scholarly journals Scale-Up Preparation of Crocins I and II from Gardeniajasminoides by a Two-Step Chromatographic Approach and Their Inhibitory Activity Against ATP Citrate Lyase

Molecules ◽  
2021 ◽  
Vol 26 (11) ◽  
pp. 3137
Author(s):  
Shuguang Guan ◽  
Qiaoli Pu ◽  
Yinan Liu ◽  
Honghong Wu ◽  
Wenbo Yu ◽  
...  

Crocins are highly valuable natural compounds for treating human disorders, and they are also high-end spices and colorants in the food industry. Due to the limitation of obtaining this type of highly polar compound, the commercial prices of crocins I and II are expensive. In this study, macroporous resin column chromatography combined with high-speed counter-current chromatography (HSCCC) was used to purify crocins I and II from natural sources. With only two chromatographic steps, both compounds were simultaneously isolated from the dry fruit of Gardenia jasminoides, which is a cheap herbal medicine distributed in a number of countries. In an effort to shorten the isolation time and reduce solvent usage, forward and reverse rotations were successively utilized in the HSCCC isolation procedure. Crocins I and II were simultaneously obtained from a herbal resource with high recoveries of 0.5% and 0.1%, respectively, and high purities of 98.7% and 99.1%, respectively, by HPLC analysis. The optimized preparation method was proven to be highly efficient, convenient, and cost-effective. Crocins I and II exhibited inhibitory activity against ATP citrate lyase, and their IC50 values were determined to be 36.3 ± 6.24 and 29.7 ± 7.41 μM, respectively.

1984 ◽  
Vol 218 (3) ◽  
pp. 733-743 ◽  
Author(s):  
R W Brownsey ◽  
N J Edgell ◽  
T J Hopkirk ◽  
R M Denton

Protein kinase activity in high-speed supernatant fractions prepared from rat epididymal adipose tissue previously incubated in the absence or presence of insulin was investigated by following the incorporation of 32P from [gamma-32P]ATP into phosphoproteins separated by sodium dodecyl sulphate/polyacrylamide-gel electro-phoresis. Incorporation of 32P into several endogenous proteins in the supernatant fractions from insulin-treated tissue was significantly increased. These included acetyl-CoA carboxylase and ATP citrate lyase (which exhibit increased phosphorylation within fat-cells exposed to insulin), together with two unknown proteins of subunit Mr 78000 and 43000. The protein kinase activity increased by insulin was distinct from cyclic AMP-dependent protein kinase, was not dependent on Ca2+ and was not appreciably affected by dialysis or gel filtration. The rate of phosphorylation of added purified fat-cell acetyl-CoA carboxylase and ATP citrate lyase was also increased by 60-90% in high-speed-supernatant fractions prepared from insulin-treated tissue. No evidence for any persistent changes in phosphoprotein phosphatase activity was found. It is concluded that insulin action on acetyl-CoA carboxylase, ATP citrate lyase and other intracellular proteins exhibiting increased phosphorylation involves an increase in cyclic AMP-independent protein kinase activity in the cytoplasm. The possibility that the increase reflects translocation from the plasma membrane, perhaps after phosphorylation by the protein tyrosine kinase associated with insulin receptors, is discussed.


2007 ◽  
Vol 1142 (2) ◽  
pp. 115-122 ◽  
Author(s):  
Lijuan Chen ◽  
Qiang Zhang ◽  
Guangli Yang ◽  
Linyu Fan ◽  
James Tang ◽  
...  

2021 ◽  
Vol 17 (4) ◽  
pp. 1-29
Author(s):  
Cheng Li ◽  
Hao Chen ◽  
Chaoyi Ruan ◽  
Xiaosong Ma ◽  
Yinlong Xu

