Amentoflavone is a potent broad-spectrum inhibitor of human UDP-glucuronosyltransferases.

Amentoflavone (AMF), an abundant natural biflavonoid found in many medicinal plants, displays various beneficial effects including anti-inflammatory, anti-oxidative and anti-cancer. Despite the extensive studies on pharmacological activities, the toxicity or undesirable effects of AMF are rarely reported. In this study, the inhibitory effects of AMF on human UDP-glucuronosyltransferases (UGTs) were carefully investigated. AMF displayed strong inhibition towards most of human UGTs including UGT1A1, 1A3, 1A4, 1A6, 1A7, 1A8, 1A9, 1A10, 2B4 and 2B17, with the IC50 values ranging from 0.12 µM to 16.81 µM. Inhibition constants (Ki) of AMF against various human UGTs varied from 0.29 µM to 11.51 µM. Further investigation demonstrated that AMF was a noncompetitive inhibitor of UGT1A1 mediated NCHN-O-glucuronidation but functioned as a competitive inhibitor of UGT1A1 mediated 4-MU-O-glucuronidation. In addition, AMF was a competitive inhibitor of UGT1A4 mediated TFP-N-glucuronidation in both UGT1A4 and human liver microsomes, while functioned as a competitive inhibitor of UGT1A9 mediated propofol or 4-MU-O-glucuronidation. These findings demonstrated that AMF was a strong and broad-spectrum natural inhibitor of most human UGTs, which might bring potential risks of herb-drug interactions (HDIs) via UGT inhibition. Additionally, this study provided novel insights into the underlying mechanism of AMF-associated toxicity from the perspective of UGT inhibition.

Dihydrochalcones and Diterpenoids from Pteris ensiformis and Their Bioactivities.

Two new dihydrochalcone enantiomers (+)-1 and (-)-1, along with eight known compounds 3-10, were obtained from Pteris ensiformis. The planar structures were determined on the basis of extensive 1D and 2DNMR and HRESIMS. The resolution of (+)-1 and (-)-1 was achieved by chiral HPLC analysis. The absolute configurations of (+)-1 and (-)-1 were established by the bulkiness rule using Rh2(O2CCF3)4-induced circular dichroism (ICD) method. Compounds (+)-1, (-)-1, 8, 9 and 10 exhibited the inhibitory assay of NO production in mouse macrophages stimulated by LPS, with IC50 values of 2.0, 2.5, 8.0, 9.5 and 5.6 µM, respectively. Otherwise, compound 10 showed moderate cytotoxic activity against HCT-116, HepG-2 and BGC-823 cell lines with IC50 values of 3.0, 10.5 and 6.3 µM, respectively.

[Chemical constituents from Pteris multifida and cytotoxic activity].

The materials were extracted by 95% ethanol, and the extracting solution was isolated by kinds of chromatographic columns including polyamide, MCI, preparative MPLC, and preparative HPLC. Eight diterpenes and two sesquiterpenes were isolated from the plant. On analysis of ESI-MS and NMR spectroscopic data, the structures were established as ent-3ß-hydroxy-kaur-16-en-19-al (1), 4-epi-kaurenic acid (2), mitrekaurenone (3), 7ß,16α,17-trihydroxy-ent-kauran-19-oic acid (4), crotonkinin E (5), crotonkinin F (6), pterisolic acid A (7), pterisolic acid C (8), (2R)-pterosin P (9), and dehydropterosin B (10). Compounds 1-6 were obtained from Pteris for the first time, and compounds 7-10 were obtained from P. ensiformis for the first time. Compounds 5-8 showed moderate activity against HCT-116, HepG2 and BGC-823 cell lines, separately.

[Bioactive quinolizidine alkaloids from Sophora tonkinensis].

Twelve quinolizidine alkaloids were isolated from Sophora tonkinensis by means of silica gel, preparative MPLC, and preparative HPLC. On analysis of NMR spectroscopic data, their structures were established as 3-(4-hydroxyphenyl)-4-(3-methoxy-4-hydroxyphenyl)-3,4-dehydroquinolizidine(1), lanatine A(2), cermizines C(3), senepodines G(4), senepodines H(5), jussiaeiines A(6), jussiaeiines B(7),(+)-5α-hydroxyoxysophocarpine(8),(-)-12ß-hydroxyoxysophocarpine(9),(-)-clathrotropine(10),(-)-cytisine(11), and (-)-N-methylcytisine(12), respectively. Compounds 1-7 were first isolated from Sophora L. plant. In the in vitro assays,the isolated compounds 1, 3, 6-10 exhibited potent activity against CVB3 with IC50 of 6.40, 3.25, 4.66, 3.21, 0.12, 0.23 and 1.60, and with selective index values(SI=TC50/IC50)of 12.0, 5.6, 13.0, 15.1, 50.1, 26.2, and 23.6, respectively. Compounds 1, 3, and 7 exhibited activity against staphylococcus aureus(ATCC 29213)with MICvalues of 8.0, 3.5, 6.0 g•L⁻¹, respectively. Compounds 1, 3, 7, and 12 exhibited activity against staphylococcus aureus(ATCC 33591)with MIC values of 18.0, 7.5, 8.0, 12.0 g•L⁻¹, respectively. Compounds 2, 6, 7 exhibited activity against Escherichia coli(ATCC 25922) with MIC values of 1.0, 3.2, 0.8 g•L⁻¹.

