L-Trp and L-Leu-OEt derivatives of the monascus pigment exert high anti-obesity effects on mice.

High-fat diets (HFDs) supplemented with the L-Trp and L-Leu-OEt derivatives of the monascus pigment were fed to mice. Compared to the HFD group, the average body weight gain of the four HFD-pigment groups was decreased by 13.6-50.9%, and the intra-peritoneal adipose tissues weight was reduced by 16.7-30.5%. The derivatives also reduced the respective serum total cholesterol and triglyceride levels of the mice by 9.7-14.4% and 12.5-17.2%. The L-Trp derivative greatly increased the HDL-cholesterol level by 64.8-66.4% and the HTR value by 73.8-81.7%. The L-Leu-OEt and L-Trp derivatives decreased the total cholesterol level in the mice liver by 9.7-24.2% and 36.2-39.9%, respectively. Reductions in the triglyceride level were 21.5-22.4% for the L-Leu-OEt derivative and 17.9-18.8% for the L-Trp derivative. The L-Leu-OEt derivative exhibited higher in vitro inhibitory activities against HMG-CoA reductase and lipoprotein lipase than the L-Trp derivative. An in vivo test with mice showed the L-Trp derivative to have higher anti-obesity effects than the L-Leu-OEt derivative.

Development of inhibitors against lipase and alpha-glucosidase from derivatives of monascus pigment.

New derivatives of monascus pigment were produced during Monascus fermentation by the addition of unnatural amino acids, and the inhibitory activities of the derivatives against diet-related lipase and alpha-glucosidase were tested. Derivatives with penicillamine (H-Pen), cyclohexylalanine (H-Cha), butylglycine (L-t-Bg), and norleucine (H-Nle) showed relatively high inhibitory activities against lipase. The H-Pen derivative exhibited the highest inhibitory activity, with an IC(50) (50% inhibition) value of 24.0 microM. The four derivatives all showed noncompetitive inhibition patterns against lipase. The inhibition constant (K(i)) of the H-Pen derivative was estimated to be 20.7 microM. The H-Pen derivative also exhibited a relatively high inhibitory activity against alpha-glucosidase, with an IC(50) value of 50.9 microM. The inhibition pattern of the H-Pen derivative against alpha-glucosidase appeared to be of a mixed type. The inhibition constants K(i) and were estimated to be 25.9, and 98.9 microM, respectively.

Evaluation of enzyme-linked immunosorbent assay in serological diagnosis of human neurocysticercosis using paired samples of serum and cerebrospinal fluid.

The applicability of micro-ELISA was evaluatd in human neuro-cysticercosis using paired samples of serum and CSF. A total of 355 cases who were mostly neurologic patients was subjected. Cystic fluid of C. cellulosae was used as antigen in protein concentration of 2.5 micro-g/ml. Serum was diluted to 1:100 and CSF was undiluted in the assay for the specific IgG antibody level. The differential criterion of the positive reaction was the abs. of 0.18 in both samples. The results were summarized as follows: The overall sensitivity of the micro-ELISA in 71 confirmed neurocysticercosis was 90.1%; the sensitivity by serum was 77.5% and that by CSF was 83.1%. CSF was a more sensitive and valuable material. Most of the false negative cases of neuro-cysticercosis showed far lower level of abs. rather than marginal. The overall specificity of the micro-ELISA in 52 confirmed other neurologic diseases was 88.5%; the specificities by serum and by CSF were 94.2% respectively. Cases of other neurologic diseases did not show false positive reactions in both samples. When serum was assayed, taeniasis(2/18), sparganosis(2/20), paragonimiasis(1/56), clonorchiasis(1/15) and fascioliasis(1/1) cases showed cross reactions. When CSF was assayed, 2 of 10 neuro-sparganosis showed cross reactions while none of 9 neuro-paragonimiasis showed it. Out of 71 confirmed neuro-cysticercosis cases, 6 and 11 showed cross reactions by serum and CSF to crude extract antigen of sparganum; but no case did show it to crude extract antigen of Paragonimus westermani. Ventricular CSF showed low or negative levels of IgG antibody than lumbar CSF unless the lesion was at the lateral ventricle itself. Out of 4 racemose cysticercosis cases, 3 showed positive reaction in serum while all of 3 examined CSF were positive. The above results indicated that the serological test for detecting the specific IgG antibody by micro-ELISA using paired samples of serum and CSF was very helpful for clinical differentiation of neuro-cysticercosis from neurologic diseases of other causes.