Impressic acid from Acanthopanax koreanum, possesses matrix metalloproteinase-13 down-regulating capacity and protects cartilage destruction.

Ethnopharmacological Relevance: Acanthopanax koreanum (Araliaceae) has been used in traditional medicine for enhancing vitality, rheumatism, and bone-related pains. But its activity on cartilage protection has not been known yet.

Aim Of The Study: Matrix metalloproteinase (MMP)-13 has an important role in degrading cartilage materials under pathologic conditions such as arthritis.

t-Butyl pyridine and phenyl C-region analogues of 2-(3-fluoro-4-methylsulfonylaminophenyl)propanamides as potent TRPV1 antagonists.

A series of 2-substituted 6-t-butylpyridine and 4-t-butylphenyl C-region analogues of 2-(3-fluoro-4-methylsulfonamidophenyl)propanamides were investigated for hTRPV1 antagonism. The analysis of structure activity relationships indicated that the pyridine derivatives generally exhibited a little better antagonism than did the corresponding phenyl surrogates for most of the series. Among the compounds, compound 7 showed excellent antagonism toward capsaicin activation with K=0.

Structure activity relationships of benzyl C-region analogs of 2-(3-fluoro-4-methylsulfonamidophenyl)propanamides as potent TRPV1 antagonists.

A series of 2-substituted 4-(trifluoromethyl)benzyl C-region analogs of 2-(3-fluoro-4-methylsulfonamidophenyl)propanamides were investigated for hTRPV1 antagonism. The analysis indicated that the phenyl C-region derivatives exhibited better antagonism than those of the corresponding pyridine surrogates for most of the series examined. Among the phenyl C-region derivatives, the two best compounds 43 and 44S antagonized capsaicin selectively relative to their antagonism of other activators and showed excellent potencies with K(i(CAP))=0.

Effects of trunk-hip strengthening on standing in children with spastic diplegia: a comparative pilot study.

[Purpose] This study evaluated the effects of trunk-hip strengthening exercise on trunk-hip activation and pelvic tilt motion during standing in children with spastic diplegia and compared the improvement of pelvic tilt between the modified trunk-hip strengthening exercise and conventional exercise. [Subjects and Methods] Ten ambulant children with spastic diplegia were randomized to the modified trunk-hip strengthening exercise (n = 5) or conventional exercise (n = 5) group. The intervention consisted of a 6-week modified trunk-hip strengthening exercise 3 times per week.

Influence of pelvic position and vibration frequency on muscle activation during whole body vibration in quiet standing.

[Purpose] The purpose of this study was to investigate muscle activation related to postural stability depending on the pelvic position and frequency of whole body vibration (WBV) during quiet standing, and to identify the most effective training conditions that elicit the highest neuromuscular responses. [Subjects and Methods] Eighteen healthy subjects voluntarily participated in this single-group, repeated-measures study in which surface electromyography (EMG) data for the upper trapezius, rectus abdominis, external oblique abdominis, erector spinae, gluteus maximus, rectus femoris, semitendinosus, and medial gastrocnemius were collected at three frequencies (0 Hz, 10 Hz, and 20 Hz) of WBV and three pelvic positions (neutral, anterior tilt, posterior tilt) for each subject during quiet standing. [Results] The EMG activities of all the recorded muscles showed significant differences between the three frequencies of WBV and three pelvic positions during quiet standing.

2-Alkyl/alkenyl substituted pyridine C-region analogues of 2-(3-fluoro-4-methylsulfonylaminophenyl)propanamides as highly potent TRPV1 antagonists.

A series of 2-alkyl/alkenyl pyridine C-region derivatives of 2-(3-fluoro-4-methylsulfonylaminophenyl)propanamides were investigated as hTRPV1 antagonists. Multiple compounds showed excellent and stereospecific TRPV1 antagonism with better potency than previous lead 2. Among them, compound 15f demonstrated a strong analgesic profile in a rat neuropathic pain model and blocked capsaicin-induced hypothermia in a dose-dependent manner.

Suitability of macrophage inflammatory protein-1beta production by THP-1 cells in differentiating skin sensitizers from irritant chemicals.

Background: Worldwide restrictions in animal use for research have driven efforts to develop alternative methods.

Objective: The study aimed to test the efficacy of the macrophage inflammatory protein-1beta (MIP-1beta) assay for testing chemicals' skin-sensitizing capacity.

Methods: The assay was performed using 9 chemicals judged to be sensitizing and 7 non-sensitizing by the standard in vivo assays.