Response of different benthic biotic indices to eutrophication and sediment heavy metal pollution, in fujian coastal water, East China sea.

The types and intensity of anthropogenic pressure in the same sea area may differ spatially and may change as time passes, but response of benthic biotic indices to different pressure is different, which makes it unreasonable to use the same benthic biotic indices in a large sea area. We provided a new way of thinking as to selecting benthic biotic indices according to pressure type. The study took six bays under eutrophication and sediment heavy metal pollution to different levels in Fujian coastal water, East China sea, as examples, analysed the response of five benthic biotic indices, namely AZTI marine biotic index (AMBI), multivariate AMBI (M-AMBI), Shannon-Wiener diversity index (H'), benthic opportunistic polychaetes amphipods (BOPA) and benthic polychaetes amphipods (BPA), to eutrophication factors and sediment heavy metal pollution factors firstly. The result indicated that AMBI well responded to dissolved inorganic nitrogen (DIN) and dissolved inorganic phosphorus (DIP); M-AMBI responded soundly in the range of DIN >0.131 mg L-1 and DIP >0.022 mg L-1 and responded universally to heavy metals; H' responded to only Hg and Cd; BOPA has response to eutrophication condition of DIN >0.242 mg L-1; BPA had response to DIN, Cu and As. Then, suitable indices were selected based on the four pressure scenarios in the study area. AMBI was selected in no pressure scenario; M-AMBI was chosen under only eutrophication pressure and under dual pressure; H' was preferred in only heavy metal pressure scenario (mainly Hg pollution). At last, the density plot of the distribution of the selected indices in the evaluation grades under different pressure scenarios proved the proposal of selecting benthic biotic indices according to pressure types feasible. This study can offer some new insights into rapidly choosing indices to evaluate the coastal benthic ecological quality status.

8-O-ß-D-Glucopyranosyl-2-methylchromone, a new chromone glycoside from the Tibetan medicine plant of Swertia punicea Hemsl.

A new chromone glycoside, 8-O-ß-D-Glucopyranosyl-2-methylchromone (1), together with eight known compounds (2-9) were isolated from the Tibetan medicine plant of Swertia punicea. All compounds of this plant were reported for the first time. The structures of these metabolites were elucidated by analysis of their HR-ESI-MS, 1D and 2D NMR spectroscopic data and comparison with data reported in the literature. In vitro test, all compounds were evaluated for their anti-inflammatory activity through the determination of nitric oxide production. Compounds 1-2 were evaluated for cytotoxic activities against three human cancer cell lines (HeLa, MDA-MB-231 and A375) by 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyl tetrazolium bromide (MTT) method. Furthermore, the chemotaxonomic significance of these compounds has also been described.

Structure Elucidation of Two New Norlignans from Anemone vitifolia and Their Anti-Inflammatory Activities.

Two new norlignans together with two known phenylpropanoids were isolated from the whole herb of Anemone vitifolia. All compounds were reported from this plant for the first time. The structures of these compounds were identified by comprehensive HR-ESI-MS, 1D and 2D NMR spectroscopic data analysis and comparison with literature data. Additionally, bioactivity study results showed that two new compounds have potential anti-inflammatory activity. The plausible biosynthetic pathway for these compounds were also speculated in this article.

Two new xanthone glycosides from Swertia punicea Hemsl. and their anti-inflammatory activity.

Two new xanthone glycosides (1-2), together with seven known analogues (3-9), were isolated from whole herb of Swertia punicea. The structures of these metabolites were established on the basis of detailed spectroscopic analysis and comparison with data reported in the literature. In an in vitro test, all isolates were evaluated for their anti-inflammatory activity. The results revealed that all of them showed significant anti-inflammatory activity with IC50 values ranging from 1.237 to 3.319 mM. Compounds 3, 4, and 5 (IC50 values in the range 1.237-1.987 mM) displayed more potent anti-inflammatory activity than the positive control, indomethacin (IC50 value of 2.004 mM).

Vasodilatory effect and structural-activity relationship of a group of iridoid glucosides from Phlomis likiangensis.

As a folk medicine, Phlomis likiangensis is traditionally used in China to activate collaterals and protect cardiovascular system. We hypothesized that the beneficial effects of Phlomis likiangensis may be related to vasodilatation. In the present study, twelve known iridoid glucosides (1-12) were isolated from Phlomis likiangensis. The vasodilatory effects and the underlying mechanisms of the main components (iridoid glucosides) of Phlomis likiangensis on rat aortic rings were investigated. The result showed that iridoid glucosides significantly increased the vasodilatation in rat aortic rings, which was abolished by removing the endothelium of the vessels or by eliminating the generation of nitric oxide. Finally, the structure-activity relationship of compounds 1-12 was also speculated. Our findings provide the first evidence that the iridoid glucosides of Phlomis likiangensis may be the pharmacodynamic basis for its traditional efficacy.

