Table of Content

02 September 2019, Volume 28 Issue 8

Previous Issue    Next Issue

Original articles

Discovery of tryptamine derivatives from Bacillus sp. PKU-TA00001

Tongtong Geng, Guiyang Wang, Xueyang Ma, Zhongyi Zhang, Tan Liu, Yuanjie Ge, Jing Jin, Xiaoxu Sun, Yingtao Zhang, Donghui Yang, Ming Ma

2019, 28(8):  527-536.  DOI: 10.5246/jcps.2019.08.050

Asbtract ( 284 )   HTML ( 8)   PDF (1313KB) ( 267 )  

References | Related Articles | Metrics

Tryptamine-derived natural products have been discovered from different sources including animals, plants and bacteria,and they show various biological activities. However, they are not discovered widely compared with the large amounts of tryptaminederivatives generated by chemical synthesis. We here report the discovery of five tryptamine-derived natural products (1–5) and one known polyketide 6 from Bacillus sp. PKU-TA00001. Compounds 1 and 2are new compounds featuring methyl-hexanamide moieties, compound 4is first discovered as a natural product, and 3 and 4’s NMR data are first provided. All compounds showed MIC (minimum inhibitory concentration) values higher than 50 µM against several Gram-positive and negative strains, and showed no cytotoxicity at the concentration of 100 µM against the human cancer cell lines A549, HCT-8 and MCF-7. The discovery of 1–4expands the structural diversity of tryptamine-derived natural products, and sets the stage for revealing their biosynthetic mechanisms and biological activities in the future.



Simultaneous determination of five phenylethanoid glycosides in Cistanches Herba using quantitative analysis of multi-components by single marker

Ruiyan Li, Mingbo Zhao, Pengfei Tu, Yong Jiang

2019, 28(8):  537-546.  DOI: 10.5246/jcps.2019.08.051

Asbtract ( 268 )   HTML ( 1)   PDF (1349KB) ( 205 )  

References | Related Articles | Metrics

In the present study, a method for the quantitative analysis of multi-components by single marker (QAMS)has been developed and validated for the simultaneous determination of echinacoside (ECH), tubuloside A, acteoside, isoacteoside, and 2'-acetylacteoside inCistanches Herba. ECH was used as the internal standard (IS) to obtain the relative correction factors (RCFs) of the other four phenylethanoid glycosides (PhGs); meanwhile, various influencing factors on RCFs were investigated under differentconditions. The content of each component was calculated with RCF. The results were compared with those obtained by the external standard method (ESM) to verify the feasibility and accuracy of the established QAMS method. No significant differencewas found in the quantitative results of 10 batches of Cistanches Herba between QAMS and ESM.The proposed QAMS method for simultaneous determination of PhGs in Cistanches Herba is accurate and feasible, providing an efficient and economical approach for the quality control of Cistanches Herba. 



A small molecule LS-1-2F promotes the endocytosis of macromolecules into tumor cells

Yanyan Yang, Dengbo Ji, Simin Yang, Siwang Yu, Zhongjun Li, Xiangbao Meng

2019, 28(8):  547-555.  DOI: 10.5246/jcps.2019.08.052

Asbtract ( 258 )   HTML ( 3)   PDF (2048KB) ( 156 )  

References | Related Articles | Metrics

In the previous research, we found that anticancer agent LS-1-2F could cause the vacuolation of tumor cells. Herein we investigated the effect of compound LS-1-2F on the endocytosis of macromolecules, including fluorescence quantum dots, human serum albumin, single-stranded RNA, and monoclonal antibody, into tumor cells. We found that LS-1-2F could accelerate the endocytosis of these large molecules by laser confocal microscope and flow cytometry. The effect of LS-1-2F on the improvement of the internalization efficiency of Herceptin biosimilar was particularly significant. Promoting endocytosis will help increase the efficiency of liquid-phase drug uptake in drug-resistant cancer cells and could potentially facilitate the use of drugs in nanoparticle delivery vehicles. 



A novel fluorescent sensor for cAMP based on E. coli CAP protein

Jiayuan Zhang, Yuxin Song, Chuchen Wang, Jing Wang

2019, 28(8):  556-560.  DOI: 10.5246/jcps.2019.08.053

Asbtract ( 333 )   HTML ( 3)   PDF (1623KB) ( 228 )  

References | Related Articles | Metrics

cAMP is an important second messenger that is capable of controlling a wide array of cellular processes, including glycogen, sugar and lipid metabolism. Here we report the design and construction of a novel genetically encoded fluorescent sensor for cAMP. The sensor was realized by fusing E. coli CAP protein with cpYFP, and displayed a one-fold fluorescence change towards cAMP binding. Further characterization assays demonstrated that the sensor had high affinity for cAMP and fast response kinetics. The development of our sensor could be a useful supplement to existing methods for cAMP detection.



