New Isoprenylated 2‐Arylbenzofurans and Pancreatic Lipase Inhibitory Constituents from Artocarpus nitidus

Two new isoprenylated 2‐arylbenzofurans, artonitidin A (=(2′R)‐2′,3′‐dihydro‐2′‐(1‐hydroxy‐1‐methylethyl)‐5′,7‐bis(3‐methylbut‐2‐en‐1‐yl)‐2,4′‐bi‐1‐benzofuran‐6,6′‐diol; 1 ) and artonitidin B (=5‐[6‐hydroxy‐7‐(3‐methylbut‐2‐en‐1‐yl)‐1‐benzofuran‐2‐yl]‐4‐(3‐methylbut‐2‐en‐1‐yl)benzene‐1,3‐diol; 2 ), together with 14 known compounds, 3 – 16 , were isolated from the stems of Artocarpus nitidus Trec. The structures were elucidated by spectroscopic methods. Norartocarpin ( 3 ), cudraflavone C ( 5 ), brosimone I ( 8 ), artotonkin ( 11 ), albanin A ( 13 ), and artopetelin M ( 14 ) showed inhibitory effects on pancreatic lipase with IC₅₀ values ranging from 1.8±0.1 to 63.8±3.6 μM .     

前胡挥发油胆碱酯酶抑制作用及化学成分研究

运用微孔高通量筛选方法研究前胡挥发油胆碱酯酶抑制活性,并用气相色谱-质谱联用技术辅以Kovats指数鉴定挥发油的主要化学成分。结果显示前胡挥发油对乙酰胆碱酯酶和丁酰胆碱酯酶均具有明显的抑制作用,当前胡挥发油浓度为1μL/mL时,其抑制率分别为(63.76±1.99)%和(51.53±1.70)%;其挥发油共鉴定出32种化学成分,主要有α-蒎烯、左旋-β-蒎烯、月桂烯、1-甲基-3-(1-甲基乙基)苯、(R)-1-甲基-4-(1-甲基乙烯基)环己烯、萜品醇、2-羟基-5-甲基苯乙酮等。本研究结果提示前胡有可能对老年痴呆等神经退行性疾病有一定的治疗作用。     

Multi-Targeting Tacrine Conjugates with Cholinesterase and Amyloid-Beta Inhibitory Activities: New Anti-Alzheimer's Agents

Alzheimer's disease (AD) is a severe age dependent and chronic problem with no cure so far. The available treatments are temporary, acting over short period of time. The main pathological hallmark of the disease includes cholinergic dysfunction, oxidative stress, accumulation of Aβ fibrils and tau tangles. In context with the multi-factorial nature of this disease, two different series of molecules were developed to hit the multifactorial disease targets. Mainly, the molecules were designed to inhibit the AChE and aggregation of Aβ, and also oxidative damage. Two novel series of TAC-fenbufen/menbutone conjugated molecules were designed, synthesized and bio-assayed. All compounds showed inhibition capacity towards AChE, Aβ aggregation and moderate to good radical scavenging capacity. Particularly, five TAC-menbutone molecules showed improved AChE and Aβ aggregation inhibition capacity compared to TAC-fenbufen conjugated molecules. Overall, these novel series of molecules may be potential drug lead molecules in the treatment of AD.     

忍冬藤挥发性成分研究

目的：研究忍冬藤中的挥发性成分。方法：利用水蒸气蒸馏法提取忍冬藤（Loruicera japonica Thunb）挥发油,用GC-MS进行测定,结合计算机检索技术对分离的化合物进行结构鉴定,应用色谱峰面积归一化法计算各成分的相对百分含量。结果：鉴定出89个化学成分,其中相对百分含量大于2％的分别确定为芳樟醇（Linalool L）7．98％,丹皮酚（Paeonal）3．73％,苯甲醛（BenzaJ-dehyde）3．46％,壬醛（Nonanal（CAS））3．19％,3-乙烯基吡啶（Pyridine,3-Ethenyl）3．11％,正庚醛（N-Heptanal）2．56％,3-羟基-1-辛烯（1-Octen-3-ol（CAS））2．02％。结论：89个挥发性成分均为首次从该植物中得到。     

