Tuning the physicochemical properties of axitinib by crystallization: Preparation, calculation and Structure-property relationship

Haibin Qu,Zhonghua Li,Guimin Zhang,Zongyi Zhou,Songgu Wu 한국공업화학회 2023 Journal of Industrial and Engineering Chemistry Vol.124 No.-

Crystal engineering is a radical method to modulate the physicochemical properties of the drugs to meetthe needs of the pharmaceutical industry. Examined herein are six axitinib solid-state forms, includinganhydrous forms (Ⅳand XLI), solvates (acetic acid, nitromethane and n-propanol), and cocrystal (nicotinamide). Comprehensive characterization containing morphology, hygroscopicity, solubility, fluorescenceand powder tabletability were performed. Calculations of lattice energy, packing coefficient andenergy framework rationalized the structure–property relationship of these six forms from the packinglandscape. This system illustrates that form IV and cocrystal improve the solubility of axitinib, but thehumidity stability is also decreased. Six crystal forms show polychromatic solid-state luminescence rangingfrom violet to indigo to green. Form IV and cocrystal with slip plane structures exhibited superior tensilestrength and compactibility than isotropic form XLI. Elusive form VI can be obtained by controllingthe humidity levels during desolvation of the solvate. This work not only realizes the regulation of betterphysicochemical properties of axtinnib for industrial manufacturing, but also provides a detailed understandingof the structure–property relationship of drugs in complex polymorphic systems.

Adaptive Fuzzy Finite Time Prescribed Performance Control for Long Stroke Hybrid Robots

Qunpo Liu,Ming Ye,Zhonghua Wu,Xuhui Bu,Naohiko Hanajima 제어·로봇·시스템학회 2023 International Journal of Control, Automation, and Vol.21 No.9

This paper focuses on the problem of finite-time trajectory tracking control of long-stroke hybrid robots with uncertain system parameters and external disturbances. A system filtering prescribed performance backstepping control based on adaptive fuzzy compensation is proposed. For the unknown terms corresponding to the parameter uncertainties and unknown disturbances existing in the system, a set of auxiliary filter variables is introduced in the adaptive fuzzy approximator and an estimation error function is constructed. An adaptive law based on the estimated error function is proposed to adjust the adaptive weight parameters of the fuzzy system. An adaptive fuzzy approximation algorithm based on the estimation error is finally constructed to compensate for the performance loss caused by the unknown term. For the system state convergence speed problem, a performance function that can transform the system tracking error into an unconstrained error is presented, and the unconstrained error is used as the backstepping control variables. To avoid the differential explosion problem, a new set of inverse control variables is defined by combining the filter variables obtained based on the low-pass filter and the joint velocity. Based on the above variables, a system filtering-based prescribed performance backstepping control strategy is proposed. Finally, the semi-global practical finite-time stability of the closed-loop system is proved by the Lyapunov function. Experiments on the MATLAB platform verify the effectiveness of the proposed method.

The length of guide RNA and target DNA heteroduplex effects on CRISPR/Cas9 mediated genome editing efficiency in porcine cells

Jiawei Lv,Shuang Wu,Renyue Wei,Yan Li,Junxue Jin,Yanshuang Mu,Yu Zhang,Qingran Kong,Xiaogang Weng,Zhonghua Liu 대한수의학회 2019 Journal of Veterinary Science Vol.20 No.3

The clustered regularly interspaced short palindrome repeats (CRISPR)/CRISPR-associated protein 9 (Cas9) system is a versatile genome editing tool with high efficiency. A guide sequence of 20 nucleotides (nt) is commonly used in application of CRISPR/Cas9; however, the relationship between the length of the guide sequence and the efficiency of CRISPR/ Cas9 in porcine cells is still not clear. To illustrate this issue, guide RNAs of different lengths targeting the EGFP gene were designed. Specifically, guide RNAs of 17 nt or longer were sufficient to direct the Cas9 protein to cleave target DNA sequences, while 15 nt or shorter guide RNAs had loss-of-function. Full-length guide RNAs complemented with mismatches also showed loss-of-function. When the shortened guide RNA and target DNA heteroduplex (gRNA:DNA heteroduplex) was blocked by mismatch, the CRISPR/Cas9 would be interfered with. These results suggested the length of the gRNA:DNA heteroduplex was a key factor for maintaining high efficiency of the CRISPR/Cas9 system rather than weak bonding between shortened guide RNA and Cas9 in porcine cells.

