Evaluation of anti-inflammatory activity of compounds isolated from the rhizome of Ophiopogon japonicas.

BACKGROUND: Ophiopogon japonicas (L.f) Ker-Gawl has been used as a traditional Chinese medicine to cure acute and chronic inflammation and cardiovascular diseases including thrombotic diseases for thousands of years. Previous phytochemical studies showed that O. japonicus contained compounds with anti-inflammatory activity. The aim of this study was to identify and isolate compounds with anti-inflammatory activity from the rhizome of O. japonicas. METHODS: Compounds were isolated by various column chromatography and their structures were identified in terms of nuclear magnetic resonance spectrum (NMR) and mass spectrum (MS). To measure the anti-inflammatory effects of thirteen compounds in LPS-induced RAW 264.7 macrophage cells, we used the following methods: cell viability assay, nitric oxide assay, enzyme-linked immunosorbent assay, quantitative real-time PCR analysis and western blotting analysis. RESULTS: One new and twelve known compounds (mainly homoisoflavonoids) were extracted from O. japonicas, in which 4'-O-Demethylophiopogonanone E (10) was considered as a new compound, additionally, compounds 4-O-(2-Hydroxy-1- hydroxymethylethyl)-dihydroconiferyl alcohol (2) and 5,7-dihydroxy-6-methyl-3-(2', 4'-dihydroxybenzyl) chroman-4-one (12) were isolated from the rhizome of O. japonicas for the first time. The isolated compounds Oleic acid (3), Palmitic acid (4), desmethylisoophiopogonone B [5,7-dihydroxy-3-(4'-hydroxybenzyl)-8- methyl- chromone] (5), 5,7-dihydroxy-6-methyl-3-(4'-hydroxybenzyl) chromone (7) and 10 significantly suppressed the production of NO in LPS-induced RAW 264.7 cells. Especially compound 10 showed the strongest effect against the production of the pro-inflammatory cytokine IL-1ß and IL-6 with the IC50 value of 32.5 ± 3.5 µg/mL and 13.4 ± 2.3 µg/mL, respectively. Further analysis elucidated that the anti-inflammatory activity of compound 10 might be exerted through inhibiting the phosphorylation of ERK1/2 and JNK in MAPK signaling pathways to decrease NO and pro-inflammatory cytokines production. CONCLUSIONS: Our results indicated that 4'-O-Demethylophiopogonanone E can be considered as a potential source of therapeutic medicine for inflammatory diseases.

Protective effects of modified linggui zhugan decoction combined with short-term very low calorie diets on cardiovascular risk factors in obese patients with impaired glucose tolerance.

OBJECTIVE: To observe the protective effects of modified Linggui Zhugan decoction combined with short-term very low calorie diets (VLCDs) on cardiovascular risk factors in obese patients with impaired glucose tolerance (IGT). METHODS: Eighty-five obese patients with IGT of spleen hypofunction and dampness accumulation type were randomly divided into treated group (n=45)and control group (n=40). The treated group was given Linggui Zhugan decoction combined short-term VLCDs. The control group was given basic weight-reduction treatment. The total course was 6 months. Changes of fasting plasma glucose (FPG), 2-hour postprandial blood glucose (2hPG), glycosylated hemoglobin (HbA1c), fasting insulin (FINS), lipid metabolism, blood pressure, body mass index (BMI) and waist circumference (WC) were observed, and the outcomes were reviewed after the treatment. RESULTS: Compared with the control group, the levels of FPG, 2 hPG, HbA1c, FINS, HOMA-IR decreased significantly (P < 0.05), and the indexes of total cholesterol (TC), triglyceride (TG), low-density lipoprotein (LDL), systolic blood pressure (SBP), diastolic blood pressure (DBP), BMI and WC were improved significantly (P < 0.05) in the treated group. The transformation rate of normal glucose tolerance (NGT) was higher in treatment group than control group (P < 0.01). No severe adverse reaction was found in the therapeutic course. CONCLUSION: The modified Linggui Zhugan decoction combined with short-term VLCDs has good protective effects on cardiovascular risk factors as a treatment intervention for IGT with obesity, as it could improve glycometabolism, significantly decrease the levels of blood pressure, blood lipids, BMI, WC and effectively cut-off and reverse the development of diabetes mellitus.

Effects of the modified linggui zhugan decoction (see text) combined with short-term very low calorie diets on glycemic control in newly diagnosed type 2 diabetics.

