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Two new iridoid glycosides, piasezkiiosides A (1) and B (2), were isolated from aqueous extract of the whole plant of Rehmannia piasezkii. Their structures were established from the spectroscopic data, chemical transformation, and X-ray diffraction analysis. Compound 1 exhibited weak hepatoprotective activity against APAP-induced HepG2 cell damage. [ABSTRACT FROM AUTHOR]

Four new iridoid glycosides (1–4), rehmaglutosides L–O, were isolated from the air-dried roots of Rehmannia glutinosa. Their structures were established from the spectroscopic data obtained and by chemical evidence. The known mellittoside (5) and ajugol (6) were also obtained in the current investigation, and the structure of mellittoside was unequivocally defined using X-ray diffraction data. Compounds 1–6 were tested for their cytotoxicity against five human tumor cell lines and proliferation effects on Lactobacillus Reuteri. [ABSTRACT FROM AUTHOR]

Phytochemical investigation on the aerial parts of Salvia deserta led to the isolation of eight new pentacyclic triterpenoids including three oleanane- (1 − 3) and five ursane-type (4 − 8) triterpenoids, whose structures were elucidated based on extensive spectroscopic analysis and quantum chemical calculation. Weak immunosuppressive potency was observed for compounds 1, 2, and 4 − 8 via inhibiting the secretion of cytokines TNF-α and IL-6 in LPS-induced macrophages RAW264.7 at 20 μM. In addition, compounds 1, 2, and 4 − 6 exhibited moderate protective activity on t-BHP-induced oxidative injury in HepG2 cells. [ABSTRACT FROM AUTHOR]

A new aromatic glycoside (1) and twelve (2–13) known aromatic glycosides were isolated from the n-butyl alcohol of the 70% EtOH extract of the aerial part of Bupleurum chinense. Among them, compounds 4–7, 9, 11–13 were isolated from Umbelliferae plants for the first time. Their structures were elucidated by NMR and MS spectroscopy, and the absolute configuration of compound 1 was elucidated by single-crystal X-ray diffraction. Compounds 6 and 10 showed moderate cytotoxic activities on MGC-803 cell lines with IC50 values of 8.63 ± 0.08 and 13.65 ± 1.73 μM, respectively. [ABSTRACT FROM AUTHOR]

As part of an ongoing project on Rehmannia species, three new pyridine alkaloides (glutinosines A − C), and one new iridoid analogue (rehmaglutin E), were isolated from the leaves of Rehmannia glutinosa. The structures of the new compounds were established by extensive spectroscopic analysis and electronic circular dichroism calculations. [ABSTRACT FROM AUTHOR]

Two new steroids meteloside F (1) and meteloside G (2), together with six known ones (3–8), were isolated and identified from the seeds of Datura metel L. The chemical constituents were isolated by silica gel, ODS chromatogram columns. and preparative HPLC. The structures of these compounds were established by one- and two-dimensional NMR spectra and HR-ESI-MS. The compounds exhibited inhibition on the nitric oxide release of lipopolysaccharide-induced RAW 264.7 cells with IC50 values from 30.2 to 44.8 μM. [ABSTRACT FROM AUTHOR]

Five new iridoids (1-5), jiohenrins A-E, together with sixteen known compounds (6-21), were isolated from the whole plants of Rehmannia henryi. The structures of these compounds were elucidated on the basis of their spectroscopic data. [ABSTRACT FROM AUTHOR]

1. Safflower injection (SI) is extracted from Chinese herbal medicine safflower that comprises many active components. Warfarin is a common anticoagulant and has exhibited drug interactions with several herbal products. This study aimed to investigate the effects of SI on pharmacodynamics and pharmacokinetics of warfarin in rats. 2. Wistar rats were randomly divided into blank control group, SI group, warfarin control group and SI + warfarin group, respectively. In SI and SI + warfarin groups, rats were injected with SI (1.6 mL/kg/d, i.p.) for 14 days. Warfarin (0.2 mg/kg) was given orally on the eighth day. Saline was given as control. The blood samples were collected at various time points. Prothrombin time (PT) and activated partial thromboplastin time (APTT) were measured. UPLC-MS/MS was used to determine the plasma concentrations of S(R)-warfarin, and the pharmacokinetic parameters were calculated. 3. PT, APTT in SI and SI + warfarin rats increased significantly compared with corresponding control rats. The pharmacokinetic parameters including Cmax, t1/2, AUC0-t and AUC0-∞ of S-warfarin and R-warfarin in SI + warfarin rats were higher than those in warfarin control rats. 4. These findings suggest that SI significantly increases the anticoagulant effect of warfarin by affecting its pharmacodynamic and pharmacokinetic parameters. [ABSTRACT FROM AUTHOR]