Key-value (KV) stores support many crucial applications and services. They perform fast in-memory processing but are still often limited by I/O performance. The recent emergence of high-speed commodity non-volatile memory express solid-state drives (NVMe SSDs) has propelled new KV system designs that take advantage of their ultra-low latency and high bandwidth. Meanwhile, to switch to entirely new data layouts and scale up entire databases to high-end SSDs requires considerable investment. As a compromise, we propose SpanDB, an LSM-tree-based KV store that adapts the popular RocksDB system to utilize selective deployment of high-speed SSDs . SpanDB allows users to host the bulk of their data on cheaper and larger SSDs (and even hard disc drives with certain workloads), while relocating write-ahead logs (WAL) and the top levels of the LSM-tree to a much smaller and faster NVMe SSD. To better utilize this fast disk, SpanDB provides high-speed, parallel WAL writes via SPDK, and enables asynchronous request processing to mitigate inter-thread synchronization overhead and work efficiently with polling-based I/O. To ease the live data migration between fast and slow disks, we introduce TopFS, a stripped-down file system providing familiar file interface wrappers on top of SPDK I/O. Our evaluation shows that SpanDB simultaneously improves RocksDB's throughput by up to 8.8 \times and reduces its latency by 9.5–58.3%. Compared with KVell, a system designed for high-end SSDs, SpanDB achieves 96–140% of its throughput, with a 2.3–21.6 \times lower latency, at a cheaper storage configuration.


Molecules ◽  
2020 ◽  
Vol 25 (21) ◽  
pp. 5219
Author(s):  
Carlota Salgado ◽  
Hugo Morin ◽  
Nayara Coriolano de Aquino ◽  
Laurence Neff ◽  
Cláudia Quintino da Rocha ◽  
...  

Arrabidaea brachypoda is a plant commonly used for the treatment of kidney stones, arthritis and pain in traditional Brazilian medicine. Different in vitro and in vivo activities, ranging from antinociceptive to anti-Trypanosoma cruzi, have been reported for the dichloromethane root extract of Arrabidaea brachypoda (DCMAB) and isolated compounds. This work aimed to assess the in vitro anti-inflammatory activity in arthritic synoviocytes of the DCMAB, the hydroethanolic extract (HEAB) and three dimeric flavonoids isolated from the DCMAB. These compounds, brachydin A (1), B (2) and C (3), were isolated both by medium pressure liquid and high-speed counter current chromatography. Their quantification was performed by mass spectrometry on both DCMAB and HEAB. IL-1β activated human fibroblast-like synoviocytes were incubated with both extracts and isolated compounds to determine the levels of pro-inflammatory cytokine IL-6 by enzyme-linked immunosorbent assay (ELISA). DCMAB inhibited 30% of IL-6 release at 25 µg/mL, when compared with controls while HEAB was inactive. IC50 values determined for 2 and 3 were 3-fold higher than 1. The DCMAB activity seems to be linked to higher proportions of compounds 2 and 3 in this extract. These observations could thus explain the traditional use of A. brachypoda roots in the treatment of osteoarthritis.


2015 ◽  
Vol 990 ◽  
pp. 104-110 ◽  
Author(s):  
Geison Modesti Costa ◽  
Paola Andrea Cárdenas ◽  
Andressa Córneo Gazola ◽  
Diana Marcela Aragón ◽  
Leonardo Castellanos ◽  
...  

2021 ◽  
Vol 11 (1) ◽  
Author(s):  
Chunsheng Zhu ◽  
Hongjuan Niu ◽  
Anzheng Nie ◽  
Meng Bian

AbstractClerodendranthus Spicatus is a traditional Dais medi-edible plant and it has been proven to have good blood glucose-lowering efficacy. However, the material basis of Clerodendranthus Spicatus has not been clarified yet and therefore needs to be determined. In this paper, the effective ingredients of this medicine were purified by high-speed counter-current chromatography. Alongside, their potential hypoglycemic activity was determined by α-glucosidase inhibitory activities in vitro and molecular docking. Finally, five compounds were purified and identified as 2-caffeoyl-L-tartaric acid (1), N-(E)-caffeoyldopamine (2), rosmarinc acid (3), methyl rosmarinate (4), 6,7,8,3′,4′-Pentamethoxyflavone (5). Examination of α-glucosidase inhibitory activity in vitro showed that 2-caffeoyl-L-tartaric acid and rosmarinic acid had a higher inhibitory activity than acarbose. Molecular docking indicated that the affinity energy of the identified compounds ranged from − 7.6 to − 8.6 kcal/mol, a more desirable result than acarbose (− 6.6 kcal/mol). Particularly, rosmarinc acid with the lowest affinity energy of − 8.6 kcal/mol was wrapped with 6 hydrogen bonds. Overall, α-glucosidase inhibitory activities and molecular docking suggested that rosmarinc acid was likely to be a promising hypoglycemic drug.


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