Hui-Zi Jin

Sesquiterpene lactones from Inula falconeri, a plant endemic to the Himalayas, as potential anti-inflammatory agents

A phytochemical investigation of Inula falconeri, a plant endemic to the Himalayas, afforded 10 new sesquiterpenoids and 26 known sesquiterpene lactones, including those bearing guaiane, pseudoguaiane, xanthane, eudesmane, germacrane, rare secocaryophyllane, chromolaevane, and carabrane frameworks. The structures were elucidated via spectroscopic analysis and compared with data from literature. All the isolates were assessed for their inhibitory effects against LPS-induced nitric oxide production in RAW264.7 macrophages. Compounds 4, 11, 24, and 31 showed stronger inhibitory activities than the positive control with IC(50) values of 0.13, 0.07, 0.11, and 0.11 μM, respectively. These studies also led to a better understanding of the structure-activity relationships for the sesquiterpene lactone family of compounds.

Metabonomic characterization of aging and investigation on the anti-aging effects of total flavones of Epimedium

A liquid chromatography coupled with mass spectrometry (LC/MS) based metabonomics approach was applied to characterize the aging of rats, and the anti-aging effect of total flavones of Epimedium (TFE), a traditional Chinese medicine, has also been investigated. Serum samples collected from 4, 10, 18 and 24 month-old rats and TFE-administered rats have been profiled by LC/MS. Thirty age-related endogenous metabolites were discovered by partial least squares (PLS) and Hotellings T(2) control chart, among which 25 metabolites were structurally identified by MS(n) analysis and ten of them were further confirmed via authentic chemicals. All important age-related metabolites, such as unsaturated fatty acids, saturated fatty acids, nucleotides, carnosine, ergothioneine and amino acids, displayed age-related changes, and most of them were reset to a younger level after TFE administration. This study indicated that aging could be characterized by changes of lipid metabolisms and accumulation of free radicals. The anti-aging effects of TFE might due to the intervention on lipid metabolism and its property of anti-oxidation.

Construction of 2-substituted-3-functionalized benzofurans via intramolecular Heck coupling: application to enantioselective total synthesis of daphnodorin B.

A novel approach was developed for the synthesis of 2-substituted-3-functionalized benzofurans, using an intramolecular Heck reaction which was further applied in the first enantioselective total synthesis of Daphnodorin B.

Inula sesquiterpenoids: structural diversity, cytotoxicity and anti-tumor activity

Introduction: The plants of the genus Inula (Asteraceae) are widely distributed throughout Europe, Africa and Asia, and many of these plants have long been used in folk medicine. This genus is a rich source of sesquiterpenoids, which exhibit a wide range of biological activities. Recently, a series of bioactive sesquiterpenoid dimers, with unusual carbon skeletons, have been reported and these have gathered considerable interest. Areas covered: This article systematically reviews sesquiterpenoids isolated from the genus Inula that have appeared in literature up to August 2013, critically highlighting their anti-tumoral activities and relevant mechanistic insights. The authors also discuss the initial structure–activity relationships for the cytotoxic and anti-tumoral activities of the Inula sesquiterpenoids. Finally, the authors discuss the challenges and potential applications of these sesquiterpenoids in the future. Expert opinion: Cytotoxic and anti-tumor activities of Inula sesquiterpenoids have been extensively studied since the 1970s. One promising compound, Japonicone A, a dimeric sesquiterpene lactone from traditional herb Inula japonica, has displayed potent in vitro and in vivo anti-tumor activity against Burkitts lymphoma. Additionally, acetylbritannilactone is thought to be capable of suppressing the abnormal vascular smooth muscle cell proliferation, with the induction of apoptosis in vivo and in vitro. In this regard, it may be worthwhile further investigating acetylbritannilactone in patients with vascular restenosis. Furthermore, given the anti-inflammatory property of britanin, clinical studies on chronic bronchitis and asthma, using the ethanol extract of I. japonica, are currently underway in South Korea. However, despite demonstrating good therapeutic effects, additional pharmacological and toxicological studies are still needed.