茶藨子叶孔菌子实体(忍冬)的化学成分研究(英文)

从茶藨子叶孔菌(忍冬)中分离了8个化合物,通过波谱法和理化性质分别鉴定为豆甾醇(1),二十八酸(2),β-谷甾醇(3),麦角甾醇(4),麦角甾醇过氧化物(5),壬二酸(6),烟酸(7),原儿茶酸(8)。化合物1,3,6均为首次从该属真菌中分到。     

葛根有效成分抑制酪氨酸酶活性的研究

为了探讨葛根对酪氨酸酶的抑制作用,将葛根用75%(v/v)的乙醇水溶液回流提取,用不同极性的溶剂萃取,经硅胶柱层析和重结晶后,分别检测对酪氨酸酶的抑制率.结果表明,在萃取物中,葛根的乙酸乙酯萃取物对酪氨酸酶的抑制率最高,为61.2%;硅胶柱层析分离得到的一部分层析物对酪氨酸酶的抑制率为89.2%,它对酪氨酸酶的抑制作用明显强于其它柱层析组分,该层析物纯化后得到的葛根素对酪氨酸酶的抑制率与浓度呈非线性变化,以熊果苷为阳性对照物.上述研究为进一步开发葛根中的美白成分提供了依据.     

Constituents from the Roots of Actinidia chinensis and Their Cytochrome P450 Enzyme Inhibitory Activities

A newly discovered triterpenoid, (2α,3β)‐2,3,23‐trihydroxyurs‐13(18)‐en‐28‐oic acid ( 1 ), along with twelve known compounds ( 2  –  13 ), were isolated from the roots of Actinidia chinensis Planch (Actinidiaceae). Their chemical structures were determined by 1D‐ and 2D‐NMR spectra and mass spectrometry (MS). The crude extracts and six main constituents ( 8  –  13 ) were tested for cytochrome P450 (CYPs) enzyme inhibitory activity. The results showed that, except for compound 8 , compounds 9  –  13 had different inhibitory effects on the cytochrome P450 (CYPs) enzyme, and compound 9 significantly inhibited the catalytic activities of CYP3A4 to < 10% of its control activities.     

CHRNA7 Polymorphisms and Response to Cholinesterase Inhibitors in Alzheimer's Disease

Background

CHRNA7 encodes the α7 nicotinic acetylcholine receptor subunit, which is important to Alzheimer''s disease (AD) pathogenesis and cholinergic neurotransmission. Previously, CHRNA7 polymorphisms have not been related to cholinesterase inhibitors (ChEI) response.

Methods

Mild to moderate AD patients received ChEIs were recruited from the neurology clinics of three teaching hospitals from 2007 to 2010 (n = 204). Nine haplotype-tagging single nucleotide polymorphisms of CHRNA7 were genotyped. Cognitive responders were those showing improvement in the Mini-Mental State Examination score ≧2 between baseline and 6 months after ChEI treatment.

Results

AD women carrying rs8024987 variants [GG+GC vs. CC: adjusted odds ratio (AOR) = 3.62, 95% confidence interval (CI) = 1.47–8.89] and GG haplotype in block1 (AOR = 3.34, 95% CI = 1.38–8.06) had significantly better response to ChEIs (false discovery rate <0.05). These variant carriers using galantamine were 11 times more likely to be responders than female non-carriers using donepezil or rivastigmine.

Conclusion

For the first time, this study found a significant association between CHRNA7 polymorphisms and better ChEI response. If confirmed by further studies, CHRNA7 polymorphisms may aid in predicting ChEI response and refining treatment choice.     