[Qualitative Determination of Organic Vapour Using Violet and Visible Spectrum].

Vapours of organic matters were determined qualitatively employed with ultraviolet-visible absorption spectroscopy. Vapours of organic matters were detected using ultraviolet-visible spectrophotometer employing polyethylene film as medium, the ultraviolet and visible absorption spectra of vegetable oil vapours of soybean oil, sunflower seed oil, peanut oil, rapeseed oil, sesame oil, cotton seed oil, tung tree seed oil, and organic compound vapours of acetone, ethyl acetate, 95% ethanol, glacial acetic acid were obtained. Experimental results showed that spectra of the vegetable oil vapour and the organic compound vapour could be obtained commendably, since ultra violet and visible spectrum of polyethylene film could be deducted by spectrograph zero setting. Different kinds of vegetable oils could been distinguished commendably in the spectra since the λ(max), λ(min), number of absorption peak, position, inflection point in the ultra violet and visible spectra obtained from the vapours of the vegetable oils were all inconsistent, and the vapours of organic compounds were also determined perfectly. The method had a good reproducibility, the ultraviolet and visible absorption spectra of the vapours of sunflower seed oil in 10 times determination were absolutely the same. The experimental result indicated that polyethylene film as a kind of medium could be used for qualitative analysis of ultraviolet and visible absorption spectroscopy. The method for determination of the vapours of the vegetable oils and organic compounds had the peculiarities of fast speed analysis, well reproducibility, accuracy and reliability and low cost, and so on. Ultraviolet and visible absorption spectrum of organic vapour could provide feature information of material vapour and structural information of organic compound, and provide a novel test method for identifying vapour of compound and organic matter.

[A study of traditional Chinese medicine syndromes correlated to neurologic function or to coagulation function in patients with acute cerebral infarction].

OBJECTIVE: To investigate the correlations between traditional Chinese medicine (TCM) syndrome elements and neurologic function and between them and coagulation function in patients with acute cerebral infarction (ACI). METHODS: Two hundred and twenty-three patients with ACI were enrolled. The syndromes of this disease were scored according to Stroke Diagnostic Criteria for Differentiation of Syndromes. Neurologic function deficit score (NDS) was scored according to stroke scale of the National Institutes of Health (NIHSS). The prothrombin time (PT), activated partial thromboplastin time (APTT) and fibrinogen (FIB) contents were detected. The correlations between TCM syndrome elements and NDS and between them and coagulation function were investigated. RESULTS: Two hundred and twenty-three patients with ACI were divided into six syndromes: wind syndrome (n=147, 65.92%), fire syndrome ( n=100, 44.84%), tan syndrome (n=123, 55.16%), blood stasis syndrome (n=78, 34.98%), deficiency of qi syndrome (n=31, 13.90%), and yin deficiency causing hyperactivity of yang syndrome (n=25, 11.21%). The wind, tan and fire syndromes were the main syndrome elements related to ACI. The scores of wind, fire, tan and deficiency of qi syndromes were positively related to NDS (r1=0.207, P1=0.002; r2=0.284, P2=0.000; r3=0.245, P3=0.000; r4=0.152, P4=0.023). The score of deficiency of qi syndrome was negatively correlated with PT (r=-0.170, P=0.011); and the scores of tan, blood stasis, and deficiency of qi syndromes were negatively correlated with APTT (r1=-0.182, P1=0.006; r2=-0.148, P2=0.027; r3=-0.211, P3=0.001).Other syndromes were not correlated to NDS or coagulation factors. CONCLUSION: The neurologic function deficiency due to ACI is more likely influenced by wind, tan, and fire syndromes; deficiency of qi syndrome also has some effects. The syndromes of tan, blood stasis, and deficiency of qi are closely correlated with coagulation function, and their scores may reflect the clotting function in patients with ACI.

[Effect of TCM treatment for dissolving phlegm and dispelling stasis on plasma protein and thrombomodulin in patients with acute cerebral infarction].

OBJECTIVE: To observe the clinical effect of TCM treatment for dissolving phlegm and dispelling stasis (DP-DS) on acute cerebral infarction (ACI) and its influences on plasma protein C and S and soluble thrombomodulin (TM). METHODS: One hundred and twenty-two patients were randomly assigned to two groups, the treated group (62 cases) and the control group (60 cases). They were all treated with the conventional treatment, and DP-DS treatment was given to the treated group additionally. The treatment course was 14 days. The changes in scores of TCM syndrome and neurofunction impairment (NIHSS), levels of plasma protein C (PC), protein S (PS) and TM before and after treatment in the two groups were observed. RESULTS: The total effective rate of TCM syndrome in the treated group was higher than that in the control group (P= 0.00). After treatment, NIHSS in the two groups was significantly different (P=0.00), and the score in the treated group was superior to that in the control group (P = 0.00). NIHSS score and levels of PC and PS were improved in both groups (P = 0.024, 0.028), and the improvement of PC in the treated group was superior to that in the control group respectively (P = 0.049). But no significant change of TM was shown after treatment. CONCLUSION: TCM DP-DS treatment shows significant effect in improving TCM syndrome and neurofunction impairment of the patients with acute cerebral infarction, and raise the levels of PC and PS.