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Preparation and Evaluation of Freeze-dried Solid Lipid Nanoparticles with Various Cryoprotectants
Li, Ri Hua,Seo, Seung-Yong,Eun, Jae-Soon,Lee, Mi-Kyung The Korean Society of Pharmaceutical Sciences and 2010 Journal of Pharmaceutical Investigation Vol.40 No.1
Solid lipid nanoparticles (SLNs) were freeze-dried to obtain a stable solid dosage form with the aid of various cryoprotectants such as trehalose, sucrose, glucose, fructose, and glycerol. Tricaprin(TC) and trilaurin(TL) were used as lipid matrices for SLNs and stabilizers were egg phosphatidylcholine and pegylated phospholipid. All cryoprotectants tested did not cause changes in mean particle size of SLNs when mixed with SLNs before freeze-drying. However, the mean particle sizes of reconstituted SLNs after freeze-drying were significantly different from those of the un-lyophilized original SLN dispersions depending on the types and concentration of cryoprotectants. Although the freeze-dried SLNs without any cryoprotectants were easily reconstituted by hand-shaking, the mean particle size drastically increased (> $8\;{\mu}m$ for TC SLNs and around $1\;{\mu}m$ for TL SLNs) compared to that of un-lyophilized original dispersion (97 nm for TC SLNs and 164 nm for TL SLNs). Trehalose and sucrose were the most effective additives to protect the SLNs during lyophilization. The reconstituted SLNs were physically stable for 24 hours when lyophilized with 12.5% trehalose, sucrose, glucose, fructose or glycerol.
Zhen-Hua Chen,Liang-Peng Sun,Wei Zhang,Qiang Shen,Li-Xin Gao,Jia Li,Hu-Ri Piao 대한화학회 2012 Bulletin of the Korean Chemical Society Vol.33 No.5
Protein tyrosine phosphatase 1B (PTP1B) is a key factor in negative regulation of the insulin pathway, and is a promising target for the treatment of type-II diabetes, obesity and cancer. Herein, compound (4) was first observed to have moderate inhibitory activity against PTP1B with an IC50 value of 13.72 ± 1.53 μM. To obtain more potent PTP1B inhibitors, we synthesized a series of chalcone derivatives using compound (4) as the lead compound. Compound 4l (IC50 = 3.12 ± 0.18 μM) was 4.4-fold more potent than the lead compound 4 (IC50 = 13.72 ± 1.53 μM), and more potent than the positive control, ursolic acid (IC50 = 3.40 ± 0.21 μM). These results may help to provide suitable drug-like lead compounds for the design of inhibitors of PTP1B as well as other PTPs.
Chen, Zhen-Hua,Sun, Liang-Peng,Zhang, Wei,Shen, Qiang,Gao, Li-Xin,Li, Jia,Piao, Hu-Ri Korean Chemical Society 2012 Bulletin of the Korean Chemical Society Vol.33 No.5
Protein tyrosine phosphatase 1B (PTP1B) is a key factor in negative regulation of the insulin pathway, and is a promising target for the treatment of type-II diabetes, obesity and cancer. Herein, compound ($\mathbf{4}$) was first observed to have moderate inhibitory activity against PTP1B with an $IC_{50}$ value of $13.72{\pm}1.53{\mu}M$. To obtain more potent PTP1B inhibitors, we synthesized a series of chalcone derivatives using compound ($\mathbf{4}$) as the lead compound. Compound $\mathbf{4l}$ ($IC_{50}=3.12{\pm}0.18{\mu}M$) was 4.4-fold more potent than the lead compound $\mathbf{4}$ ($IC_{50}=13.72{\pm}1.53{\mu}M$), and more potent than the positive control, ursolic acid ($IC_{50}=3.40{\pm}0.21{\mu}M$). These results may help to provide suitable drug-like lead compounds for the design of inhibitors of PTP1B as well as other PTPs.
