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Biomedical subjects

Hui Ji

Publications and source records attributed to Hui Ji.

13 recordsLinked to original sources

Protective effects of sodium daidzein sulfonate on trabecular bone in ovariectomized rats.

The ovariectomized (OVX) rat, as an established animal model of human osteoporosis, was adopted in the present experiment to study the protective effects of sodium daidzein sulfonate (SDS) on trabecular bone. Six-month-old Sprague-Dawley rats were sham-operated or ovariectomized. Five days later, the OVX rats were randomly assigned to one of three experimental groups and treated for 90 days with vehicle, 17beta-estradiol (E(2)) or SDS. Compared with OVX rats, SDS administration (15 mg/kg) prevented OVX-induced decrease in lumbar vertebral and femoral bone mineral density (BMD), and significantly increased bone mechanical strength parameters, including ultimate stress and elastic modulus. In the OVX group, the structure of trabecular plate in the femoral head was absorbed and became progressively thinner or was removed completely, accompanied by enlargement of marrow cavities and amalgamation of two or more marrow cavities. Administration of SDS and E(2 )prevented the change of trabecular bone microarchitecture induced by OVX, increasing the trabecular bone area and trabecular thickness, while decreasing the trabecular separation. These results indicate that SDS administration prevents OVX-induced decrease in BMD and bone mechanical strength, and has a moderate protective effect on the microarchitecture of trabecular bone in aged Sprague-Dawley rats.

Amino Acids↗

Design and synthesis of furoxan-based nitric oxide-releasing glucocorticoid derivatives with potent anti-inflammatory activity and improved safety.

A series of furoxan-based nitric oxide-releasing glucocorticoid derivatives was synthesized. The pharmacological assays indicated that three compounds, including I(4), I(5), and I(6), had anti-inflammatory activity. Furthermore compared with the leading compound hydrocortisone the safety of I(6) was greatly improved. Due to releasing NO in vivo the side effects of glucocorticoids, including hypertension and osteoporosis, were effectively avoided.

Alkaline Phosphatase↗

Selective antagonism activity of alkaloids from bulbs Fritillariae at muscarinic receptors: functional studies.

15 alkaloids were isolated from five Fritillariae species and 6 derivatives were synthesized. Alkaloids having anticholinergic effect on guinea-pig tracheal smooth muscle were screened out and their mechanism was further studied on the cAMP formation in Chinese hamster ovary cells stably expressing human muscarinic M2 receptor (CHO-hM2 cells) and intracellular calcium ([Ca(2+)](i)) transient in Chinese hamster ovary cells stably expressing human muscarinic M3 receptor (CHO-hM3 cells). In normal Krebs-Henseleit (KH) solution, imperialine (15), 3beta-acetylimperialine (16) and sinpeinine A (17) concentration-dependently relaxed 1 microM carbachol-induced contraction of guinea-pig tracheal rings with EC(50) of 4.19, 1.71 and 4.67 microM, respectively. In Ca(2+)-free KH solution, 10 microM 3beta-acetylimperialine (16), imperialine (15) and sinpeinnine A (17) caused 97.42%, 5.45% and 6.55% inhibition, respectively, which indicated that the three components might inhibit muscarinic receptor in different mechanism. Results of muscarinic M2 receptor-inhibited cAMP formation in CHO-hM2 cells showed that imperialine (15) and sinpeinine A (17) could potently elevate the cAMP formation whereas 3beta-acetylimperialine (16) only had weak effect on antagonism of cAMP inhibition. Furthermore, the investigations of muscarinic M3 receptor-stimulated [Ca(2+)](i) transient in CHO-hM3 cells revealed that imperialine (15) and sinpeinine A (17) could not antagonize [Ca(2+)](i) transient, but 3beta-acetylimperialine (16) significantly inhibited [Ca(2+)](i) peak elevation with an IC(50) of 5.26 microM. The functional studies suggest that the mechanism of relaxant action of imperialine (15) and sinpeinine A (17) is due to their selective inhibitory effects on muscarinic M2 receptors and the mechanism of 3beta-acetylimperialine (16) originates from its selective muscarinic M3 receptors antagonism.

Alkaloids↗

Noise causes slant underestimation in stereo and motion.

This paper discusses a problem, which is inherent in the estimation of 3D shape (surface normals) from multiple views. Noise in the image signal causes bias, which may result in substantial errors in the parameter estimation. The bias predicts the underestimation of slant found in psychophysical and computational experiments. Specifically, we analyze the estimation of 3D shape from motion and stereo using orientation disparity. For the case of stereo, we show that bias predicts the anisotropy in the perception of horizontal and vertical slant. For the case of 3D motion we demonstrate the bias by means of a new illusory display. Finally, we discuss statistically optimal strategies for the problem and suggest possible avenues for visual systems to deal with the bias.

Form Perception↗

Metabolic effects of telmisartan in spontaneously hypertensive rats.

