Cytotoxic monacolin analogs from Monascus purpureus-fermented rice

Two new monacolin analogs, monacolins O (1) and P (2), along with three known analogs, have been isolated from the ethanolic extract of Monascus purpureus-fermented rice. Their structures and absolute configurations were elucidated by spectroscopic methods, especially 2D NMR and CD spectral analyses as well as chemical method. Both 1 and 2 were tested against five tumor cell lines, and compound 1 exhibited selective cytotoxic activity against A2780 and A549 cell lines, with IC₅₀ values of 3.7 and 8.0 μM, respectively.     

血脂康胶囊中的一个新莫纳克林类似物(英文)

血脂康胶囊(红曲醇提取物)是北京北大维信生物科技有限公司自主研究的特制红曲霉发酵制成的调脂中药。通过血脂康调整血脂的临床观察,发现血脂康可降低各种冠心病相关事件的危险性及各种死亡率。为了解释血脂康的许多临床表现,对血脂康进行系统的成分研究。通过成分分析研究,从血脂康中分离纯化了一个新的莫纳克林类化合物,命名为α,β-dehydromonacolin L(1)及两个已知的莫纳克类化合物monacolin L(2)和3-(2,6-dimethyl-1,2,4a,5,6,7,8,8a-octahydronaphthalen-1-yl)propanoic acid(3)。结合核磁共振和质谱分析确定了化合物的化学结构。     

A new decalin derivative from red yeast rice

A new decalin derivative, monascusic acid A (1), together with a new natural product (2), was isolated from the ethanol extract of red yeast rice. Their structures were elucidated by spectroscopic methods.     

Three new tetralol analogs from soil-derived fungus Myrothecium verrucaria with anti-inflammatory activity

Three new tetralol analogs, myrochromanols A-C (1–3), together with 11 known trichothecenes (4–14), were isolated from a soil fungus Myrothecium verrucaria HL-P-1. The structures of the three new compounds were elucidated by extensive spectroscopic analysis including HRESIMS, NMR, and ECD calculation. All of the new compounds were tested for their anti-inflammatory activity and cytotoxicity. Compounds 1 and 3 inhibited lipopolysaccharide (LPS)-induced NO production in BV2 cells with IC₅₀ values of 26.04 and 25.80 μM, respectively.     

红曲霉粗多糖的提取及含量测定

目的:从红曲霉发酵液和菌丝体中提取粗多糖并测定多糖含量。方法:将红曲霉发酵液和菌丝体用水提醇沉法提取粗多糖,用苯酚-硫酸法测定红曲霉多糖的含量。结果:红曲霉粗多糖中多糖含量为62.87%,平均回收率为99.35%,RSD=1.44%。结论:本实验方法可以提取出红曲霉多糖,多糖含量测定准确,苯酚-硫酸法可作为红曲霉多糖含量的测定方法。     

Two new glycosides from Dryopteris fragrans with anti-inflammatory activities

Phytochemical investigation on the aqueous extract from Dryopteris fragrans led to the isolation of one new chromone glycoside, frachromone C (1), and one new coumarin glycoside, dryofracoulin A (2), together with one known undulatoside A (3). Their structures were elucidated by a combination of 1D and 2D NMR, HRMS, and chemical analysis. Compounds 1–3 exhibited inhibition on nitric oxide production in lipopolysaccharide induced RAW 264.7 macrophages with their IC₅₀ values of 45.8, 65.8, and 49.8 μM, respectively.     

Synthesis and biological investigations of new tuftsin analogs with elongated peptide chain

In this paper the synthesis of the following elongated tuftsin analogs: Thr-Lys-Pro-Lys-Thr-Lys-Pro-Lys (I), Thr-Lys-Pro-Lys-Thr-Lys-Pro-Arg (II) and Ala-Lys-Thr-Lys-Pro-Arg-Glu-Gln (III) by the classical method is described. The compound II markedly inhibited the growth of murine sarcoma viruses (MSV).     