Saponins from Lonicera bournei

The lupane-triterpene glycosides, bourneioside A and bourneioside B, and two known saponins were isolated from Lonicera bournei Hemsl. The structures of bourneioside A and B were elucidated as 3-O-beta-D-glucopyranosyl-23-hydroxy-lup-20(29)-en-28-oic acid-28-O-beta-D-glucopyranosyl ester and 3-O-beta-D-glucopyranosyl-23-hydroxy-lup-20(29)-en-28-oic acid-28-O-[beta-D-glucopyranosyl-(1 --> 6)-beta-D-glucopyranosyl] ester, respectively, on the basis of spectral data and chemical evidence.     

Biflavonoids from Lonicera japonica

Two biflavonoids, 3'-O-methyl loniflavone [5,5',7,7'-tetrahydroxy 3'-methoxy 4',4'-biflavonyl ether (1)] and loniflavone [5,5',7,7',3'-pentahydroxy 4',4'-biflavonyl ether (2)] along with luteolin (3) and chrysin (4) were isolated from the leaves of Lonicera japonica. The structures were established on the basis of UV/vis, 1D, 2D NMR (HMQC and HMBC) and ESI-QTOF-MS/MS spectroscopic methods and chemical evidences.     

Design,Synthesis, Molecular Docking,and Cholinesterase Inhibitory Potential of Phthalimide‐Dithiocarbamate Hybrids as New Agents for Treatment of Alzheimer's Disease

A novel series of phthalimide‐dithiocarbamate hybrids was synthesized and evaluated for in vitro inhibitory potentials against acetylcholinesterase (AChE) and butyrylcholinesterase (BuChE). The anti‐cholinesterase results indicated that among the synthesized compounds, the compounds 7g and 7h showed the most potent anti‐AChE and anti‐BuChE activities, respectively. Molecular docking and dynamic studies of the compounds 7g and 7h , respectively, in the active site of AChE and BuChE revealed that these compounds as well interacted with studied cholinesterases. These compounds also possessed drug‐like properties and were able to cross the BBB.     

Iridoid glycosides from Lonicera quinquelocularis

A new iridoid glycoside 6'-O-beta-apiofuranosylsweroside was isolated from the ethanolic extract of the roots of Lonicera quinquelocularis along with the known compounds loganin and sweroside.     

New Pterosin Sesquiterpenes and Antitubercular Constituents from Pteris ensiformis

Two new pterosin sesquiterpenes, (2S)‐13‐hydroxypterosin A ( 1 ) and (2S,3S)‐12‐hydroxypterosin Q ( 2 ), were isolated from the whole plants of Pteris ensiformis, together with six known compounds. The structures of 1 and 2 were determined through extensive 1D/2D‐NMR and MS analyses. Compound 2 exhibited antitubercular activity (MIC 6.25 μg/ml) against Mycobacterium tuberculosis H₃₇Rv in vitro.     

蓝锭果(Lonicera caerulea)中的花青素色素的研究

本研究从蓝果忍冬（LoniceraCaerulea）的果实中分离出红色素纯组分,通过层林、水解、光谱、高效液相色谱、核磁共振等方法的研究,鉴定红色素花青素的主要组分是花青定-3-葡萄糖,其他少量成份是花青定-3,5-双葡萄糖、花青定-3-芸香糖、花青定-3-龙胆二糖、芍药定-3-葡萄糖。     

A lignan from Lonicera hypoleuca

A new lignan characterised as (-)-4-hydroxy-2,6-di-(4′-hydroxy-3′-methoxy)phenyl-3,7-dioxabicyclo-(3.3.0)octane along with n-10-nonacosanol, scopoletin, syringic acid, β-sitosterol and its glucoside, has been isolated from the aerial parts of Lonicera hypoleuca. The stereochemistry of the lignan has been established by its spectroscopic analysis and those of its derivatives, and by its conversion to (+)-pinoresinol. β-Sitosterol-β-D-glucoside displayed good spasmolytic activity.     

灰毡毛忍冬化学成分研究进展

综述了忍冬科忍冬属植物灰毡毛忍冬的化学成分及药理作用方面的研究进展.