Whole Cell-mediated Biocatalytic Synthesis of Helicid Cinnamylate and Its Biological Evaluation as a Novel Tyrosinase Inhibitor

Rong-ling Yang,Xi Chen,Yu-ye Song,Qian-lin Zhu,Muhammad Bilal,Yu Wang,Zheng Tong,Ting-ting Wu,Zhao-Yu Wang,Hong-zhen Luo,Xiang-jie Zhao,Ting-ting He 한국생물공학회 2022 Biotechnology and Bioprocess Engineering Vol.27 No.3

Tyrosinase inhibitors are clinically effective for treating some dermatological disorders related to melanin hyperpigmentation. Accordingly, the discovery and development of tyrosinase inhibitors have great value in the pharmaceutical and cosmetic industry. Here, a novel tyrosinase inhibitor, 6′-O-cinnamoyl-helicid (helicid cinnamylate) was successfully synthesized by a simple and effective biocatalytic approach with Aspergillus oryzae cells. Investigation of the effects of several key variables on helicid cinnamylate synthesis found that the reaction conversion, reaction rate and regioselectivity reached 99%, 9.40 mM/h and > 99%, respectively, at the optimal conditions with anhydrous acetone as the solvent, whole-cell concentration of 40 mg/mL, and the molar ratio of vinyl cinnamate to helicid of 10 at 45°C. The whole-cells retained 68.87% of its initial activity after reusing for seven batches, indicating a potent application potential in non-aqueous biocatalytic systems. It was worth noting that helicid cinnamylate demonstrated a more potent tyrosinase inhibitory activity with an IC50 value of 3.55 mM than helicid (IC50 = 4.48 mM) and arbutin (IC50 = 5.48 mM), which suggest that helicid cinnamylate could be developed as a more potential tyrosinase inhibitor. In conclusion, this study provides a novel whole-cell catalytic approach for the synthesis of helicid cinnamylate and insight into its application as a tyrosinase inhibitor.

Effects of L-malic acid on alpha-glucosidase: inhibition kinetics and computational molecular dynamics simulations.

Gou, Lin,Zhan, Yi,Lee, Jinhyuk,Li, Xuan,Lü,, Zhi-Rong,Zhou, Hai-Meng,Lu, Hang,Wang, Xi-Yao,Park, Yong-Doo,Yang, Jun-Mo Humana Press 2015 Applied biochemistry and biotechnology Vol.175 No.4

<P>The inhibitory effect of L-malic acid (MA) on alpha-glucosidase (EC 3.2.1.20) was investigated by combination study between inhibition kinetics and computational simulations. The results from the serial kinetics demonstrated that MA could directly inactivate the enzyme activity in a dose-dependent manner and a typical non-competitive type, as well as in a fast inactivate process without detectable time course. The tertiary conformation study with an application of spectrofluorimetry showed that MA modulated the tertiary structural conformation of alpha-glucosidase both on the overall and on regional active site pocket, which monitored by red-shift intrinsic fluorescence peak with decreases intensities, and the significant intensity increasing of 1-anilinonaphthalene-8-sulfonate (ANS)-binding fluorescence, respectively. To have more insight, we also adapted the computational molecular dynamics (MD) simulations. The results showed that MA was located in the entrance of active pocket for the catalytic reaction and blocked the passage of substrate. It confirmed that MA inhibits as a non-competitive type, not direct docking to the glucose binding site. Our study provides important molecular mechanisms to figure out alpha-glucosidase inhibition that might associate to development of type 2 diabetes mellitus drug.</P>

Synthesis and Structural Studies of an Organic Complex and its Association with BSA

Meng, Fa-Yan,Yu, Sheng-Rong,Liang, Li-Xi,Zhong, Xue-Ping,Wang, Li,Zhu, Jin-Mei,Lin, Cui-Wu Korean Chemical Society 2011 Bulletin of the Korean Chemical Society Vol.32 No.7

