A new triterpenoid saponin, loniceroside C was isolated from the aerial parts of Lonicera japonica. Its structure was established to be 3-O-beta-D-glucopyranosyl hederagenin 28-O-alpha-L-rhamnopyranosyl (1-->2)-[beta-D-xylopyranosyl(1-->6)]-beta-D-glucopyranosyl ester by spectroscopic techniques and chemical transformations. Loniceroside C showed in vivo antiinflammatory activity against mouse ear edema provoked by croton oil.
Periodic evolution of H 2 S during aerobic chemostat culture of Saccharomyces cerevisiae resulted in ultradian metabolic oscillation via periodic inhibition of respiratory activity. To understand the nature of periodic H 2 S evolution, we investigated whether oxidative stress is associated with H 2 S production. The cellular oxidative states represented by intracellular level of lipid peroxides oscillated out of phase with the oscillation of dissolved O 2 . Pulse addition of antioxidant, oxidative agent or inhibitor of antioxidation enzymes perturbed metabolic oscillation producing changes in H 2 S evolution. Analysis of H 2 S production profiles during perturbation of oscillation revealed that the amount of H 2 S production is closely linked with cellular oxidative states. Based on these results and our previous reports, we suggest that oxidative stresses result in periodic depletion of glutathione and cysteine, which in turn causes stimulation of the sulfate assimilation pathway and H 2 S production. ß
The structural relationship of 16 asiatic acid (AA) derivatives, including AA and asiaticoside (AS) to cytotoxicity and anti-hepatofibrotic activity in HSC-T6 cells, were investigated. Cytotoxicities of AA derivatives varied from 5.5 microM to over 2000 microM of IC50 depending on AA functional group modifications. Substituting the hydroxyl group at the C(2) to N[triple bond]C and substituting bulky groups for dihydroxyl groups at (3), (23) of the A-ring increased the cytotoxicity, but keto group at C(11) and benzoyl ester at C(2) were greatly reduced it. Modification of the carboxylic acid group at C28 also reduced the cytotoxicity. The collagen synthesis determined by hydroxyproline content in the cells was inhibited from a maximum of 48% (Zlx-i-85 and 87) to 15% (AS) by AA derivatives. The anti-hepatofibrotic effect of these compounds might be due to the reduced expression of prolyl 4-hydroxylase alpha and beta subunits and TIMP2. However, the inhibition of collagen by asiaticoside derivatives did not show any structural-activity relationship.
The efficacy and safety of SKI306X, an herbal anti-arthritic agent, was compared with that of diclofenac sodium for the treatment of osteoarthritis of the knee. In a randomized, double-blind, active comparator-controlled trial, a total of 249 patients were randomly assigned to receive either 200 mg of SKI306X three times daily or 100 mg of diclofenac sustained release (SR) once daily. Clinical efficacy variables (visual analog scale, Lesquesne index and global satisfaction score) and adverse events were monitored at baseline and 2nd and 4th weeks of treatment. SKI306X demonstrated efficacy statistically comparable to that of diclofenac, as assessed by the VAS and patients' and investigators' global satisfaction score. Both treatments were well tolerated, however, the SKI306X treatment group experienced less heartburn (4.0% versus 13.7%, p = 0.015, chi-square test). In this four-week trial, SKI306X was well tolerated and demonstrated clinical efficacy comparable to that of diclofenac SR.
Papyriflavonol A, a new prenylated flavonol isolated from Broussonetia papyrifera, selectively inhibits recombinant human secretory phospholipase A 2 s (sPLA 2 s). Papyriflavonol A was found to inhibit human group IIA and V sPLA 2 s potently and irreversibly in a dose-dependent manner, with respective IC 50 values of 3.9 and 4.5 m mM. The inhibitory effects of papyriflavonol A against bovine group IB (IC 50 of 76.9 m mM) and the human group X (IC 50 of 225 m mM) sPLA 2 s were weaker than those against human group IIA and V sPLA 2 s, and human group IIF sPLA 2 was not inhibited. In addition, papyriflavonol A potently inhibited the stimulus-induced production of leukotriene C 4 with an IC 50 value of approximately 0.64 m mM in mouse bone marrow-derived mast cells. In addition, papyriflavonol A significantly reduced IgE-dependent passive cutaneous anaphylaxis in rats. These results indicate that papyriflavonol A provides a basis for novel types of antiinflammatory drugs.
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