"Yellow-dragon Wonderful-seed Formula" for hyperuricemia in gout patients with dampness-heat pouring downward pattern: a pilot randomized controlled trial.

BACKGROUND: In Traditional Chinese Medicine (TCM) theories, the typical clinical manifestations of gout are attributed to the "dampness-heat pouring downward." Therefore, TCM practitioners always consider prescribing the formulae which are believed to clear heat and drain dampness for the management of gout. This clinical trial aims: (1) to determine the hypouricemic effect of "Yellow-dragon Wonderful-seed Formula" (YWF) decoction in gout patients with dampness-heat pouring downward pattern and (2) to determine if gypsum could provide additional significant benefits to YWF. METHODS: A total of 72 hyperuricemic individuals with gout and dampness-heat pouring downward pattern were included with 62 of them completing the trial. Participants were randomly assigned to the YWF group, the YWF + gypsum group, or the allopurinol group. YWF and YWF + gypsum decoctions were orally administered for four weeks. Allopurinol was also orally administered for four weeks as the active control. Serum uric acid (sUA) level was the primary outcome measure. Urine urate level, scores on the SF-36 scale, erythrocyte sedimentation rate (ESR), X ray film, and C reactive protein (CRP) level were the secondary outcome measures. RESULTS: Compared with the values at week 0, YWF and YWF + gypsum did not significantly decrease the sUA level at each weekend reading. YWF, YWF + gypsum, and allopurinol decreased the urine urate levels and there were significant differences between the YWF group and the YWF + gypsum group. All the changes in the eight structures of SF-36 during the intervention period were not significantly different among the three groups and there was no significant difference in the CRP level among the three groups at each weekend reading. CONCLUSIONS: YWM, which modified on the basis of Two Wonderful Herbs Powder (2WHP), does not show significant hypouricemic effect. There is a possibility that Gypsum Fibrosum may provide additional effects to YWF in decreasing the urine urate levels but cannot add benefits to YWF in other outcome measures. TRIAL REGISTRATION: Chinese Clinical Trial Registry, ChiCTR-TRC-12001933 . Registered on 10 February 2012.

Three new xanthones from Swertia bimaculata and their anti-5α-reductase activity.

Three new xanthones (1-3), together with five known ones (4-8), were isolated from whole herb of Swertia bimaculata. Their structures were established on the basis of detailed spectroscopic analysis (1D- and 2D-NMR, HRESIMS, UV, and IR) and comparison with data reported in the literature. New isolates were evaluated for their anti-5α-reductase activity. The results revealed that all new compounds showed weak activity with reductase inhibitions of 40.5 ± 2.8, 38.6 ± 2.5, and 48.9 ± 3.0%, respectively.

Bioactive Enmein-Type ent-Kaurane Diterpenoids from Isodon phyllostachys.

Thirty-two enmein-type ent-kaurane diterpenoids, including 13 new compounds, were isolated from the aerial parts of Isodon phyllostachys. Compounds 1 and 2 are the first examples of 3,20:6,20-diepoxyenmein-type ent-kauranoids, and the structures of these new compounds were established mainly by analyzing NMR and HREIMS data. The absolute configurations of 1 and 8 and the relative configuration of 9 were determined using single-crystal X-ray diffraction. Compounds 11, 15, 20, and 21 were active against five human cancer cell lines (HL-60, SMMC-7721, A-549, MCF-7, and SW-480), with IC50 values ranging from 1.2 to 5.0 µM. Compounds 3, 11, 15, 17, 20, 21, 25, and 29 strongly inhibited NO production in LPS-stimulated RAW264.7 cells, with IC50 values ranging from 0.74 to 4.93 µM.

Six new cytotoxic and anti-inflammatory 11, 20-epoxy-ent-kaurane diterpenoids from Isodon wikstroemioides.