Schisandra sphenantheraRehd. et Wils. belongs to theSchisandrafamily and its fruits are known to be the effective parts in Traditional Chinese Medicine (TCM). The chemical compositions of the essential oils from different parts of fruits ofS. sphenantheraisolated by hydrodistillation extraction were analyzed by GC-MS. The extraction yield percentage of the essential oils from the seed and pulp were 2.82% and 0.65% (% dry weight,v/w), respectively. The color of the essential oils from the seed were ivory-white and yellowish for pulp, respectively. A total of sixty compounds were identified and there were 15 mutual compounds existed in two different parts. Although the majority of these compounds (more than 65%) belonged to sesquiterpenes and oxygenated sesquiterpenes. The differences between seed and pulp were readily observed: ketones were only found in seed, and aldehyde, halogenated hydrocarbons, olefin hydrocarbons, acids and alcohols were only found in pulp. [ABSTRACT FROM PUBLISHER]

Tripterygium wilfordiiHook. f. is the traditional medicinal plants in China. Triptolide, wilforgine, and wilforine are the bioactive compounds inT. wilfordii.In this study, the contents of three metabolites and transcription levels of 21 genes involved in three metabolites biosynthesis inT. wilfordiiwere examined using high-performance liquid chromatography and reverse transcription PCR after application of methyl jasmonate (MeJA) on hairy roots in time course experiment (3–24 h). The results indicated that application of MeJA inhibited triptolide accumulation and promoted wilforgine and wilforine metabolites biosynthesis. In hairy roots, wilforgine content reached 693.36 μg/g at 6 h after adding MeJA, which was 2.23-fold higher than control. The accumulation of triptolide and wilforine in hairy roots increased the maximum at 9 h, which was 1.3- and 1.6-folds more than the control. Most of the triptolide secretes into the medium, but wilforgine and wilforine cannot secrete into the medium. The expression levels of unigenes which involved terpenoid backbone biosynthesis exist the correlation with marker metabolites (triptolide, wilforgine and wilforine) after induction by MeJA, and can be then used to infer flux bottlenecks inT. wilfordiisecondary metabolites accumulation. These results showed that these genes may have potential applications in the metabolic engineering ofT. wilfordiimetabolites production. [ABSTRACT FROM PUBLISHER]

Three new flavonoid glycosides (1–3) and one new aristololactamN-glycoside (4) were isolated from the rhizome ofAristolochia championii. The structures of compounds1–4were elucidated on the basis of their spectroscopic data and chemical evidence (UV, IR, HR-ESI-MS, 1D and 2D NMR). Their structures were determined as 8-(5-formyl-2-furanmethyl)-isorhamentin 3-O-robinobioside (1), 8-(5-methyl-2-furanoyl)-isorhamentin 3-O-robinobioside (2), 8-formylisorhamentin 3-O-robinobioside (3), and N-β-D-glucopyranosylaristololactam V (4), respectively. [ABSTRACT FROM PUBLISHER]

Phytochemical investigation of the rhizomes ofIris tectorumresulted in the isolation and characterization of three new apocynin derivatives, apocynin-4-O-β-D-(6′-O-syringyl)glucopyranoside (1), scrophenoside C-7-ethyl ether (2,3), together with a new naturally occurring compound but known by synthesis, apocynin-4-O-β-D-xylopyranoside (4), and five known ones (5–9). Their structures were elucidated on the basis of spectroscopic data interpretation. [ABSTRACT FROM PUBLISHER]