Quantized Consensus Control for Multi-UAVs based on Prescribed Performance

Zhihui Du,Jingping Shi,Zhonghua Wu 제어·로봇·시스템학회 2022 International Journal of Control, Automation, and Vol.20 No.1

A distributed adaptive control approach based on a prescribed performance is proposed for multiple unmanned aerial vehicles (multi-UAVs) with disturbances and input quantization. The tracking error is converted into the consensus error by relying on the communication topology so that the distributed controller can be implemented. The radial basic function (RBF) neural network with composite learning is used to estimate the unknown nonlinear functions, and adaptive compensation terms are applied to compensate for the errors caused by filters and disturbances. A hysteretic quantizer is introduced to process the control input signal to relax the channel burden, and an estimator is implemented to solve the problem where the quantizer parameters are unknown. An improved Barrier Lyapunov function (BLF) is developed to ensure that the consensus error satisfies the prescribed performance requirements. Stability analysis proves that the tracking error and all signals in the closed-loop systems are bounded. Finally, all follower UAVs can track the virtual leader and maintain the given formation. A numerical simulation is provided to validate the effectiveness of the proposed control approach.

Study on the Embedded SPC System Based on LAN

Jun, Yinjian,Yu, Zhonghua,Wu, Zhaotong 한국품질경영학회 2003 The Asian Journal on Quality Vol.4 No.1

Statistical Process Control (SPC) is recognized as one of the most important tool of quality control (QC), and is one research focus in order to implement SPC quickly and effectively using computer technology and network environments. This paper proposes the principle and topology of embedded SPC based on the Internet/Intranet, emphatically discusses the embedded data sampling block, embedded network interface and SPC strategy. An example of application is given.

Study on the Embedded SPC System Bused on LAN

Yin, Jianjun,Yu, Zhonghua,Wu, Zhaotong The Korean Society for Quality Management 2003 The Asian Journal on Quality Vol.4 No.1

Statistical Process Control (SPC) is recognized as one of the most important tool of quality control (QC), and is one research focus in order to implement SPC quickly and effectively using computer technology and network environments. This paper proposes the principle and topology of embedded SPC based on the Internet/lntranet, emphatically discusses the embedded data sampling block, embedded network interface and SPC strategy. An example of application is given.

Regulation of cuticular wax biosynthesis in plants under abiotic stress

Md Shaheenuzzamn,Shandang Shi,Kamran Sohail,Hongqi Wu,Tianxiang Liu,Peipei An,Zhonghua Wang,Mirza Hasanuzzaman 한국식물생명공학회 2021 Plant biotechnology reports Vol.15 No.1

Cuticular waxes are the covering of the outer layer of the plant, consist of hydrocarbon appears like whitish flm or bloom in plant organs. They play a vital role like a safeguard from diferent stress condition in the plant. Since environmental factors are active regulators of cuticular wax biosynthesis, composition, quantity, and deposition, it is evident that cuticular wax is associated with plant stress responses. The diversity of cuticular wax compositions is a proof of the wealth of genes associated in plant wax production. Moreover, a number of wax genes were distinguished in plant/crops at abiotic stress conditions but, regulation of control of those wax genes has not been studied very well in major crop plants at abiotic conditions. A very few transcriptions factors were identifed to regulate the expression level of wax genes of cuticular wax biosynthesis at abiotic stress condition. However, further study is needed to identify more candidate transcriptional regulation factors to cuticular wax production in diferent crop plants in diverse abiotic environments. Therefore, regulation of cuticular wax production under diverse abiotic stresses and the role of transcription factors into the plant cuticular wax accumulation will be helpful to engineer crop plants and improve transgenic crops for stress tolerance. In this review, we focused on a new perspective on transcriptional factors to regulate functional genes of cuticular wax biosynthesis in plants at abiotic stresses.

Distribution and dynamics of esterase alleles in Culex pipiens complex in China

Shuaiguo Yan,Ping Nan,Feng Cui,Zhonghua Wu,Chuanling Qiao 한국응용곤충학회 2013 Journal of Asia-Pacific Entomology Vol.16 No.1