The present study was designed to determine the chemical constituents of EtOAc extracts of the aerial parts of Isodon wikstroemioides. Compounds 1-8 were isolated and purified by normal-phase silica gel and reversed-phase C18silica gel column chromatography and HPLC. Their structures were elucidated by extensive spectroscopic methods. Most of them were evaluated for their in vitro cytotoxicity against human cancer HL-60, SMMC-7721, A-549, MCF-7, and SW-480 cells and their inhibitory activity against nitric oxide (NO) production in LPS-activated RAW264.7 macrophages. Among the eight 11, 20-epoxy-ent-kauranoids isolated, compounds 1-6 (isowikstroemins H-M) were new diterpenoids. Compounds 1, 3, and 7 exhibited significant cytotoxicity with IC50 values ranging from (0.84 ± 0.02) to (4.09 ± 0.34) µmol · L(-1), while compounds 4 and 5 showed selective cytotoxicity. In addition, compounds 1, 3, 4, and 7 exhibited inhibitory activity against nitric oxide (NO) production in LPS-activated RAW264.7 macrophages. These results provide a basis for future development of these compounds as anti-cancer and anti-inflammatory agents.

Two New 18-Norschiartane-type Schinortriterpenoids from Schisandra lancifolia.

Two new 18-norschiartane-type schinortriterpenoids, namely wuwezidilactones Q (1) and R (2) were isolated from the stems of Schisandra lancifolia. Their structures were determined on the basis of extensive spectroscopic analysis. The absolute configurations of the new compounds were further determined by ROESY and an empirical comparison of their experimental ECD spectra with literature.

Cytotoxic and anti-inflammatory ent-kaurane diterpenoids from Isodon wikstroemioides.

Seven new ent-kaurane diterpenoids, isowikstroemins A-G (1-7), were isolated from EtOAc extracts of the aerial parts of Isodon wikstroemioides. Their structures were elucidated by extensive spectroscopic analysis. The isolates were evaluated for their cytotoxicity against five human tumor cell lines, and compounds 1-4 exhibited significant activity with IC50 values ranging from 0.9 to 7.0 µM. In addition, compounds 1, 2, 3, 4, and 7 exhibited inhibitory activity against nitric oxide (NO) production in LPS-activated RAW264.7 macrophages.

Cytotoxic ent-kaurane diterpenoids from Isodon wikstroemioides.

Phytochemical investigation of EtOAc extracts of the aerial parts of Isodon wikstroemioides afforded 18 new ent-kaurane diterpenoids (wikstroemioidins E-V, 1-18), along with 17 known analogues (19-35). The absolute configurations of 1 and 16 were confirmed by single-crystal X-ray diffraction analysis. The isolates were screened against five human tumor cell lines; compounds 3, 4, 9, 11-13, 23, 25-28, and 33 exhibited significant cytotoxic activity against all five, with IC50 values ranging from 0.4 to 5.1 µM. In addition, 17 of the isolates strongly inhibited nitric oxide production in LPS-activated RAW264.7 macrophages.

Diterpenoids from Isodon sculponeatus.

Phytochemical investigation of the aerial parts of Isodon sculponeatus afforded six new 7,20-epoxy-ent-kauranoids, sculponins U-Z (1-6), and 11 known diterpenoids (7-17). The structures of these new compounds were elucidated primarily by means of extensive spectroscopic analysis, and the absolute configuration of 1 was determined by single crystal X-ray diffraction. Compound 5 exhibited weak cytotoxic activity against HL-60, SMMC-7721, MCF-7, and SW-480 cell lines, and it also inhibited NO production in LPS-stimulated RAW264.7 cells, with IC50 value of 13.8 µM.

Laxiflorolides A and B, epimeric bishomoditerpene lactones from Isodon eriocalyx.

Laxiflorolides A (1) and B (2), two unprecedented epimeric bishomoditerpene lactones with a unique C(22) framework, along with laxiflorins P-R (3-5), maoecrystal P (6), maoecrystal C (7), and eriocalyxin B (8), were isolated from the leaves of I. eriocalyx var. laxiflora. The structures of 1 and 2, including the absolute configurations, were determined by spectroscopic methods and single-crystal X-ray diffraction analysis. All of the compounds isolated were evaluated for their cytotoxicity against five tumor cell lines. Compounds 3, 6, and 8 showed remarkable cytotoxic activity against certain cell lines compared with the positive control.

[Estimation of river nutrients thresholds based on benthic macroinvertebrate assemblages: a case study in the upper reaches of Xitiao Stream in Zhejiang, China].