Construction and characterization of intestinal oligopeptide transporter PepT1-targeted polymeric micelles for enhanced intestinal absorption of poorly water-soluble agents

Yao Jin, Qi Liu, Chuhang Zhou, Shidi Han, Yuanhang Zhou, Xinping Hu, Leqi Wang, Yan Liu

2019, 28(8):  561-570.  DOI: 10.5246/jcps.2019.08.054

Asbtract ( 264 )   HTML ( 2)   PDF (3851KB) ( 69 )  

Related Articles | Metrics

To overcome the main barrier of intestinal epithelium for the oral absorption of poorly water-soluble drugs and further improve their oral absorption, Gly-Sar, the substrate of the oligopeptide transporter PepT1 widely distributed in the small intestine,conjugated poly(ethylene glycol)-block-poly(D,L-lactide) (Gly-Sar-PEG-b-PLA) was designed and synthesized, and PepT1-targetedpolymeric micelles were prepared and characterized. The structure of the synthesized Gly-Sar-PEG-b-PLA was confirmed by use of TLC and ¹H-NMR. The average molecular weight measured by GPC was 5954 g/mol with PDI of 1.34. The DiI-loaded polymeric micelles from Gly-Sar-PEG-b-PLA with drug loading content of 0.076% were characterized to exhibit 40.36 nm in diameter with PDI of 0.294, and well-defined spherical shape observed by TEM. Furthermore, the PepT1-targeted polymeric micelles profoundly enhanced intestinal absorption of poorly water-soluble drug. Therefore, the designed PepT1-targeted polymeric micelles might have a promising potential for oral delivery of water-insoluble drugs.



Decoration of bacterial outer membrane vesicles with liposomes

Jiaxing Wang, Yu Wang, Jiahui Mou, Xiaomeng Wei, Mengya Yin, Yajie Liu, Jiajia Li, Xinru Li

2019, 28(8):  571-578.  DOI: 10.5246/jcps.2019.08.055

Asbtract ( 363 )   HTML ( 12)   PDF (1757KB) ( 114 )  

References | Related Articles | Metrics

In this study, liposomes were used to decorate bacterial outer membrane vesicles (OMVs), and decorated OMVs were evaluated in vitro. The OMVs of Pseudomonas aeruginosa were extracted by pressure-induced ammonium sulfate precipitation, and their particle size, distribution, zeta potential, protein content and stability were determined. Several types of liposomes were prepared by thin film dispersion method, and the OMVs were decorated by vortexing, sonication and extrusion, respectively. The interaction between liposome and OMV was studied with fluorescence resonance energy transfer (FRET) method. The results showed that the OMVs were spherical in shape and negatively charged. The vortexing method exerted little effect on the particle size and distribution of the decorated OMVs. The sonication process reduced the particle size and distribution of OMVs. FRET experiment indicated that the OMVs were decorated through membrane fusion. The above-mentioned results indicated that liposomes could successfully decorate OMVs, and decorated OMVs certainly widened their applications. 



Preparation of a Hippophae rhamnoides Linn oil nanoemulsion and the visualization of its transdermal permeation

Qi Shen, Mei Wang, Xiaohui Tang, Munire Kuerban

2019, 28(8):  579-594.  DOI: 10.5246/jcps.2019.08.056

Asbtract ( 324 )   HTML ( 3)   PDF (2104KB) ( 148 )  

References | Related Articles | Metrics

A Hippophae rhamnoides Linn oil nanoemulsion was developed, and its physicochemical properties and in vitro transdermalcharacteristics were investigated. Then its skin irritation was investigated.The optimum Hippophae rhamnoides Linn oil nanoemulsion prescription was determined using Cremophor EL as an emulsifier, Transcutol P as a co-emulsifier, and isopropyl myristate (IPM) as the oil phase (IPM%:Cremophor EL%:Hippophae rhamnoides Linn oil% = 5:16:20, Km = 4:1). The prepared Hippophaerhamnoides Linn oil nanoemulsion was pale yellow and transparent. Globular droplets were observed under a transmission electronmicroscope (TEM). The average particle size was 52.2±4.8 nm. The loading capacity was 10.68%, and the oil-in-water (O/W) type nanoemulsion was stable after centrifugation. The CLSM results showed that the fluorescence intensity of the OB Hippophae rhamnoides Linn oil nanoemulsion group was stronger than that of the Hippophae rhamnoides Linn oil cream and Hippophae rhamnoides Linn oil groups in each layer of skin. The study also showed that skin surface treated with the Hippophae rhamnoides Linn oil nanoemulsion had strong fluorescence. The skin depth had weak fluorescence, while the areas near the hair follicle and its appendages had the strongest fluorescence. The skin irritation test showed that the prepared Hippophae rhamnoides Linn oil nanoemulsion was applied to the normal and damaged skin of the rabbit, and there was no apparent redness and swelling. These results suggested that the nanoemulsion coated with Hippophae rhamnoides Linn oil was a potential delivery system for skin disorders.