The favorable metabolic effects of telmisartan are supposedly related to the changes in carbohydrate and lipid metabolism driven by peroxisome proliferators-activated receptor-gamma (PPARgamma). The fatty acid translocase CD36 is one of the PPARgamma targets that mediate these actions. We studied the metabolic effects of telmisartan in the NIH-derived strain of spontaneously hypertensive rats (SHR/NIH), which harbors a deletion mutation in CD36, in comparison to the original SHRs (SHR/Izm), which express wild-type CD36. In SHR/Izm, administration of telmisartan was associated with significantly lower serum levels of free fatty acids (42%), triglycerides (29%), glucose (11%), insulin (31%), and lower hepatic triglyceride (17%) levels, as well as larger epididymal fat pads (1.19-fold) than in SHR/NIH. Additionally, insulin-stimulated glucose incorporation into epididymal fat tissues was significantly augmented in SHR/Izm (1.33-fold) compared with SHR/NIH. In the epididymal fat pads of SHR/Izm treated with telmisartan, CD36 mRNA transcript (1.55-fold) and protein expression (1.37-fold) were also significantly enhanced. However, after 4 weeks of treatment with telmisartan, in SHR/NIH only serum free fatty acid levels were slightly reduced (20%). Overall, these results showed marked discrepancies in the metabolic actions of telmisartan in SHR/Izm and SHR/NIH and further supported the involvement of CD36 in the actions of this drug, suggesting that this pharmacogenetic interaction may be of particular importance in CD36-deficient patients.

Angiotensin II Type 1 Receptor Blockers↗

Inhibitors of acetylcholine esterase in vitro--screening of steroidal alkaloids from Fritillaria species.

18 alkaloids were successfully isolated from five Fritillaria species and 5 derivatives were synthesized. Their effects on the bioactivity of human whole blood cholinesterase (ChE) were assessed. The results showed that N-demethylpuqietinone, hupeheninoside, ebeiedinone, yibeinoside A and chuanbeinone inhibited the bioactivity of human whole blood ChE at the concentration of 1.0 x 10 ( - 4) M, with the inhibitory effects of 55.5 +/- 2.7 %, 66.8 +/- 2.0 %, 69.0 +/- 1.7 %, 71.2 +/- 1.8 % and 70.7 +/- 3.3 %, respectively. The effects of the five alkaloids on human red blood cell (RBC) acetylcholinesterase (AChE) and human plasma butyrylcholinesterase (BChE) were further studied, and their IC (50) values for human RBC AChE were 6.4 +/- 0.003 microM, 16.9 +/- 0.018 microM, 5.7 +/- 0.004 microM, 6.5 +/- 0.013 microM and 7.7 +/- 0.001 microM, respectively, and the IC50 values for human plasma BChE were 12.5 +/- 0.026 microM, 2.1 +/- 0.005 microM, 5.2 +/- 0.002 microM, 7.3 +/- 0.005 microM and 0.7 +/- 0.001 microM, respectively. These data suggest, therefore, that N-demethylpuqietinone, hupeheninoside, ebeiedinone, yibeinoside A and chuanbeinone have both anti-RBC AChE and anti-plasma BChE activities, N-demethylpuqietinone is a selective inhibitor of AChE, whereas hupeheninoside and chuanbeinone are the selective inhibitors of BChE.

Alkaloids↗

A 3D shape constraint on video.

We propose to combine the information from multiple motion fields by enforcing a constraint on the surface normals (3D shape) of the scene in view. The fact that the shape vectors in the different views are related only by rotation can be formulated as a rank = 3 constraint. This constraint is implemented in an algorithm which solves 3D motion and structure estimation as a practical constrained minimization. Experiments demonstrate its usefulness as a tool in structure from motion providing very accurate estimates of 3D motion.

Algorithms↗

The effects of five alkaloids from Bulbus Fritillariae on the concentration of cAMP in HEK cells transfected with muscarinic M(2) receptor plasmid.

The aim of this study was to investigate the effects of five alkaloids, namely verticine, verticinone, imperialine, imperialine-3beta-D-glucoside, and puqietinone, purified from Bulbus Fritillariae and used as an antitussive drug in traditional Chinese medicine, on their antimuscarinic M(2) function and the cAMP level of HEK cells transfected with muscarinic M(2) receptor plasmid. By transfecting the HEK cells with the method of calcium phosphate co-precipitation and screening with G418, the cells stably expressing M(2) receptor were identified. The expression of M(2) receptor in HEK cells was confirmed by both RT-PCR and western blot. The cAMP level in the treated cells was analyzed with RIA method ((125)I-cAMP KIT). And the results suggested that the five alkaloids could significantly elevate the cAMP concentration in the HEK cells transfected with muscarinic M(2) receptor plasmid (p < 0.01).

Alkaloids↗

[Design, synthesis and antiasthmatic activities of NO-donating seratrodast derivatives].

