗化学成分研究

目的 研究来自贵州省安顺市波叶山蚂蝗全草的化学成分.方法 采用硅胶、凝胶色谱法进行化学成分的分离纯化,通过理化性质和波谱分析进行结构鉴定.结果 从波叶山蚂蝗全草75％乙醇提取物中分离鉴定了7个化合物,分别为β-香树脂醇(1),β-谷甾醇(2),胡萝卜苷(3),羽扇20(29)-烯-3-酮(4),(Z,Z,Z)-9,12,15-十八三烯酸甲酯(5),4’,5,7-三羟基异黄酮(6),尿囊素(7).结论 化合物1～7均为首次从波叶山蚂蝗植物中分离得到.     

Potent antimutagenic and their anti-lipid peroxidative effect of kaikasaponin III and tectorigenin from the flower of Pueraria thunbergiana

The MeOH extract of Pueraria thunbergiana (Leguminosae) flowers and its fractions were subjected to Ames test to test the antimutagenicity. EtOAc fraction (1 mg/plate) decreased the number of revertants of Salmonella typhymurium TA100 by 95% against aflatoxin B, (AFB1). Phytochemical isolation of the EtOAc fraction afforded four isoflavonoids (tectorigenin, glycitein, tectoridin and glycitin) and one saponin (kaikasaponin III). Though the three isoflavonoids other than tectoridin showed significant antimutagenicity, the activity of kaikasaponin III was the most potent. Kaikasaponin III (1 mg/plate) decreased the number of revertants of S. typhymurium TA100 by 99% against AFB, but by 75% against N-methyl-N'-nitro-N-nitrosoguanidine (MNNG). Tectorigenin (1 mg/plate) inhibited the AFB1-induced mutagenicity by 90% and MNNG-induced one by 76%. Glycitein and glycitin were less active than tectorigenin and kaikasaponin III. This result suggested that kaikasponin III prevents the metabolic activation of AFB1 and scavenge electrophilic intermediate capable of mutation. The two components with potent activities, tectorigenin and kaikasaonin III, significantly prevented the malondialdehyde formation caused by bromobenzene in the rat.     

A new coumaronochromone from Sophora japonica

A new coumaronochromone derivative, sophorophenolone ( 1 ), along with 13 known compounds, l -maackiain ( 2 ), medicagol ( 3 ), 7- O -methylpseudobaptigenin ( 4 ), pseudobaptigenin ( 5 ), 7,3'-di- O -methylorobol ( 6 ), genistein ( 7 ), prunetin ( 8 ), daidzein ( 9 ), formononetin ( 10 ), Di- O -methyldaidzein ( 11 ), quercetin ( 12 ), kaempferol ( 13 ) and isorhamnetin ( 14 ) were isolated from pericarps of Sophora japonica L. The structure of compound 1 was established by UV, IR, MS, and one-dimensional and two-dimensional NMR spectroscopy, including DEPT, NOESY, 1 H- 1 H COSY, HMQC, and HMBC experiments.     

Kaempferia parviflora, a plant used in traditional medicine to enhance sexual performance contains large amounts of low affinity PDE5 inhibitors

Aim of the study

A number of medicinal plants are used in traditional medicine to treat erectile dysfunction. Since cyclic nucleotide PDEs inhibitors underlie several current treatments for this condition, we sought to show whether these plants might contain substantial amounts of PDE5 inhibitors.

Materials and methods

Forty one plant extracts and eight 7-methoxyflavones from Kaempferia parviflora Wall. ex Baker were screened for PDE5 and PDE6 inhibitory activities using the two-step radioactive assay. The PDE5 and PDE6 were prepared from mice lung and chicken retinas, respectively. All plant extracts were tested at 50 μg/ml whereas the pure compounds were tested at 10 μM.

Results

From forty one plant extracts tested, four showed the PDE5 inhibitory effect. The chemical constituents isolated from rhizomes of Kaempferia parviflora were further investigated on inhibitory activity against PDE5 and PDE6. The results showed that 7-methoxyflavones from this plant showed inhibition toward both enzymes. The most potent PDE5 inhibitor was 5,7-dimethoxyflavone (IC₅₀ = 10.64 ± 2.09 μM, selectivity on PDE5 over PDE6 = 3.71). Structure activity relationship showed that the methoxyl group at C-5 position of 7-methoxyflavones was necessary for PDE5 inhibition.

Conclusions

Kaempferia parviflora rhizome extract and its 7-methoxyflavone constituents had moderate inhibitory activity against PDE5. This finding provides an explanation for enhancing sexual performance in the traditional use of Kaempferia parviflora. Moreover, 5,7-dimethoxyflavones should make a useful lead compound to further develop clinically efficacious PDE5 inhibitors.     

Constituents of the roots ofPueraria lobata inhibit formation of advanced glycation end products (AGEs)

Two isoflavone C-glucosides, puerarin (1) and PG-3 (2), a but-2-enolide, (+/-)-puerol B (3), two isoflavone O-glucosides, daidzin (4) and genistin (5), and three pterocarpans, (-)-medicarpin (6), (-)-glycinol (7) and (-)-tuberosin (8), were isolated from a MeOH extract of the roots of Pueraria lobata, using an in vitro bioassay based on the inhibition of the formation of advanced glycation end products (AGEs) to monitor chromatographic fractionation. The structures of 1-8 were determined by spectroscopic data interpretation, particularly by 1D- and 2D-NMR studies, and by comparison of these data with values in the literature. All of the isolates (1-8) were evaluated for their inhibitory activity on AGEs formation in vitro. Of these, puerarin (1), PG-3 (2), and (+/-)-puerol B (3) exhibited more potent inhibitory activity than the positive control aminoguanidine.     

Two new compounds from the roots of Lysidice rhodostegia

Two new compounds, lysidicin D (1) and lysidicin E (2), were isolated from the roots of Lysidice rhodostegia. Their structures were elucidated by means of spectroscopic methods. Among them compound 1 showed potent anti-oxidant activity on in vitro.