A novel method for the direct detection of light stabilizer Tinuvin 622 in polymer additives by gel permeation chromatography combined with multi-angle laser light scattering.

Tinuvin 622, an oligomeric light stabilizer, is widely used in plastics to reduce light and heat induced degradation and extend their service life, therefore its detection is of great importance for quality control of plastic products. However, the classical analytical methods of Tinuvin 622, such as chromatography and mass spectrometry, are difficult to achieve direct qualitative and quantitative analysis, and simultaneously to obtain the molecular weight and molecular weight distribution information. Herein, we propose for the first time the combination of gel permeation chromatography with multi-angle laser light scattering as a simple and direct method to detect Tinuvin 622 in polymers and simultaneously to obtain its molecular weight distribution information. The linearity of the method was good in the concentration range of 0.1-5.0 mg/mL Tinuvin 622 with correlation coefficient (R2 = 0.9999), and the recoveries of Tinuvin 622 at three addition levels ranged from 94.0% to 98.7%, with relative standard deviations of no more than 1.73%. The proposed method has been successfully used to detect Tinuvin 622 in actual samples of polymer additives. Compared with existing analytical methods, Tinuvin 622 has a single peak shape in our method, which is easy to identify and quantify accurately; more importantly, our method can simultaneously characterize the molecular weight and molecular weight distribution of Tinuvin 622, which makes up for the shortcomings of other approaches and provides a new tool for quality monitoring of polymer additives.

Anti-Ovarian Cancer Conotoxins Identified from Conus Venom.

Conotoxins constitute a treasury of drug resources and have attracted widespread attention. In order to explore biological candidates from the marine cone snail, we isolated and identified three novel conopeptides named as Vi14b, Vi002, Vi003, three conotoxin variants named as Mr3d.1, Mr3e.1, Tx3a.1, and three known conotoxins (Vi15a, Mr3.8 and TCP) from crude venoms of Conus virgo, Conus marmoreus and Conus texile. Mr3.8 (I-V, II-VI, III-IV) and Tx3a.1 (I-III, II-VI, IV-V) both showed a novel pattern of disulfide connectivity, different from that previously established for the µ- and ψ-conotoxins. Concerning the effect on voltage-gated sodium channels, Mr3e.1, Mr3.8, Tx3a.1, TCP inhibited Nav1.4 or Nav1.8 by 21.51~24.32% of currents at semi-activated state (TP2) at 10 µmol/L. Certain anti-ovarian cancer effects on ID-8 cells were exhibited by Tx3a.1, Mr3e.1 and Vi14b with IC50 values of 24.29 µM, 54.97 µM and 111.6 µM, respectively. This work highlights the role of conotoxin libraries in subsequent drug discovery for ovarian cancer treatment.

Isolation and characterization of five novel disulfide-poor conopeptides from Conus marmoreus venom.

Background: Conopeptides from cone snail venom have aroused great interest related to the discovery of novel bioactive candidates, due to their excellent prospects for the treatment of various health problems such as pain, addiction, psychosis and epilepsy. In order to explore novel biopeptides, we investigated the structure and function of five novel conopeptides isolated from the venom of Conus marmoreus from South China Sea. Methods: C. marmoreus crude venom was prepared, fractionated and purified by HPLC system. The primary sequences of the five novel disulfide-poor conopeptides Mr-1 to Mr-5 were identified by comprehensive analysis of de novo MALDI-TOF tandem mass spectrometry and Edman degradation data. In order to investigate their function, these five conopeptides were synthesized by Fmoc-SPPS chemistry, and their biological effects at several heterologous rat nicotinic acetylcholine receptor (nAChR) subtypes (α1ß1δε, α3ß2, α3ß4, α4ß2) were determined by electrophysiological technique. Results: Five novel disulfide-poor conopeptides were identified and named as follows: Mr-1 (DWEYHAHPKPNSFWT), Mr-2 (YPTRAYPSNKFG), Mr-3 (NVIQAPAQSVAPP NTST), Mr-4 [KENVLNKLKSK(L/I)] and Mr-5 [NAVAAAN(L/I)PG(L/I)V]. None of them contains a disulfide bond. The sequences of conopeptides Mr-2 to Mr-5 do not belong to any category of the known disulfide-poor conopeptides. No significant activity against the above nAChR subtypes were observed for the five conopeptides at 100 µM. Conclusion: We purified and structurally characterized five novel disulfide-poor conopeptides from C. marmoreus crude venom and first investigated their nAChR inhibitory effects. This work expanded our knowledge on the structure and function of disulfide-poor conopeptides from this cone snail venom.

Isolation and characterization of five novel disulfide-poor conopeptides from Conus marmoreus venom

Background: Conopeptides from cone snail venom have aroused great interest related to the discovery of novel bioactive candidates, due to their excellent prospects for the treatment of various health problems such as pain, addiction, psychosis and epilepsy. In order to explore novel biopeptides, we investigated the structure and function of five novel conopeptides isolated from the venom of Conus marmoreus from South China Sea. Methods: C. marmoreus crude venom was prepared, fractionated and purified by HPLC system. The primary sequences of the five novel disulfide-poor conopeptides Mr-1 to Mr-5 were identified by comprehensive analysis of de novo MALDI-TOF tandem mass spectrometry and Edman degradation data. In order to investigate their function, these five conopeptides were synthesized by Fmoc-SPPS chemistry, and their biological effects at several heterologous rat nicotinic acetylcholine receptor (nAChR) subtypes (α1β1δε, α3β2, α3β4, α4β2) were determined by electrophysiological technique. Results: Five novel disulfide-poor conopeptides were identified and named as follows: Mr-1 (DWEYHAHPKPNSFWT), Mr-2 (YPTRAYPSNKFG), Mr-3 (NVIQAPAQSVAPP NTST), Mr-4 [KENVLNKLKSK(L/I)] and Mr-5 [NAVAAAN(L/I)PG(L/I)V]. None of them contains a disulfide bond. The sequences of conopeptides Mr-2 to Mr-5 do not belong to any category of the known disulfide-poor conopeptides. No significant activity against the above nAChR subtypes were observed for the five conopeptides at 100 µM. Conclusion: We purified and structurally characterized five novel disulfide-poor conopeptides from C. marmoreus crude venom and first investigated their nAChR inhibitory effects. This work expanded our knowledge on the structure and function of disulfide-poor conopeptides from this cone snail venom.(AU)

Metabolomic profiling of M. speciosa champ at different growth stages.

Millettia speciosa Champ (M. speciosa) is an edible food and folk medicine and extracts from its roots exhibit a hepatoprotective effect. However, its metabolic growth process and the best harvest time have not been reported. This study systematically evaluated the metabolomic profiling of M. speciosa root extracts at different growth stages through the UPLC-Q-TOF-MS, nuclear magnetic resonance (NMR) and An orthogonal partial least squares-discriminant analysis (OPLS-DA). The results revealed there were significant differences among extracts from six ages of M. speciosa, and 110 compounds were identified. Pharmacological studies showed that 5-year and 20-year old M. speciosa roots may exhibit higher fat-lowering effects, while 5-year-old (M.s-5Y) showed better hepatoprotective activity in high-fat diet (HFD)-induced nonalcoholic fatty liver disease (NAFLD) mice. Hence, our study suggested that M.s-5Y may have potent efficacy in ameliorating NAFLD, which might be useful in determining the optimum time to harvest M. speciosa.