It was found that psoralen derivative could perform a Friedel-Crafts acylation smoothly with acetic anhydride to give 5'-acetylpsoralen in a 73% yield. In the presence of boron trifluoride etherate, 5'-acetylpsoralen reacted with both aromatic amines and aliphatic amine smoothly to afford 5'-Schiff-base group substituted psoralen derivatives in 72%-92% yields. The novel synthetic method has the advantages of cheap materials, mild reaction conditions, good yields and high regioselectivity in the Friedel-Crafts acylation. Cell viability assay by MTT demonstrates that some of the psoralen derivatives 6 have antiproliferative activities.
Acylation ; Boranes ; chemistry ; Cell Line, Tumor ; Cell Proliferation ; drug effects ; Furocoumarins ; chemical synthesis ; chemistry ; pharmacology ; Humans ; Molecular Structure ; Schiff Bases ; chemistry

To identify the expression of thrombopoietin (TPO) receptors (c-mpl) on central nervous system (CNS) and to evaluate the role of TPO on neural cell proliferation and protection, immunohistochemical staining, RT-PCR, MTT, and annexin-V methods were used in this study. The results showed the expression of TPO receptor on human CNS and murine neural cells. C-mpl mRNA was identified in human cerebral hemispheres and cerebellum, and mouse neural cell line C17.2 by RT-PCR. C-mpl was also confirmed in human cerebral hemispheres by immunohistostaining with con-focal microscopy. Furthermore, TPO had a stimulating effect on the growth of in vitro neural cell C17.2 by MTT assay. The anti-apoptotic effect of TPO on C17.2 cells was also demonstrated by staining with annexin-V and PI. In conclusion, the first evidence showed the expression of TPO receptor c-mpl in central nervous system. Moreover, the effect of TPO on neural cell proliferation and anti-apoptosis was also demonstrated on in vitro neural cells.
Animals ; Apoptosis ; drug effects ; Brain Chemistry ; Cell Line ; Cell Proliferation ; drug effects ; Erythropoietin ; pharmacology ; Humans ; Mice ; Neoplasm Proteins ; analysis ; Neurons ; drug effects ; Oncogene Proteins ; analysis ; Proto-Oncogene Proteins ; analysis ; Receptors, Cytokine ; analysis ; Receptors, Thrombopoietin ; Thrombopoietin ; pharmacology

OBJECTIVETo investigate the efficacy of a herbal formula in the prevention of influenza or influenza-like syndrome among elderies residing in old-people's home in Hong Kong. The secondary objectives are to investigate the quality of life (QOL) and symptomology changes among the herbal users and to evaluate the safety of this formula.

METHODSIn ten old people's home or community centres in New Territories, Hong Kong, 740 eligible subjects agreed to join the study and were randomized to receive a herbal formula or a placebo on alternate days over 8 weeks. Among those 740 participants, 113 had provided blood samples for immunological assessments before and after the study drug. Assessments were done at 0, 4, 8 and 12 weeks. Participants were instructed to keep a daily record of body temperature and any symptoms as sore throat, myalgia, running nose or cough, and to report to assessor accordingly. Those reporting body temperature of 37.8 °C and above would be visited and a proper nasopharyngeal swab be taken for viral study.

RESULTSSeventy-two participants developed influenza-like-symptoms but none of them was proven influenza in their nasopharyngeal swabs, 40 of these patients belonged to the herbal group and 32 to the placebo group, without significant differences between groups. The difference on the changes in QOL between the two groups was not statistically significant. However, in the immunological study, the natural killer cell absolute count was significantly increased in the herbal group compared with the placebo group (463 ± 253 vs 413 ± 198, P<0.05).

CONCLUSIONSThe herbal preparation was not effective compared with placebo in the prevention of influenza-like syndrome. It was however safe and possibly supporting immunological responses.

