Saponins from Dolichos lablab seeds with anti-inflammatory activity.

As one of a traditional Chinese medicine with dual applications in both medicinal treatment and dietary consumption, the mature seeds of D. lablab were reported to be rich in saponins and have a good effect on inflammatory related diseases. However, the substance basis for its anti-inflammatory activity remains unclear. Thus, a comprehensive phytochemical investigation on triterpenoid saponins from D. lablab seeds was carried out, resulting in the isolation and identification of twenty-one new triterpenoid saponins including dolilabsaponins A1-A4, B, C, D1-D3, E-M, N1, N2 and O (1-21) along with thirteen known analogs (22-34). Notably, the known saponins, 31, 32, and 34 were obtained from Leguminosae family for the first time. The 1H and 13C NMR data of saponins 24 and 28 were firstly reported here. Additionally, lipopolysaccharide (LPS)-stimulated RAW264.7 cells model was utilized to assess inhibitory activities of compounds 1-34 on nitric oxide (NO) production. The results revealed that compounds 1-3, 9, 10, 13-15, 18, 22, 23 and 28-34 significantly suppressed the elevation of NO levels in LPS-induced RAW264.7 cells at the concentration of 30 µM, exhibiting a concentration-dependent manner at 3, 10, and 30 µM. The results suggested that compounds 1-3, 9, 10, 13-15, 18, 22, 23, and 28-34 possessed potential anti-inflammatory activity. Further western blot assay demonstrated that 1, 9, 10, 13, 14, and 18 suppressed inflammatory response via down-regulated the expression levels of inflammatory factors, tumor necrosis factor-alpha and interleukin-6.

Constituents from Dolichos lablab L. Flowers and Their Anti-Inflammatory Effects via Inhibition of IL-1ß Release.

The occurrence of inflammation is closely related to the activation of the NLRP3 inflammasome. IL-1ß produced during the activation of the NLRP3 inflammasome has strong pro-inflammatory activity and can also promote the release of inflammatory factors by other immune cells, exacerbating inflammatory damage to tissues. Utilizing IL-1ß as the detection index to find small-molecule inhibitors targeting NLRP3 from natural products will benefit the search for drugs for inflammation-related diseases. During the exploration of anti-inflammatory active components derived from the flowers of Dolichos lablab L., an ingredient in traditional Chinese medicine with dual applications in both medicinal treatment and dietary consumption, fourteen compounds (1-14), including seven previously unreported ones, named flosdolilabnitrogenousols A-D (1-4) and flosdolilabsaponins A-C (5-7), were found. Their structures were established through extensive NMR spectra determination, HR-ESI-MS analysis, ECD calculations, and chemical reactions. Flosdolilabsaponin A (5) stands out as an exceptionally rare tetracyclic lactone oleane-type saponin. Additionally, the inhibitory activity on IL-1ß release of all compounds, without cytotoxicity, was evaluated using BMDMs stimulated with LPS/Nigericin. An Elisa assay revealed that compounds 1, 8, 9, and 11-14 exhibited significant inhibition of IL-1ß release at a concentration of 30 µM. Structure-activity relationships were also discussed. This study indicates that D. lablab flowers possess anti-inflammatory activity, which might exert its effect by suppressing the activation of the NLRP3 inflammasome.

Aromatic compounds from the seeds of Dolichos lablab L. with anti-inflammatory activity.

Twenty-four aromatic compounds including five novel ones, dolilabphenosides A (1), B1 (2), B2 (3), C1 (4), and C2 (5) were obtained from the seeds of Dolichos lablab L. Their structures were established based on spectroscopic analyses and chemical reactions. Among the known compounds, 9, 10, 14, 17, 19, and 22-24 were gained from the family Leguminosae for the first time, and 6, 8, 11-13, 15, 16, 18, 20, as well as 21 were firstly identified from Dolichos genus. Moreover, the inhibitory effect evaluation of all the isolates against LPS-induced nitric oxide (NO) production in RAW264.7 macrophages suggested that compounds 1-3, 6, 7, 11-15, 17, 20, 21, 23, 24 exhibited anti-inflammatory activity in a concentration-dependent manner. Moreover, the novel compounds, dolilabphenosides A (1), B1 (2), B2 (3) were found to inhibit the secretion of inflammatory cytokine IL-1ß.

Synthesis of Methyl-d3 Arene via Electrochemical Deuterodefluorination of Trifluoromethyl Arene.

The methyl-d3 group is a new isotopic functional group for medicine design. In this work, we report an electrochemical deuteration approach for converting aromatic trifluoromethyl to methyl-d3 groups with deuterium water in common DMF. Yields up to 94%, D ratio up to 97%, and CD3 incorporation up to 90% were achieved. A basic additive is the key factor enabling the highly chemoselective reaction.

Understanding the Competitive Advantages of Car Sharing from the Travel-Cost Perspective.

The emergence and development of car sharing can not only satisfy people's diverse travel demands, but also can bring a new solution to facilitate urban low-carbon and green development. With the increasing acceptance of car sharing, the market competition between car sharing and traditional taxis is becoming increasingly fierce. Therefore, we explore the advantages of car sharing to travelers compared with taxis. In this paper, we first use the GPS (Global Positioning System) trajectory data of car sharing orders to construct a comparative advantage model based on travel-cost. Then, we take Beijing as the research area to explore the travel-cost advantages of car sharing in terms of the time and space dimensions compared with taxis, through calculating the travel-cost of car sharing and using simulation to calculate that of taxis. The results of the comparison between car sharing and taxis from the perspective of travel-cost are as follows: (1) Compared with short trips, the travel-cost advantage of car sharing is relatively higher in medium and long trips; for travelers, the taxi has a higher travel-cost advantage when the travel time is either very long or very short. (2) On weekdays, it is more cost-effective to travel by shared cars for travelers before the rush hours in the evening, and the travel-cost advantage of using taxis is greater after the evening peak. (3) Compared with weekdays, it is more cost-effective to travel by shared cars on weekends wherever travelers are living in the main urban areas or in the remote suburbs. It is suggested that relevant departments should understand the travelers' preference and analyze the influence mechanism of other various factors on the market demand for car sharing as per the focus on the market on the travel-cost advantages of car sharing, so as to promote the healthy and sustainable development of urban shared transportation.