Synthesis and in vitro antioxidant activity of some new fused pyridine analogs

A new series of pyrano[3,2-c]pyridines, pyrazolo[4,3-c]pyridines, and pyrido[4,3-d]pyrimidines were synthesized and screened for their in vitro antioxidant activity. Compounds 13, 14, 15, 23, 29, 30, and 31 exhibited the most active oxygen free-radical scavenger activity with percentage inhibitions of 99.4, 99.6, 99.8, 97.3, 99.0, 99.3, and 99.5%; respectively, which is comparable to the curcumin potency. Most of the tested compounds proved to be safe towards peripheral multinuclear neutrophils (PMNs). The detailed synthesis and antioxidant activity data are reported.     

Influence of the peptide chain length of new elongated tuftsin analogs on phagocytosis process

In this paper the synthesis of the following elongated tuftsin analogs: Arg-Thr-Lys-Pro-Arg (1), Pro-Arg-Thr-Lys-Pro-Arg(II), Lys-Pro-Arg-Thr-Lys-Pro-Arg(III) and Thr-Lys-Pro-Arg-Thr-Lys-Pro-Arg(IV) by classical and solid-phase methods are described. The obtained peptides were tested for their biological activity: restoration of the phagocytosis of defected granulocytes from blood of children with acute lymphoblastic leukemia (ALL).     

丁公藤碱Ⅱ类似物的合成及其生物活性

本文设计合成了丁公藤碱Ⅱ的C₂脱氧和C₈电子等排类似物。药理结果表明,丁公藤碱Ⅱ的C₂羟基是保持其缩瞳活性的关键部分之一;目的物2和4各自分别具有拟和抗胆碱活性;电子等排目的物16和17既无拟也无抗胆碱作用。     

New triterpenoid saponins from the aerial parts of Comastomapedunculatum

Three new saikosaponin analogs, comastomasaponins I–K (1–3), were isolated from the aerial portions of Comastomapedunculatum. The structures of these compounds were elucidated on the basis of spectroscopic data analysis, and their nitric oxide production inhibitory activity was evaluated invitro.     

Vasopressin analogs with high and specific antidiuretic activity

A systematic approach to structure-activity studies is described. Its application to the vasopressin field made possible the preparation of vasopressin analogs with very high and very specific antidiuretic activity, analogs with increased pressor specificity, and analogs with high agonistic-antagonistic properties.     

HPLC测定糯米红曲中的洛伐他汀

目的 采用HPLC法测定糯米红曲中洛伐他汀类成分的含量.方法 以酸式洛伐他汀及内酯型洛伐他汀为指标性成分测定糯米红曲中洛伐他汀的含量.结果 糯米红曲中酸式洛伐他汀和内酯型洛伐他汀的含量分别为0.29％ ～0.51％、0.59％ ～0.81％.结论 所用方法操作简单、准确可靠、重复性良好,可用于糯米红曲的质量控制.     

Effect of somatostatin analogs on gastric acid secretion in dogs and rats

The effects of several superactive analogs of somatostatin on gastric acid response to various exogenous and endogenous stimulants were investigated in conscious dogs and rats with gastric fistulae (GF). The inhibition was compared to that induced by somatostatin-14 (S-S-14) at two dose levels. Several octapeptide analogs of somatostatin including (RC-160) and (RC-121), which were superactive in tests on suppression of GH levels, were 4-5 times more potent than S-S-14 in inhibiting desglugastrin-stimulated gastric acid secretion in GF dogs. The analog RC-160 also reduced the rise in serum gastrin levels and gastric acid secretion induced by sham feeding (SF) in dogs with gastric and esophageal fistulae (EF), but did not decrease food consumption. Gastric acid secretion induced by histamine (80μg/kg/h) in dogs was not affected by 1-5μg/kg/h of analog RC-121 or by 5μg/kg/h of S-S-14. Analogs RC-160, RC-121, and RC-98-I and others also powerfully inhibited desglugastrin-induced gastric acid secretion in GF rats. Hexapeptide cyclo(-Pro-Phe-D-Trp-Lys-Thr-Phe) was only about half as potent as S-S-14 in dogs but its activity was higher in rats. The results indicate that octapeptide analogs which are superactive in GH-inhibition tests are also more potent than S-S-14 in suppressing gastric acid secretion. These findings may be of clinical value.     