Inhibition of Poly(I:C)-Induced Inflammation by Salvianolic Acid A in Skin Keratinocytes
( Qing-ling Zhang ),( Ri-hua Jiang ),( Xue Mei Li ),( Jung-woo Ko ),( Chang Deok Kim ),( Ming Ji Zhu ),( Jeung-hoon Lee ) 대한피부과학회 2019 Annals of Dermatology Vol.31 No.3
Background: Skin keratinocytes participate actively in inducing immune responses when external pathogens are introduced, thereby contributing to elimination of pathogens. However, in condition where the excessive inflammation is occurred, chronic skin disease such as psoriasis can be provoked. Objective: We tried to screen the putative therapeutics for inflammatory skin disease, and found that salvianolic acid A (SAA) has an inhibitory effect on keratinocyte inflammatory reaction. The aim of this study is to demonstrate the effects of SAA in poly(I:C)-induced inflammatory reaction in skin keratinocytes. Methods: We pre-treated keratinocytes with SAA then stimulated with poly(I:C). Inflammatory reaction of keratinocytes was verified using real-time polymerase chain reaction, enzyme-linked immunosorbent assay and Western blot. Results: When skin keratinocytes were pre-treated with SAA, it significantly inhibited poly (I:C)-induced expression of inflammatory cytokines including interleukin (IL)-1β, IL-6, IL-8, tumor necrosis factor-α, and CCL20. SAA inhibited poly(I:C)-induced activation of nuclear factor-κB signaling. And SAA also inhibited inflammasome activation, evidenced by decrease of IL-1β secretion. Finally, SAA markedly inhibited poly(I:C)-induced NLRP3 expression. Conclusion: These results demonstrate that SAA has an inhibitory effect on poly(I:C)-induced inflammatory reaction of keratinocytes, suggesting that SAA can be developed for the treatment of inflammatory skin diseases such as psoriasis. (Ann Dermatol 31(3) 279∼285, 2019)
CUBIC B-SPLINE FINITE ELEMENT METHOD FOR THE ROSENAU-BURGERS EQUATION
Xu, Ge-Xing,Li, Chun-Hua,Piao, Guang-Ri The Youngnam Mathematical Society 2017 East Asian mathematical journal Vol.33 No.1
Numerical solutions of the Rosenau-Burgers equation based on the cubic B-spline finite element method are introduced. The backward Euler method is used for discretization in time, and the obtained nonlinear algebraic system is changed to a linear system by the Newton's method. We show that those methods are unconditionally stable. Two test problems are studied to demonstrate the accuracy of the proposed method. The computational results indicate that numerical solutions are in good agreement with exact solutions.
CUBIC B-SPLINE FINITE ELEMENT METHOD FOR THE ROSENAU-BURGERS EQUATION
Ge-Xing Xu,Chun-Hua Li,GUANG-RI PIAO 영남수학회 2017 East Asian mathematical journal Vol.33 No.1
Numerical solutions of the Rosenau-Burgers equation based on the cubic B-spline finite element method are introduced. The back- ward Euler method is used for discretization in time, and the obtained nonlinear algebraic system is changed to a linear system by the Newton’s method. We show that those methods are unconditionally stable. Two test problems are studied to demonstrate the accuracy of the proposed method. The computational results indicate that numerical solutions are in good agreement with exact solutions.
Nan, Ji-Xing,Jin, Xue-Jun,Lian, Li-Hua,Cai, Xing Fu,Jiang, Ying-Zi,Jin, Hong Ri,Lee, Jung Joon Pharmaceutical Society of Japan 2008 Biological & pharmaceutical bulletin Vol.31 No.4
<P>The hepatoprotective effects of a diterpenoid acanthoic acid isolated from <I>Acanthopanax koreanum</I> N<SMALL>AKAI </SMALL>were evaluated in a <SMALL>D</SMALL>-galactosamine/lipopolysaccharide-induced fulminant hepatic failure mouse model. Mice were pretreated orally with acanthoic acid 12 and 1 h before intraperitoneal injection of <SMALL>D</SMALL>-galactosamine and lipopolysaccharide. Pretreatment with the compound markedly reduced lethal liver injury in experimental animals. The effects were likely associated with a significant decrease in serum tumor necrosis factor (TNF)-α levels, which are correlated not only with those of alanine aminotransferase and aspartate aminotransferase but also with the reduced number of apoptotic hepatocytes in the liver as confirmed using the terminal deoxynucleotidyl transferase-mediated dUTP nick end-labeling method and DNA fragmentation assay. These results suggest that acanthoic acid protects against <SMALL>D</SMALL>-galactosamine/lipopolysaccharide-induced fulminant liver failure at least in part by a mechanism associated with the down-regulation of TNF-α secretion.</P>