Aged ; Demography ; Double-Blind Method ; Drugs, Chinese Herbal ; adverse effects ; therapeutic use ; Female ; Humans ; Immunologic Tests ; Influenza, Human ; drug therapy ; immunology ; prevention & control ; Male ; Quality of Life ; Vaccination

OBJECTIVETo assess the biological effects of the six-herb mixture Anti-Insomia Formula (AIF) extract using caffeine-induced insomnia Drosophila model and short-sleep mutants.

METHODSCaffeineinduced insomnia wild-type Drosophila and short-sleep mutant flies minisleep (mns) and Hyperkinetic(Y) (Hk(Y)) were used to assess the hypnotic effects of the AIF in vivo. The night time activity, the amount of night time sleep and the number of sleep bouts were determined using Drosophila activity monitoring system. Sleep was defined as any period of uninterrupted behavioral immobility (0 count per minute) lasting > 5 min. Night time sleep was calculated by summing up the sleep time in the dark period. Number of sleep bouts was calculated by counting the number of sleep episodes in the dark period.

RESULTSAIF at the dosage of 50 mg/mL, effectively attenuated caffeine-induced wakefulness (P<0.01) in wild-type Canton-S flies as indicated by the reduction of the sleep bouts, night time activities and increase of the amount of night time sleep. AIF also significantly reduced sleeping time of short-sleep Hk(Y) mutant flies (P<0.01). However, AIF did not produce similar effect in mns mutants.

CONCLUSIONAIF might be able to rescue the abnormal condition caused by mutated modulatory subunit of the tetrameric potassium channel, but not rescuing the abnormal nerve firing caused by Shaker gene mutation. This study provides the scientific evidence to support the use of AIF in Chinese medicine for promoting sleep quality in insomnia.

Animals ; Caffeine ; Chromatography, High Pressure Liquid ; Disease Models, Animal ; Drosophila melanogaster ; drug effects ; physiology ; Hypnotics and Sedatives ; pharmacology ; therapeutic use ; Mutation ; genetics ; Potassium Channels ; genetics ; Sleep ; drug effects ; Sleep Initiation and Maintenance Disorders ; drug therapy ; Wakefulness ; drug effects

OBJECTIVETo investigate the protective effects of a Chinese herbal formula, taikong yangxin prescription (TKYXP) against bone deterioration in a hindlimb unloaded (tail-suspension) rat model.

METHODSThirty-two male Sprague-Dawley rats were divided into 4 groups: tail-suspension group fed with 2.5 g•kg(-1)•day(-1) of TKYXP extract (high dose), tail-suspension group fed with 1.25 g•kg(-1)•day(-1) (low dose), tail-suspended group treated with water placebo (placebo control group) and non tail-suspended group. The effects of TKYXP on bone were assessed using peripheral quantitative computed tomography (pQCT), microcomputerized tomography (micro-CT) and three-point bending biomechanical test on the femur in vivo.

RESULTSTKYXP had a significant protective effect against bone loss induced by tail-suspension on day 28, as shown in the reduction in bone mineral density (BMD) loss, preservation of bone micro-architecture and biomechanical strength. The administration ofhigh dose TKYXP could significantly reduce the total BMD loss by 4.8% and 8.0% at the femur and tibia regions, respectively, compared with the placebo control group (P<0.01) on day 28. Its bone protective effect on the femur was further substantiated by the increases of the trabecular BMD (by 6.6%), bone volume fraction (by 20.9%), trabecular number (by 9.5%) and thickness (by 11.9%) as compared with the placebo control group.

CONCLUSIONTKYXP may protect the bone under weightless influence from gradual structural deterioration in the tail-suspension model.

Animals ; Biomechanical Phenomena ; drug effects ; Bone Density ; drug effects ; Bone and Bones ; diagnostic imaging ; drug effects ; Drugs, Chinese Herbal ; administration & dosage ; pharmacology ; Femur ; Male ; Rats ; Rats, Sprague-Dawley ; Tibia ; Tomography Scanners, X-Ray Computed ; Weightlessness ; X-Ray Microtomography