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BACKGROUND Osteoarthritis (OA) of the knee is a common form of arthritis, and affects quality of life. We investigated factors associated with functional limitation in stair climbing among female Japanese patients with knee OA. As weight is a known risk factor for knee OA, we focused on body weight at 40 years of age, and examined the association with present weight, past weight, and weight change. METHODS Subjects were 360 Japanese women aged 40-92 years who were newly diagnosed with knee OA at 3 university hospitals over a 1-year period. Factors associated with the severity of functional limitation in stair climbing were assessed by calculating odds ratios (OR) using the proportional odds model in logistic regression. RESULTS Weight at diagnosis showed a positive association with severe functional limitation in stair climbing; however, a negative association was observed for weight change since age 40. Further analysis indicated that the association with weight at age 40 (highest vs. lowest quartile, OR=2.84, 95% confidence interval: 1.03-7.83, trend p=0.071) is stronger than weight at diagnosis. Other significant characteristics were age (70+ vs. 40-59 years, OR=7.37), previous knee pain and/or swelling 12 years or more before diagnosis (OR=2.67), and physical work (OR=1.94). In addition, higher parity was found to be a negatively associated factor (for tripara or more, OR=0.41). CONCLUSIONS This study identified factors, such as heavy weight at age 40 and physical labor, which are potentially useful for preventing severe functional limitation for female knee OA patients. In addition, higher parity was associated with milder stair climbing limitation.

Enantiomeric differentiations of various (R)-and (5')ammonium and (R)and (S)-a-amino acid ester salts bySUMMARY The interactions of the hydrobromides of (R)and (S)-alanine-N-methylanilides (1) with 24-, 27and 36-membered ring pseudopeptides (H-24, H-27 and H-36, respectively) derived from glycine and (2 S, 3'S)-4-methyl-2-(2'-0~0-3'-isobutyl-l'-piperazinyl)pentanoic acid were studied by means of ' H and I3C NMR measurements in CDCI, . It was found from these results that H-24 and H-27 distinguished ( R )and (S)-isomers of 1, while H-36 did not entirely. Moreover, the enantioface-differentiating abilities of these cyclic peptides were investigated by means of 'H NMR measurements in CDCI, using ( R )and (S)-1-phenylethylammonium and ( R )and (S)-p-methoxy-1-phenylethylammonium bromides as the substrates, showing that the enantioselectivity of H-36 is superior to those of H-24 and H-27. Also, the chiral recognition ability of H-24 for the hydrochlorides of (R)and (S)-alanine (Ala), -leucine (Leu), -methionhe (Met), -phenylalanine (Phe), -proline (Pro) and -valine (Val) methyl esters were examined by 'H and I3C NMR measurements in CDCI, . Among these hydrochlorides, HCI . Phe-OCH, was distinguished more effectively with H-24.

Enantiomeric piperazin-2-one derivatives, N,N'-ethylene-bridged alanylphenylalanines (1a or 1b), were synthesized using (S)- or (R)-alanine and phenylalanine as starting materials, and were inserted into the second and third positions of enantiomeric pseudo-tetrapeptides (P1a- or P1b-OEt). The corresponding piperazine derivatives (1a- or 1b-sRed) obtained by selective BH3 reduction of the amide carbonyl groups of 1a or 1b were similarly inserted into the same positions of tetrapeptides (P1a- and P1b-sRed). Enantiomeric N,N'-ethylene-bridged tyrosyltyrosine derivatives (2a or 2b) obtained from (S)- or (R)-tyrosine were also inserted into the first and second positions of two pairs of enantiomeric tetrapeptides (P2a- and P2b-OEt or P'2a- and P'2b-OEt). The opiate activities of the eight peptides thus obtained were studied by use of the mouse vas deferens and the guinea pig ilcum assays in order to elucidate the structure-activity relationships of these peptides, especially with respect to stereochemistry.