The synthesis of analogs of shuangkangsu,a novel natural cycloperoxide glucoside from Lonicera japonica Thunb

Four novel optically pure cycloperoxide glucosides 9a, 9b, 10a, and 10b, analogs of shuangkangsu – a natural product with unusual skeleton and antivirus activity from the buds of Lonicera japonica Thunb, were firstly synthesized by employing peroxidation and glucosidation reactions from phthalaldehyde or 4,5-dichloro phthalaldehyde and glucose.     

Effects of anabaseine-related analogs on rat brain nicotinic receptor binding and on avoidance behaviors

Several novel anabaseine-derived compounds were investigated with respect to their ability to displace high affinity [³H]cytisine binding in rat brain membranes, as well as their ability to improve passive and active avoidance behaviors in nucleus basalis-lesioned rats. The relative potencies for displacement of 1 nM [³H]cytisine binding IC50 in parentheses: anabaseine (70 nM) > DMAB (140 nM) = DMXB (150 nM) > anabasine (270 nM) > DMAC (420 nM). Passive avoidance behavior in bilaterally nucleus basalis-lesioned rats was improved by each of these drugs to an extent comparable to that observed with (–)-nicotine. The relative potencies of these compounds for improving this behavior exhibited a pattern very similar to their affinities for displacing [³H]cytisine binding (nicotine > anabaseine > DMXB > DMAB = DMAC > anabasine). Acquisition of active avoidance behavior was slower in unilaterally and bilaterally nucleus basalis-lesioned rats than unlesioned controls; (?)-nicotine improved acquisition behavior only in the former group. At doses that improved passive avoidance behavior, DMXB also improved acquisition of active avoidance behavior in unilaterally lesioned rats, while DMAB and DMAC did not. (?)Nicotine and DMXB had no effect on escape behavior in the active avoidance task at doses that improved retention of avoidance behavior itself. These results suggest that anabaseine and several of its analogs bind to brain α4β2 nicotinic receptors and mimic non-spatial, memory-related behaviors in a nicotine-like manner. © 1994 Wiley-Liss, Inc.     

Four new compounds from the roots of Uvaria macrophylla

Four new compounds, uvamalols A-C (1-3) and uvarimacrophin A (4), have been isolated from the roots of Uvaria macrophylla. Their structures have been elucidated by spectroscopic methods. The relative configurations of uvamalols A-C have been established by NOE experiments, and the relative stereochemistry of uvarimacrophin A inferred from the diagnostic NMR data by comparison with known model compounds.     

Four new compounds from the roots of Uvaria macrophylla

Four new compounds, uvamalols A–C (1–3) and uvarimacrophin A (4), have been isolated from the roots of Uvaria macrophylla. Their structures have been elucidated by spectroscopic methods. The relative configurations of uvamalols A–C have been established by NOE experiments, and the relative stereochemistry of uvarimacrophin A inferred from the diagnostic NMR data by comparison with known model compounds.     

红曲霉降胆固醇有效成分的研究

红曲霉以其能产生大量天然红色素的特性而著称于世，此外还能产生多种有效的生理活性物质。日本学者对红曲降血脂，降血压等功能的发现，掀起了利用红曲开发保健食品的热潮。本文主要对红曲霉生产胆固醇合成途径中的限速酶抑制剂-MonacolinK类物质的研究、特性、药用价值和生产概况和进展等方面进行综述。