To investigate insecticide resistance and dynamic changes of carboxylesterase polymorphism in mosquitoes with time in the Culex pipiens complex (Diptera: Culicidae), nine field mosquito populations were collected in China. The resistance levels of fourth-instar larvae to organophosphate (dichlorvos, parathion, and chlorpyrifos),carbamate (fenobucarb and propoxur), and pyrethroid (permethrin, deltamethrin and tetramethrin)insecticides were determined by bioassay. Larvae had more resistance to organophosphate insecticides than to carbamate insecticides. A low but significant resistance was observed for carbamate insecticides. The resistance to pyrethroid insecticides varied from sensitive to high. Starch gel electrophoresis revealed the presence of the overproduced esterases B1, A2B2, A8B8, A9B9, B10 and A11B11. The frequency of each overproduced esterases varied depending on its regional localities. Compared with published surveys, the C. pipiens complex,which exhibited a high polymorphism of applied esterase alleles in China, showed dynamic evolution over time under local specific insecticide selection. The results are discussed in the context of recent alterations to insecticide campaigns, and in the evolution of resistance genes in Chinese C. pipiens populations.

Heat Treatment Influence on the Structural Properties of Supported Ni Nanoclusters

Vasile Rednic,Nicolae Aldea,Petru Marginean,Marius Rada,Adrian Bot,Zhonghua Wu,Zhang Jing,Florica Matei 대한금속·재료학회 2014 METALS AND MATERIALS International Vol.20 No.4

Ni nanoclusters supported on Al2O3 were prepared using a coprecipitation method. A heat treatment at differenttemperatures was applied. The obtained samples were analyzed by X-ray diffraction (XRD), X-rayabsorption spectroscopy and X-ray photoelectron spectroscopy in order to determine their global, local andelectronic structures. The average particle size, the mean squares of the microstrain, the particle size andmicrostrain distribution functions of the supported Ni nanoclusters were determined by the XRD methodusing a generalized Fermi function for the approximation of the X-ray line. The recrystallization inducedduring the heat treatment process was analyzed. The present study indicated strong deformation of thelocal structure of the active metal in all of the samples investigated due to the metal-support interactionand the effects of the small particle size. Electronic structural investigations showed the presence of Ni ina metallic state as well as Ni2+ on the cluster surfaces.

Expression of DNA Damage Response Proteins and Associations with Clinicopathologic Characteristics in Chinese Familial Breast Cancer Patients with BRCA1/2 Mutations

Xinyi Zhu,Tian Tian,Miao Ruan,Jia Rao,Wentao Yang,Xu Cai,Menghong Sun,Guangqi Qin,Zhonghua Zhao,Jiong Wu,Zhimin Shao,Ruohong Shui,Zhen Hu 한국유방암학회 2018 Journal of breast cancer Vol.21 No.3

Purpose: The characteristic expression of DNA damage response proteins in familial breast cancers with BRCA1, BRCA2, or non-BRCA1/2 mutations has not been analyzed in Chinese patients. Our study aimed to assess the differential expression of microcephalin 1 (BRIT1), ATM serine/threonine kinase (ATM), checkpoint kinase 2 (CHEK2), BRCA1, RAD51 recombinase (RAD51), and poly (ADP-ribose) polymerase 1 (PARP-1) and establish the profile of Chinese familial breast cancers with different mutation status. Methods: We constructed five tissue microarrays from 183 familial breast cancer patients (31 with BRCA1 mutations; 14 with BRCA2 mutations, and 138 with non-BRCA1/2 mutations). The DNA response and repair markers used for immunohistochemistry analysis included BRIT1, ATM, CHEK2, BRCA1, RAD51, and PARP-1. The expressions of these proteins were analyzed in BRCA1/2 mutated tumors. The association between pathologic characteristics with BRCA1/2 mutation status was also analyzed. Results: In familial breast cancer patients, BRCA1 mutated tumors were more frequent with high nuclear grade, estrogen receptor/progesterone receptor/human epidermal growth factor receptor 2 negative, low Ki-67, and positive CK5/6. BRCA1 mutated tumors had lower CHEK2 and higher cytoplasmic BRIT1 expression than BRCA2 and non-BRCA1/2 mutation tumors. BRCA2-associated tumors showed higher CHEK2 and cytoplasmic RAD51 expression than those in other groups. Nuclear PARP-1 expression in BRCA1/2-associated tumors was significantly higher than in non-BRCA1/2 mutation tumors. Moreover, we found quite a few of negative PARP-1 expression cases in BRCA1/2 mutated groups. Conclusion: The clinicopathologic findings of BRCA1-associated Chinese familial breast cancers were similar to the results of other studies. Chinese familial breast cancer patients with BRCA1/2 mutations might have distinctive expression of different DNA damage response proteins. The reduced expression of PARP-1 in Chinese BRCA1/2 mutated breast cancer patients could influence the therapeutic outcome of PARP-1 inhibitors.