The self-assembly of one novel organic complex based on chlorogenic acid (HCA) and 2,2'-bipyridine (2,2'-bipy) has been synthesized and characterized. The complex achieved by hydrogen-bonding interactions, adopted a 1:1 stoichiometry in a solid state. The proton transfer occurred from the carboxyl oxygen to the aromatic nitrogen atom to form salts CA${\cdot}$(2,2'-Hbipy), the 2,2'-Hbipy molecule individually occupies the pseudo-tetragonum that is formed with CA. In this paper, the interactions of CA${\cdot}$(2,2'-Hbipy) with bovine serum albumin (BSA) were studied by fluorescence spectrometry. For CA${\cdot}$(2,2'-Hbipy), HCA and 2,2'-bipy, the average quenching constants for BSA were $2.4384{\times}10^4$, $4.653{\times}10^3$, and $3.059{\times}10^3\;L{\cdot}mol^{-1}$, respectively. The mechanism for protein fluorescence quenching is apparently governed by a static quenching process. The Stern-Volmer quenching constants and corresponding thermodynamic parameters ${\Delta}$H, ${\Delta}$G and ${\Delta}$S were calculated. The binding constants and the number of binding sites were also investigated. The conformational changes of BSA were observed from synchronous fluorescence spectra.

Design of Acquisition and Control System of Granary Supervisory Control and Data Acquisition System

Li-hua Wu,Jia-yu Yao,Xi-rong Lin,Hai-yang Zhang 보안공학연구지원센터 2015 International Journal of Multimedia and Ubiquitous Vol.10 No.6

Grain stored in granary is easily spoiled due to accumulated hear or humidity if not monitored and maintained properly. Supervisory control and data acquisition (SCADA) system is commonly used in granary to provide real-time storage information. Major functionalities in the granary SCADA system is usually provided by an acquisition and control system based on single chip computer installed inside or near the granary. Based on theoretical and commissioning data, the design of the acquisition and control system was introduced in this paper. The acquisition and control system is able to acquire real-time data of temperature, humidity and concentration of CO2 inside the granary. It also provides the functionalities of open/shut the granary windows, as well as turning on/off the high-power roller shutter doors and blowers. Users are able to obtain real-time monitored data and control the system accordingly.

Electroacupuncture Promotes Neural Proliferation in Hippocampus of Perimenopausal Depression Rats via Wnt/β-Catenin Signaling Pathway

Qin Jing,Lu Ren,Xue Deng,Nan Zhang,Martin Fu,Ge Wang,Xi-Rong Jiang,Shu-Ru Lin,Cai-Rong Ming 사단법인약침학회 2020 Journal of Acupuncture & Meridian Studies Vol.13 No.3

Background and Objective: Perimenopausal depression is caused by the impaired function of the ovarium before menopause and with a series of symptoms. Electroacupuncture (EA) therapy has been demonstrated to improve clinically depression. However, the mechanism underlying its therapeutic activity remains unknown. This study aimed to investigat the effects of EA treatment on the hippocampal neural proliferation through Wnt signaling pathway. Methods: Chronic unpredictable mild stress (CUMS) combined with bilateral ovariectomy (OVX) were used to establish a rat model of perimenopausal depression. The open field test (OFT) and sucrose preference test (SPT) were used to assess depression-like behaviors in rats. ELISAs were used to measure estrogen (E2), luteinizing hormone (LH) and gonadotropin-releasing hormone (GnRH) levels in the serum. RT-PCR and Western blot assay were utilized for measuring the mRNA expressions and protein expressions of GSK-3β/β-catenin. Results: Four-week EA treatment at three points including “Shenshu” (BL23), “Baihui” (GV20) and “Sanyinjiao” (SP6) simultaneously ameliorated depression-like behaviors in rats with CUMS and OVX, whereas rescued the decreased serum level of E2 and prevented the increased serum levels of GnRH and LH. EA treatment ameliorated CUMS and OVX-induced alterations of glycogen synthase kinase-3b (GSK-3β) and β-catenin mRNA levels, β-catenin and phosphorylated β-catenin (p-β-catenin) protein levels. Conclusions: The results showed that EA treatment promoted hippocampal neural proliferation in perimenopausal depression rats via activating the Wnt/b-catenin signaling pathway, indicating that EA may represent an efficacious therapy for perimenopausal depression.