Water eutrophication is a global problem, and one of the major environmental problems in China. At present, its studies in China are mainly focused on lakes and reservoirs, whereas a few on rivers. Based on the stress-response of benthic macroinvertebrate assemblages to water nutrients, we used the nonparametric deviance reduction (change point analysis) to compute the breakpoints of nutrients concentrations, in the upper reaches of Xitiao Stream in Zhejiang. The results indicated that the breakpoints of total nitrogen (TN) and total phosphors (TP) were 1.409 mg x L(-1) and 0.033-0.035 mg x L(-1), respectively. The TN and TP concentrations at reference sites were lower, while those at urban sewage- polluted sites were higher than the thresholds. In latter case, a serious degradation of benthic macroinvertebrates assemblages could be induced. To establish water nutrients criteria with relation to aquatic organisms would make the biological monitoring play a full role in water management, and provide scientific data to estimate the total maximum daily load (TMDL) of TN and TP in water body.

Study on modified shengmai yin injection for prevention and treatment of brain impairment in endotoxin shock rats.

OBJECTIVE: To examine the effects of modified Shenmai Yin on invigorating vital energy, promoting blood flow, and protection against neural impairment in an endotoxin-induced shock rat model. METHODS: Ninety-six SD rats were randomly divided into four groups: sham operation (saline 20 ml/kg), shock model (lipopolysaccharide, LPS, 8 mg/kg), Reformed Shengmai Yin (Pulse-activating Decoction) (LPS 8 mg/kg + reformed Shengmai Yin Injection 10 ml/kg), and dexamethasone (LPS 8 mg/kg + dexamethasone 5 mg/kg) groups. Each group was subdivided into 1 h, 2 h, 3 h, and 6 h time points for observation. The carotid artery was separated and connected with a biological functional system to monitor mean arterial pressure (MAP). Brain water levels, malonaldehyde (MDA) content, and superoxide dismutase (SOD) activity were also determined. RESULTS: In the shock model group, MAP was progressively decreased after injection of LPS, brain water and MDA contents were increased, brain SOD activity was decreased, and capillary vessel edema in brain tissue was also observed. All these parameters were improved significantly in both treatment groups, although the effects were more marked with Shengmai Yin than with dexamethasone. CONCLUSION: Modified Shengmai Yin exhibits strong anti-shock and neuroprotective effects against Endotoxin-induced shock.

[Clinical effect of prunrllae oral solution in treating hyperthyrea].

OBJECTIVE: To observe the clinical effects of prunrllae oral solution in treating hyperthyrea. METHOD: 56 cases with hyperthyrea were randomized into two groups; group A1 was treated by classic method, B1 was treated by classic method combined with prunrllae oral solution. The size, vessel caliber of thyroidea, volume of blood flow and blood flow rate pre-and post-treatment were measured by color supersonic, meanwhile, 20 normal thyroidea were measured as control group. RESULT: The size and vessel caliber of thyroidea of the two groups pre-treatment were obviously bigger than those of the control group, the volume of blood flow and blood flow rate were obviously slower than those of the control group (P < 0.001), the sizes of thyroidea of the two groups became smaller, especially the group B1 was more obvious, and there was no significant difference in the size of thyroidea between group B1 and control group. CONCLUSION: It is indicated that combined treatment of traditional Chinese medicine (prunrllae oral solution) and western medicine is superior to western medicine in treating hyperthyrea.

[Clinical effect of Prunellae Oral Liquid on goiter with different thyroid function].

OBJECTIVE: To observe the clinical effects of Prunellae Oral Liquid (POL) on the size of thyroid with different states of thyroid function in patients of goiter. METHODS: Fifty-six patients with hyperthyroidism, 24 with hypothyroidism and 18 with simple goiter were randomized into two groups. Group A treated by classical therapy, Group B by POL based on classical therapy. Size of thyroid of patients before and after treatment was measured by color ultrasonic Doppler and compared with the data obtained from 20 healthy subjects as control. RESULTS: Size of thyroid in all patients before treatment were obviously larger than that of normal control (P<0.01), but it reduced after treatment in both groups, especially in group B, in which it differed insignificantly to that in the normal control (P > 0.05). CONCLUSION: Combined treatment of Chinese medicine (using POL) and Western medicine is superior to Western medicine alone in treating goiter with different states of thyroid function.

[Studies on chemical constituents from leaves of Securinega suffruticosa].

OBJECTIVE: To investigate the chemical constituents of Securinega suffruticosa. METHOD: It was isolated and purified by silica gel chromatography. Their structures were elucidated by means of spectral analysis. RESULT: Four compounds were isolated and identified as ent-phyllanthidine (1), virosecurinine (2), 14,15-dihydrovirosecurinine (3) and viroallosecurinine (4). CONCLUSION: All of four compounds were isolated from S. suffruticosa for the first time and were the enantiomers isolated from this plant before.