Sesquiterpenoids from Inula lineariifolia Inhibit Nitric Oxide Production

Fourteen sesquiterpenoids including six new analogues (1-6) were isolated from the aerial parts of Inula lineariifolia.. The structures of the new sesquiterpenoids were determined by spectroscopic data analysis, and the structures of 1 and 6 were confirmed by single-crystal X-ray diffraction data and the modified Mosher method. All 14 compounds were examined for the inhibition of LPS-induced nitric oxide production in RAW264.7 macrophages. Compounds 6, 13, and 14 were found to inhibit nitric oxide production potently, with IC(50) values of 0.11, 0.25, and 0.10 microM, respectively.

Ainsliatrimers A and B, the First Two Guaianolide Trimers from Ainsliaea fulvioides

Ainsliatrimers A (1) and B (2), the first two guaianolide-type sesquiterpene lactone trimers, together with one new structurally related sesquiterpene dimer ainsliadimer B (3), were isolated from the aerial part of Ainsliaea fulvioides. Their structures were elucidated by spectroscopic techniques, including X-ray crystal diffraction. Both 1 and 2 showed potent cytotoxicites against LOVO and CEM cell lines.

Pseudoguaianolides and guaianolides from Inula hupehensis as potential anti-inflammatory agents.

Eight new pseudoguaianolides (1-8), two new guaianolides (9 and 10), and 14 known sesquiterpenes were isolated from the aerial parts of Inula hupehensis. The structures were elucidated using spectroscopic methods and circular dichroism analysis. All compounds were tested for inhibitory activities against LPS-induced nitric oxide production in RAW264.7 macrophages. Compounds 13 and 22 were found to inhibit nitric oxide production potently, with IC50 values of 0.9 and 0.6 μM, respectively. Preliminary structure-activity relationships for these compounds are proposed.

Chemical Constituents of Toona ciliata var. pubescens

Aim To study the chemical constituents of the leaves and stems of Toona ciliata var. pubescens.

Analysis of the bioactive constituents of ChanSu in rat plasma by high performance liquid chromatography with mass spectrometric detection

A plasma pharmacochemistry analysis of the bioactive constituents in rat plasma after oral administration of ChanSu was performed. High performance liquid chromatography coupled with the electrospray ionization mass spectrometry techniques of HPLC/ESI-IT-MS/MS and RRLC/ESI-Q-TOF-MS were used for the chemical profiling of samples of dosed plasma, control plasma and ChanSu extract. Comparative analysis of the resulting chemical profiles revealed 20 prototype compounds and 4 metabolites derived from ChanSu as potential bioactive components. By MS/MS analysis and accurate molecular weight assessments, the majority of these bioactive components (19 prototype compounds and 2 metabolites) were structurally identified. Moreover, seven were confirmed by comparing their retention behaviors using MS and MS/MS analysis. This study proposes a series of potential bioactive components of ChanSu, which we hope will lead to new drug discovery based on ChanSu and other traditional Chinese medicines.

A systematical study of neutron-rich Zr isotopes by the projected shell model

We present results from three-dimensional ideal magnetohydrodynamic simulations of unmagnetized dense plasma jet injection into a uniform hot strongly magnetized plasma, with the aim of providing insight into core fueling of a tokamak with parameters relevant for ITER and NSTX (National Spherical Torus Experiment). Unmagnetized dense plasma jet injection is similar to compact toroid injection but with much higher plasma density and total mass, and consequently lower required injection velocity. Mass deposition of the jet into the background appears to be facilitated via magnetic reconnection along the jet’s trailing edge. The penetration depth of the plasma jet into the background plasma is mostly dependent on the jet’s initial kinetic energy, and a key requirement for spatially localized mass deposition is for the jet’s slowing-down time to be less than the time for the perturbed background magnetic flux to relax due to magnetic reconnection. This work suggests that more accurate treatment of reconnection is needed to fully model this problem. Parameters for unmagnetized dense plasma jet injection are identified for localized core deposition as well as edge localized mode (ELM) pacing applications in ITER and NSTX-relevant regimes. PACS numbers: 28.52.Cx,52.30.Cv,52.55.Fa,52.65.Kj,52.35.Py ‡ Present address: Department of Radiation Physics, The University of Texas M. D. Anderson Cancer Center, Houston, TX, USA, 77030 Unmagnetized dense plasma jet injection into a hot strongly magnetized plasma 2