Synthesis and Structural Studies of an Organic Complex and its Association with BSA

Fa-Yan Meng,Jin-Mei Zhu,Li Wang,Xue-Ping Zhong,Li-Xi Liang,Sheng-Rong Yu,Cui-Wu Lin 대한화학회 2011 Bulletin of the Korean Chemical Society Vol.32 No.7

The self-assembly of one novel organic complex based on chlorogenic acid (HCA) and 2,2'-bipyridine (2,2'-bipy) has been synthesized and characterized. The complex achieved by hydrogen-bonding interactions,adopted a 1:1 stoichiometry in a solid state. The proton transfer occurred from the carboxyl oxygen to the aromatic nitrogen atom to form salts CA·(2,2'-Hbipy), the 2,2'-Hbipy molecule individually occupies the pseudo-tetragonum that is formed with CA. In this paper, the interactions of CA·(2,2'-Hbipy) with bovine serum albumin (BSA) were studied by fluorescence spectrometry. For CA·(2,2'-Hbipy), HCA and 2,2'-bipy,the average quenching constants for BSA were 2.4384 × 10^4, 4.653 × 10^3, and 3.059 × 10^3 L·mol^−1, respectively. The mechanism for protein fluorescence quenching is apparently governed by a static quenching process. The Stern-Volmer quenching constants and corresponding thermodynamic parameters ΔH, ΔG and ΔS were calculated. The binding constants and the number of binding sites were also investigated. The conformational changes of BSA were observed from synchronous fluorescence spectra.

Histological Validation of Cardiovascular Magnetic Resonance T1 Mapping for Assessing the Evolution of Myocardial Injury in Myocardial Infarction: An Experimental Study

Zhang Lu,Yang Zhi-gang,Xu Huayan,Yang Meng-xi,Xu Rong,Chen Lin,Sun Ran,Miao Tianyu,Zhao Jichun,Zhou Xiaoyue,Fu Chuan,Guo Yingkun 대한영상의학회 2020 Korean Journal of Radiology Vol.21 No.12

Objective: To determine whether T1 mapping could monitor the dynamic changes of injury in myocardial infarction (MI) and be histologically validated. Materials and Methods: In 22 pigs, MI was induced by ligating the left anterior descending artery and they underwent serial cardiovascular magnetic resonance examinations with modified Look-Locker inversion T1 mapping and extracellular volume (ECV) computation in acute (within 24 hours, n = 22), subacute (7 days, n = 13), and chronic (3 months, n = 7) phases of MI. Masson’s trichrome staining was performed for histological ECV calculation. Myocardial native T1 and ECV were obtained by region of interest measurement in infarcted, peri-infarct, and remote myocardium. Results: Native T1 and ECV in peri-infarct myocardium differed from remote myocardium in acute (1181 ± 62 ms vs. 1113 ± 64 ms, p = 0.002; 24 ± 4% vs. 19 ± 4%, p = 0.031) and subacute phases (1264 ± 41 ms vs. 1171 ± 56 ms, p < 0.001; 27 ± 4% vs. 22 ± 2%, p = 0.009) but not in chronic phase (1157 ± 57 ms vs. 1120 ± 54 ms, p = 0.934; 23 ± 2% vs. 20 ± 1%, p = 0.109). From acute to chronic MI, infarcted native T1 peaked in subacute phase (1275 ± 63 ms vs. 1637 ± 123 ms vs. 1471 ± 98 ms, p < 0.001), while ECV progressively increased with time (35 ± 7% vs. 46 ± 6% vs. 52 ± 4%, p < 0.001). Native T1 correlated well with histological findings (R2 = 0.65 to 0.89, all p < 0.001) so did ECV (R2 = 0.73 to 0.94, all p < 0.001). Conclusion: T1 mapping allows the quantitative assessment of injury in MI and the noninvasive monitoring of tissue injury evolution, which correlates well with histological findings.