OBJECTIVE: To evaluate the effects of the modified Linggui Zhugan Decoction (see text) combined with short-term very low calorie diets (VLCDs) on glycemic control in newly diagnosed type 2 diabetes mellitus (T2DM) patients. METHODS: A total of 20 subjects with newly diagnosed T2DM were treated with the modified Linggui Zhugan Decoction (one-month administration) combined with short-term VLCDs (5 days), and 3-months follow-up. A standard 75-g oral-glucose-tolerance test (OGTT) indexes fasting plasma glucose (FPG), post-prandial 0.5 h and 2 h plasma glucose (P0.5hPG, P2hPG), glycated hemoglobin A(1c) (GHbA(1c)), body weight, body mass index (BMI), insulin function, insulin resistance index, incidence of hypoglycemia, and the liver and renal functions were evaluated before and after treatment. Correlations of BMI with insulin function and insulin resistance were also assessed. RESULTS: After the treatment, the patients' plasma glucose decreased steadily, FPG decreased from 5.8 +/- 0.9 mmol/L at pre-treatment to 5.0 +/- 0.6 mmol/L at 3-months follow-up (P < 0.05), and P2hPG decreased from 11.7 +/- 3.8 mmol/L at pre-treatment to 6.9 +/- 0.9 mmol/L at 3-months follow-up (P < 0.01). The level of GHbA(1c) declined from (6.47 +/- 1.24)% at pre-treatment to (6.14 +/- 0.99)% at 3-months follow-up (P < 0.01). Body weight and BMI also declined significantly. Insulin resistance index was improved obviously and no event of hypoglycemia occurred. Part of the patients companied with fatty liver had a transient increase in hepatic transaminase during the treatment, but it turned to normal after the treatment. CONCLUSIONS: The modified Linggui Zhugan Decoction combined with short-term VLCDs can be safely implemented for steady glycemic control in newly diagnosed T2DM patients.

[Purification of complicated industrial organic waste gas by complex absorption].

Complicated industrial organic waste gas with the characteristics of low concentration,high wind volume containing inorganic dust and oil was employed the research object by complex absorption. Complex absorption mechanism, process flow, purification equipment and engineering application were studied. Three different surfactants were prepared for the composite absorbent to purify exhaust gas loaded with toluene and butyl acetate, respectively. Results show that the low surface tension of the composite absorbent can improve the removal efficiency of toluene and butyl acetate. With the advantages of the water film, swirl plate and fill absorption device, efficient absorption equipment was developed for the treatment of complicated industrial organic waste gas. It is with superiorities of simple structure, small size, anti-jam and high mass transfer. Based on absorption technology, waste gas treatment process integrated with heating stripping, burning and anaerobic and other processes, so that emissions of waste gas and absorption solution could meet the discharge standards. The technology has been put into practice, such as manufacturing and spraying enterprises.

Correlation of the cerebral microvascular blood flow with brain temperature and electro-acupuncture stimulation.

OBJECTIVE: To investigate the relationship between the temperature and the microvascular blood flow of the cerebral cortex, and the influence of electro-acupuncture (EA) on the cortical microcirculation. METHODS: High temperature spots on the anterior ectosylvian and low temperature spots on the posterior suprasylvian on the cortical surface of 20 cats were identified using cortical infrared thermography (CIT); the blood flow in the microcirculation on these spots was measured with laser-Doppler flowmetry. EA was given at Zusanli (ST 36) and changes in the blood flow in the cerebral cortex microcirculation were detected. RESULTS: 1) The mean temperatures on the high (34.83 +/- 0.24 degrees C) and low (32.28 +/- 0.27 degrees C) temperature spots were significantly different (P < 0.001); this was indicative of a temperature difference on the cortical surface; 2) The average blood flow in the microcirculation of the high (266.8 +/-19.2 PU) and low (140.8 +/- 9.9 PU) temperature spots was significantly different (P < 0.001). 3) On the cortical high temperature spots, the mean blood flow in the microcirculation significantly increased from 266.8 +/- 86.8 PU before EA, to 422.5 +/- 47.4 PU following 5 minutes of EA (58.35%; P < 0.01), and 431.8 +/- 52.8 PU 5 minutes after ceasing EA (61.84%; P < 0.01). 4) On the low temperature spots, there were no significant differences in blood flow following 5 minutes of EA (146.3 +/- 11.5 PU), and 5 minutes after ceasing EA (140.5 +/- 11.6 PU), when compared with that before acupuncture (140.8 +/- 9.9 PU; P > 0.9). CONCLUSION: The high temperature spots of the cortex are active functional regions of neurons with higher blood flow and a stronger response to EA. EA induces a significant increase in blood flow in the high temperature spots of the cortex.

Relationship between growth hormone (GH) pulses in the peripheral circulation and GH-releasing hormone and somatostatin profiles in the cerebrospinal fluid of goats.

Growth hormone (GH) is secreted in a pulsatile manner, but the underlying mechanisms of GH pulse generation remain to be resolved. In the present study, we investigated the relationship between GH pulses in the peripheral circulation and GH-releasing hormone (GHRH) and somatostatin (SRIF) profiles in the cerebrospinal fluid (CSF) of male goats. The effects of an intracerebroventricular (icv) injection of neuropeptide Y (NPY), galanin and ghrelin were also analyzed. Blood and CSF samples were collected every 15 min for 8 hr from the jugular vein and third ventricle, respectively. GH pulsatility in the goat was found to consist of distinct large pulses of 5 hr periodicity and small pulses of 1 hr periodicity. GHRH and SRIF in the CSF fluctuated in a pulsatile manner with 1 hr periodicity, and most of the descending phase of SRIF pulses were associated with the initiation of GH pulses. Icv injections of NPY, galanin and ghrelin stimulated GHRH release without affecting SRIF release. In addition, NPY suppressed, and galanin and ghrelin induced large GH pulses, although ghrelin was much more effective than galanin. These results suggest that an hourly fall in SRIF is involved in generating intrinsic circhoral rhythm of GH pulsatility. The mechanisms underlying the generation of large GH pulses of 5 hr periodicity remain unknown, while direct action of NPY and/or ghrelin on the pituitary might be involved.