4-oxo-4H-pyran-2.6-dicarboxylic acid (chelidonic acid, ChA) in the native state and in the complex with calcium [Ca(ChA)(H2O)3], named saucalchelin (CaChA), was isolated from the extract of Saussurea controversa leaves for the first time for the Asteraceae family. The structure of ChA was determined by NMR, MS and confirmed by X-ray analysis of its monomethyl ester, and CaChA was described by IR, ICP-MS, CHN analysis. The yield of ChA and CaChA was 45 mg/g and 70 mg/g of extract, respectively. The osteogenic activity of ChA, n-monobutyl ester of chelidonic acid, and CaChA has been studied in vitro in a 21-day culture of human adipose-derived multipotent mesenchymal stromal cells (hAMMSCs) in a standard nutrient medium without osteogenic supplements. CaChA significantly stimulated the growth of cell mass and differentiation of hAMMSCs into osteoblasts with subsequent mineralization of the culture and it may be a promising substance for accelerating bone tissue regeneration and engineering.
Five flavonoids were isolated from leaves of Saussurea controversa, one new flavonoid (5), three described for the first time from the genus Saussurea (1, 2, and 4), and one described previously (3). A number of flavonol glycosides can be easily isolated from the butanol fraction of the ethanol extract from S. controversa. As a result of separating these using column chromatography on silica gel and microcrystalline cellulose, five glycosides of quercetin were isolated in the proportional relationship of 2 (1): 8 (2): 10 (3): 1 (4): 4 (5). The structure of these substances was determined using the method of NMR by conducting various 1H-1H and 1H-13C correlation spectroscopy experiments and by comparing their spectroscopic data with published values, 5,3/,4/-trihydroxyflavone-7-О-α-L-rhamnopyranoside-3-О-β-D-glucopyranosidе (1), 5,7,3/,4/-tetrahydroxyflavone-3-О-β-D-glucopyranoside-(1→6)-β-D-glucopyranoside-(1→6)-О-α-L-rhamnopyranoside (2), 5,7,3/,4/-tetrahydroxyflavone-3-О-β-D-glucopyranoside-(1→6)-О-α-L-rhamnopyranoside (3), 5,3/,4/-trihydroxyflavone-7-О-α-L-rhamnopyranoside-3-О-β-D-xylopyranoside (4), and 5,3/,4/-trihydroxyflavone-7-О-β-D-glucopyranoside-3-O-α-L-rhamnopyranoside-(1→2)-О-β-D-glucopyranoside (5). It was established for the first time that flavonol glycosides from S. controversa stimulate granulopoiesis and lymphopoiesis in the bone marrow of rats, and enhance the reparative process in the affected area in experimental osteomyelitis.
A chromatographically inseparable crystalline mixture of the previously undescribed quercetin-4′-O-β-galactopyranoside and the known quercetin-3-O-β-glucopyranoside (isoquercitrin) in a 7:5 ratio was isolated from the extract of the aerial part of Filipendula ulmaria (L.) Maxim.
Constituent composition of the essential oils from some species of the genus Saussurea DCThe genus Saussurea DC is well known for its rich chemical composition and wide range of biological activities. Although content and biological effects of major chemical components are thoroughly studied, the composition and concentrations of minor constituents, such as essential oils, still remains unclear. In total, 62 different chemical compounds have been identified in the essential oils from S. controversa, S. latifolia, S. parviflora and S. salicifolia using a gas chromatography-mass spectrometry method. The essential oils include 1-5% of linalool, 2-7% of eudesmol and oxygen-containing sesquiterpenoids: 7 -25 % of caryophyllene oxide, 4 -5% of spathulenol, 4 -6% of humulene-6.7-oxide. The presence of sesquiterpenoids can be considered as a chemotaxonomic feature of the studied species of Saussurea DC. The essential oils can be candidates for new anti-inflammatory, analgesic and anti-tumor drugs due to relatively high concentration of caryophyllene oxide.
A model of traumatic osteomyelitis in rats is created. The disease development was evaluated by bone marrow myelograms, results of scintigraphy, and histological studies.