Four new ionone and ionone glycosides (1–4), and a new monoterpene (5), together with 10 known analogues (6–15), were isolated from the air-dried roots of Rehmannia glutinosa. The structures of these compounds were elucidated on the basis of spectroscopic data analysis. Furthermore, in in vitro assays, compound 3 (10 μM) exhibited moderate hepatoprotective activities against d-galactosamine-induced HL-7702 cell damage. [ABSTRACT FROM AUTHOR]

Two new monacolin analogs, monacolins O (1) and P (2), along with three known analogs, have been isolated from the ethanolic extract ofMonascus purpureus-fermented rice. Their structures and absolute configurations were elucidated by spectroscopic methods, especially 2D NMR and CD spectral analyses as well as chemical method. Both1and2were tested against five tumor cell lines, and compound1exhibited selective cytotoxic activity against A2780 and A549 cell lines, with IC50values of 3.7 and 8.0 μM, respectively. [ABSTRACT FROM PUBLISHER]

The cytotoxic activity of 36 saponins isolated from roots ofPulsatilla chinensis(Bunge) Regel against the human cancer cell lines (A549, SGC-7901) and the human hepatic cell line (HL-7702) was tested by 3-(4,5-dimethylthiazole-2-yl)-2,5-diphenyltetrazolium bromide assay. Saponins1–14showed considerable cytotoxic activity, whereas saponins15–36showed no significant activity, which suggested that a free carboxylic group located at C-28 of aglycon is essential for their cytotoxic activity. Moreover, the analysis of structure–activity relationships also suggested that the oleanane-type saponins showed better cytotoxic activity than lupane-type saponins, and the length and linkage of glycolic chain attached to C-3 of aglycon displayed an important effect to the potent cytotoxicity. In conclusion, oleanolic acid 3-O-α-l-rhamnopyranosyl-(1 → 2)-[β-d-glucopyranosyl-(1 → 4)]-α-l-arabinopyranoside (5) exhibited the most significant cytotoxic activity. [ABSTRACT FROM PUBLISHER]

Background: Wurenchun is the alcohol extract from Fructus Schisandrae Chinensis, which has good efficiency in lowering abnormal serum glutamic pyruvic transaminase (SGPT) level of patients suffering from acute or chronic hepatitis. The main purpose of this work is to prepare self-emulsifying drug delivery systems (SEDDS) for enhancing the solubility, dissolution rate, and oral bioavailability of poorly water-soluble traditional Chinese medicines, Wurenchun. Methods: Pseudoternary phase diagrams were used to evaluate the efficient self-emulsification domains, and particle size distributions of resultant emulsions were determined. The dissolution test was performed according to the second method of Chinese Pharmacopoeia dissolution procedure. The pharmacokinetic study in rats for the optimized formulation was performed and compared to commercial capsules. Results: The optimized formulation for bioavailability assessment consisted of 20% oleic acid, 65% Tween 20, and 15% Transcutol P. The mean droplet size distribution of the optimized SEDDS was approximately 240 nm when diluted with 1000-fold volume of the distilled water. The in vitro dissolution rates of the active components of Wurenchun SEDDS were significantly higher than those of the commercial capsules. SEDDS have significantly increased the Cmax and area under the curve) (AUC) of Wurenchun compared to reference capsules ( P < 0.05). And the relative bioavailability of SEDDS for schisandrin and schisandrin B was 292.2% and 205.8% compared to the commercial capsules, respectively. Conclusion: The results suggest the potential use of SEDDS to improve oral absorption of the sparingly soluble drugs or traditional Chinese medicine, such as Wurenchun. [ABSTRACT FROM AUTHOR]

Two new C28 sterols with a cyclopentane ring at C-22 and 26, alkesterol A (1) and alkesterol B (2), along with β-sitosterol (3), were isolated from the berries of Physalis pubeacens L. (cape gooseberry). The structures of the new compounds were established by HR-EI-MS, 1D and 2D (1H-1H COSY, HSQC, HMBC) NMR experiments. The known compound was identified by comparison of spectral data with published references. The two new compounds showed some cytotoxic activities by MTT assay. [ABSTRACT FROM AUTHOR]