Polypeptide/Doxorubicin Hydrochloride Polymersomes Prepared Through Organic Solvent‐free Technique as a Smart Drug Delivery Platform

Rapid and efficient side‐chain functionalization of polypeptide with neighboring carboxylgroups is achieved via the combination of ring‐opening polymerization and subsequent thiol‐yne click chemistry. The spontaneous formation of polymersomes with uniform size is found to occur in aqueous medium via electrostatic interaction between the anionic polypeptide and cationic doxorubicin hydrochloride (DOX·HCl). The polymersomes are taken up by A549 cells via endocytosis, with a slightly lower cytotoxicity compared with free DOX ·HCl. Moreover, the drug‐loaded polymersomes exhibit the enhanced therapeutic efficacy, increase apoptosis in tumor tissues, and reduce systemic toxicity in nude mice bearing A549 lung cancer xenograft, in comparison with free DOX ·HCl.     

药物化学中的大分子效应※

药物种类按照分子量来划分可以分为小分子药物(自然提取或化学合成的)和大分子药物(生物制剂). 尽管目前小分子药物仍然是市场的主流, 但其研发增速趋缓, 而大分子药物在药物研发中的地位日渐突显, 并被预期在未来药物市场中占据越来越高的份额. 除了生物制剂大分子药物, 将小分子药物与天然或合成大分子结合制备得到的化学合成大分子药物, 近年来受到药物研究者们越来越多的关注. 由于大分子具有丰富的骨架结构及空间构架, 其所特有的骨架效应、多价效应, 以及通过分子组装而产生的聚集效应和靶向效应等, 能够为药物化学的设计带来更多新的可能. 有鉴于此, 本综述将简略介绍药物化学设计中的大分子效应, 重点讨论合成大分子的骨架效应、多价效应、聚集效应和靶向效应等为药物化学设计所带来的新性能. 通过对药物化学中大分子效应所带来的优势、问题和重要研究进展的探讨, 以期能够推动化学合成大分子药物的发展, 为药物化学设计提供新的思路.     

测度链上p-Laplacian边值问题的三个正对称解

该文研究了p-Laplacian动力边值问题（g（u^△（t）））△＋a（t）f（t，u（t））=0，t∈[0，T]T,u（0）=u（T）=w，u△（0）=-u^△（T）正解的存在性．其中W是非负实数，g（v）=｜v｜p-2v1 P＞1．根据对称技巧和五泛函不动点定理，证明了边值问题至少有三个正的对称解，同时，给出了一个例子验证了我们的结果。     

OSCILLATION OF HIGHER ORDER NEUTRAL DIFFERENTIAL EQUATIONS WITH POSITIVE AND NEGATIVE COEFFICIENTS

ＯＳＣＩＬＬＡＴＩＯＮＯＦＨＩＧＨＥＲＯＲＤＥＲＮＥＵＴＲＡＬＤＩＦＦＥＲＥＮＴＩＡＬＥＱＵＡＴＩＯＮＳＷＩＴＨＰＯＳＩＴＩＶＥＡＮＤＮＥＧＡＴＩＶＥＣＯＥＦＦＩＣＩＥＮＴＳＬｉＷａｎｔｏｎｇ（李万同）（ＺｈａｎｇｙｅＴｅａｃｈｅｒｓ＇Ｃｏｌｌｅｇｅ...     

AN OSCILLATION CRITERION FOR SECOND ORDER SUBLINEAR DIFFERENTIAL EQUATIONS

ＡＮＯＳＣＩＬＬＡＴＩＯＮＣＲＩＴＥＲＩＯＮＦＯＲＳＥＣＯＮＤＯＲＤＥＲＳＵＢＬＩＮＥＡＲＤＩＦＦＥＲＥＮＴＩＡＬＥＱＵＡＴＩＯＮＳ￥ＬｉＷａｎｔｏｎｇ（ＺｈａｎｇｙｅＴｅａｃｈｅｒｓ＇Ｃｏｌｌｅｇｅ，７３４０００）ＱｕａｎＨｏｎｇｓｈｕｎ（Ｌａｎｚ...     

新重丰中子同位素239Pa

用50MeV/u ¹⁸O离子同天然铀靶反应产生了新重丰中子同位素²³⁹Pa.用放射化学法从反应产物中分离Pa活性,通过观测²³⁹Pa及子体²³⁹U衰变所得到的结果显示:首次合成和鉴别了新重丰中子核素²³⁹Pa,并测定出²³⁹Pa的半衰期为106±30min.     

175Er的衰变纲图

用14MeV中子照射天然Yb靶,通过¹⁷⁶Yb(n,2p)¹⁷⁵Er反应产生了新的重丰中子同位素¹⁷⁵Er,借助X-γ,γ-γ符合测量方法,首次鉴别出了¹⁷⁵Er,并测得其半衰期为(1.2±0.3)min.同时还观察到了¹⁷⁵Er衰变所发射的8条新γ射线,建立了¹⁷⁵Er的部分γ衰变纲图,从中指定了¹⁷⁵Tm的一个基态转动带.     

Traveling Waves of a Reaction-Diffusion SIRQ Epidemic Model with Relapse

This paper is concerned with the traveling waves of a reaction-diffusion SIRQ epidemic model with relapse. We find that the existence and nonexistence of traveling waves are determined by the basic reproduction number of the system and the minimal wave speed. This threshold dynamics is proved by Schauder''s fixed-point theorem combining Lyapunov functional with the theory of asymptotic spreading. Moreover, the numerical simulations are provided to illustrate our analytical results and the effect of the relapse is also discussed.     

Methoxypoly(ethylene glycol)‐block‐Poly(L‐glutamic acid)‐Loaded Cisplatin and a Combination With iRGD for the Treatment of Non‐Small‐Cell Lung Cancers

CDDP is loaded into methoxypoly(ethylene glycol)‐block‐poly(L ‐glutamic acid) (mPEG‐b‐PLG), and a combination with iRGD is applied for NSCLC chemotherapy. The CDDP‐loaded micelles show sustained cisplatin release in PBS, dose‐ and time‐dependent inhibition to HeLa and A549 cell proliferation, and no apparent hemolysis activities. In in vivo studies using subcutaneous NSCLC xenograft models (A549), both free CDDP and CDDP‐loaded micelles show an evident anti‐tumor effect. However, the toxicity of CDDP is significantly reduced in the cases of CDDP‐loaded micelles and co‐administration with iRGD, and the survival time is prolonged by over 30%. Therefore, mPEG‐b‐PLG‐loaded cisplatin and the combination with iRGD provides a promising new therapy for NSCLC.

     

Production and identification of new neutron-deficient isotope235Am in region of transuranium

A new transuranium neutron-deficient isotope²³⁵Am was produced by 35 MeV proton to bombard the rare radioactive²³⁸Pu target. The products were transported and collected by the He-jet system. The Am isotopes were separated and purified by radiochemistry method and the y-ray, X-ray and y-X(y) coincidence of the samples was measured. The synthesis of²³⁵Am was definitely identified. Its measured half-life is (15±5) min. Project supported by the National Natural Science Foundation of China and the Chinese Academy of Sciences.