The osteogenic, cytotoxic, and antibacterial activities of polysaccharide (PS-SC) and flavonoid (F-SC) fractions isolated from the leaves extract of Saussurea controversa were studied in vitro. F-SC consists of the five quercetin glycosides in the ratio 2:8:10:1:4, which were isolated from the leaves extract of S. controversa and have been characterized previously. PS-SC was first isolated from the leaves extract of S. controversa and has been described. PS-SC consists in 30 compounds is characterized by a high degree of heterogeneity with a heterogeneity index of 19.74. The Mw and Mn of PS-SC were 108.6 and 5.5 kDa, respectively. Structural fragments are represented by galactose, arabinose, xylose, glucose, uronic acids, mannose, and rhamnose in a 10.1:3.3:2.2:2.1:1.7:0.9:0.5 molar ratio. F-SC as compared with PS-SC showed in vitro microbicidal (50 g/L) and better bacteriostatic (6.25 g/L versus 25 g/L of PS-SC) effects against the 24-h growth of Staphylococcus aureus strain 209 P and a 21-day absence of cytotoxicity on human adipose-derived multipotent mesenchymal stromal cells (hAMMSCs). Both fractions (PS-SC > F-SC) at doses of 10–50 mg/L stimulated differentiation of hAMMSCs into secreting osteoblasts accompanied by local mineralization of extracellular matrix. These fractions of S. controversa and especially F-SC, might be promising peroral drugs in the complex treatment of bone fractures and for prophylaxis of their infectious complications.
Aim To analyze frequency and profile of the lipid-lowering therapy (LLT) in patients with dyslipidemia (DLP) and cardiometabolic diseases (CMD) in a population sample aged 55-84 years at the current time (2015–2017).Material and methods Despite guidelines on DLP treatment and the availability of effective and safe lipid-lowering drugs, control of DPL in primary and secondary prevention of cardiovascular diseases (CVD) is insufficient. Knowledge of the level of pharmaceutical correction of DLP in the Russian population is limited; it requires an LLT assessment in various regions and in a wide age range, and a regular monitoring taking into account changing approaches to the correction of DLP. A random population of men and women aged 55–84 years (n=3 896) was evaluated in Novosibirsk in 2015–2017 (project HAPIEE). A joint DLP category was established as low-density lipoprotein cholesterol (LDL-C) ≥3.0 mmol/l, or total cholesterol (TC) ≥5.0 mmol/l, or triglycerides (TG) ≥1.7 mmol/l, or LLT. The combined group of DLP and CMD included ischemic heart disease (IHD), type 2 diabetes mellitus (DM2), and DLP. Regular LLD treatment for the recent 12 months, excluding the dosage of medicines, was assessed using the Anatomic Therapeutic Chemical (ATC) classification. The conditional control of serum lipids was taken as the achievement of LDL-C <3.0 mmol/l, TC <5.0 mmol/l, and TG <1.7 mmol/l.Results In the study sample, the total prevalence of DLP and CMD was 88 % (82.8 % for men and 91.3 % for women, p<0.001). 48.3% of patients in the IHD group, 35.0% in the DM2 group, 29.4% in the DLP group, and 32.8% in the CMD group took LLT. Control of serum lipids was achieved in 18.3% (37.9 % of patients on LLT) of patients with IHD; 9 % (25.6 % of patients on LLT) of patients with DM2; 7.3 % (24.8 % of patients on LLT) of patients with DLP; and 9.0 % (27.6 % of patients on LLTсреди) in the DLP and CMD group. Women with DM2 and DLP more frequently achieved lipid control than men (p<0.001). 98.7 % of study participants took statins as LLT.Conclusion In the sample of urban population aged 55–84 years in 2015–2017, 90 % of patients had DLP or CMD, and at least ¾ of them required blood lipid control. The lipid control was achieved in every fifth IHD patient and in approximately 40% of those who took LLT. For DM2 or DLP patients, the lipid control was achieved in every tenth patient and in approximately 25% of those receiving LLT. Frequency of lipid control in IHD patients was comparable for men and women; in DM2 and DLP, men less frequently achieved the lipid control than women. About 70% of patients in the combined DLP and CMD group and more than 50% of IHD patients did not take LLT, which considerably contributed to the insufficient lipid control in primary and secondary prevention of atherosclerotic CVDs in this population.
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