AIM: To search for novel antiasthmatic agents. METHODS: Coupling seratrodast (SD), an antiasthmatic drug, with several different types of NO donors including oxatriazoles, N-hydroxyguanidines and furoxans; evaluating the antiasthmatic effects of coupled compounds by determining their inhibitory activity of guinea pig asthma induced by acetylcholine and histamine; and assessing NO releasing ability. RESULTS: Nine novel target compounds (I1-9) were synthesized, and their structures were established by IR, NMR, MS and elemental analysis. Preliminary pharmacological test showed that most of the compounds showed high antiasthmatic activities (the latent period of induced asthma was prolonged from 10 s (SD) to 26-62 s), among which 3 compounds (I4, I6, I7) were more potent than SD (P < 0.05, P < 0.01) and released more NO than others. The maximum concentrations (Cmax) of NO-release in vitro were 0.1878, 0.1393 and 0.2473 mg x L(-1), respectively. CONCLUSION: NO donating-SD derivatives are worthy to be futher investigated.

Acetylcholine↗

[Synthesis and anti-inflammatory activity of p-(methanesulfonyl) styrene-linked cyclic ketone derivatives].

AIM: To search for new compounds with strong anti-inflammatory activity and low gastrointestinal (GI) side effects. METHODS: A series of p-(methanesulfonyl) styrene-linked cyclic ketone derivatives were synthesized. Their anti-inflammatory activities against xylene-induced mice ear swelling and carrageenan-induced rat paw edema were evaluated, and their GI side effects in the rats were examined. RESULTS: Nine target compounds (ZA(1-9)) were obtained, and their structures were determined by IR, 1HNMR, MS and elemental analysis. Compared with controls diclofenac (DC) and rofecoxib (RC) , ZA(3, 5-9) showed no significant difference in anti-inflammatory activity against xylene-induced ear swelling in mice. ZA(3, 7, 8) showed potency comparable to DC and RC (P > 0.05) and ZA6 was more potent than DC and RC (P < 0.05) in the treatment of carrageenan-induced rat paw edema. ZA(3, 5-9) showed less GI side effects than DC (P < 0.05, P < 0.01) and no significant difference compared with RC (P > 0.05). CONCLUSION: p-(Methanesulfonyl) styrene-linked cyclic ketone derivatives showed strong anti-inflammatory activity but few GI side effects and deserve to be further investigated.

Animals↗

[Synthesis and anti-inflammatory activity of alpha-substituted p-(methanesulfonyl)phenylpropenamides].

AIM: To search for new compounds with strong anti-inflammatory activity and low gastrointestinal (GI) side effects. METHODS: A series of alpha-substituted p-(methanesulfonyl) phenyl-propenamides were synthesized. Their anti-inflammatory activities against xylene-induced mice ear swelling and carrageenan-induced rat paw edema were evaluated, and their GI side effects in rats were examined. RESULTS: Twenty-five target compounds (II1-25) were obtained, and their structures were determined by IR, 1H NMR, MS and elemental analysis. Thirteen compounds (II1,3,5,8-13,15,18,19,23) exhibited marked anti-inflammatory activity comparable to diclofenac sodium (DC) and rofecoxib (RC) in xylene-induced mice ear swelling model, and twelve compounds (II1,3,5,7,8,10-12,17,18,20,23) showed remarkable anti-inflammatory activity comparable to DC and RC in carrageenan-induced rat paw edema. Compounds II3,8,10,11,18,20 showed GI side effects less than DC (P < 0.01), and no significant difference compared with RC and CMC-Na (P > 0.05). CONCLUSION: alpha-Substituted p-(methanesulfonyl)phenylpropenamides showed strong anti-inflammatory activity but few GI side effects and deserve to be further investigated.

Animals↗

[Determination of epimedin C and icariin in Herba Epimedii by HPLC].

OBJECTIVE: To establish a RP-HPLC method for the determination of epimedin C and icariin in Herba Epimedii. METHOD: Chromatographic conditions: Hypersil BDS-C18 column, acetonitrice and water containing 0.05% phosphoric acid as gradient eluents, G1315A photodiode array detector at 272 nm. RESULT: The average recovery rate of epimedin C was 99.7%, RSD 1.5% (n = 9), icariin 102.5%, RSD 1.1% (n=9). CONCLUSION: The method is reliable, stable and well repeatable. It provides the useful information for quality evaluation.

China↗

[Synthesis and anti-inflammatory analgesic activities of phenylfuroxan-coupled diclofenac].

AIM: To search for new derivatives of diclofenac (DC) having higher potency than the parent drug and lacking its undesirable effects. METHODS: Coupling DC with NO donor 3-hydroxymethyl-4-phenylfuroxan and its isomer through esterification, evaluating anti-inflammatory and analgesic activities, observing side effects in the rat gastrointestinal (GI) tract and assessing NO releasing ability both in vitro and in vivo. RESULTS: Fifteen new compounds including nine target ones (II1-9) were synthesized, and their structures were determined by IR, 1HNMR, MS and elemental analysis. Compounds II3 and II9 showed anti-inflammatory activity comparable to DC. Compound II2 showed stronger anti-inflammatory and analgesic activities and less GI side effect than DC, and released NO in vivo. CONCLUSION: Compound II2 is worthy to be intensively studied.

Analgesics↗