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排序方式: 共有737条查询结果,搜索用时 15 毫秒
1.
青蒿琥酯皮肤擦剂在小鼠和兔体内的药代动力学研究 总被引:1,自引:0,他引:1
将青蒿琥酯溶于苯二甲酸二甲酯,加适量氨酮制成皮肤擦剂。给兔脱毛后,皮肤涂抹此擦剂25mg/kg后,血药浓度达峰时间平均为2 h,峰浓度平均为1.80μg/ml。药物在兔体内平均驻留时间为3.54 h,清除半衰期约为2.46 h。给小鼠脱毛皮肤涂抹擦剂6.7,31.3和71.4 mg/kg,血药浓度在给药后0.5~4 h达高峰,峰浓度分别为0.82,2.05和7.11μg/ml,体内药物平均驻留时间为3.39,2.79及3.54 h,清除半衰期为2.35,1.93及2.45 h。可见,给兔及小鼠皮肤擦剂后,青蒿琥酯吸收良好,血药浓度维持时间较长。 相似文献
2.
取代四氢异喹啉衍生物的合成及其生物活性 总被引:7,自引:0,他引:7
粉防己碱有钙拮抗作用,临床试用于治疗高血压,其裂解产物钙拮抗作用降低,但有α-肾上腺素能受体拮抗作用,本文以裂解物为先导化合物设计合成了两类取代的四氢异喹啉衍生物Ⅲ及Ⅳ。初步药理试验表明:大部分化合物有α-肾上腺素能受体拮抗作用,少数化合物钙拮抗活性有所增强,其中Ⅲ15,19对正常麻醉大鼠有一定的降压作用、Ⅳ17,19对实验性动物心律失常有明显的保护作用。部分化合物量化计算表明:化合物与α1-受体作用方式可能是形成电荷转移复合物。 相似文献
3.
4.
以18-甲基-17β-羟基-17α-乙炔基-雌甾-4-烯-3-酮(18-甲基炔诺酮),17β-羟基-17α-乙缺基-雌甾-4-烯-3-酮(炔诺酮),17β-羟基-17α-乙炔基-雄甾-4-烯-3-酮(妊娠素)和17a-羟基孕甾-4-烯-3,20二酮(17α-羟基黄体酮)为原料,经NaBH,还原、脱水、双键转位和酯化等反应合成一系列3,5-甾二烯化合物,用1HNMR和MS证明了它们的结构。动物筛选结果表明,17β-丙酰氧基-17α-乙炔基-雌甾-3,5-二烯(IVb2有明显的抗早孕活性。中断早期妊娠的作用似与其雌激素活性有关。 相似文献
5.
6.
Localization of plasminogen activator and inhibitor, LH and androgen receptors and inhibin subunits in monkey epididymis 总被引:4,自引:1,他引:4
Epididymis is a site of sperm maturation and storage. Limited and
directed-proteolysis regulated by plasminogen activator (PA), plasminogen
activator inhibitor type-1 (PAI-1) and other related factors may play an
essential role in these processes. Our previous studies have demonstrated
that rat epididymis expressed luteinizing hormone receptor (LHR), tissue
type (t) and urokinase type (u)PA, mRNAs, and tPA activity was stimulated
in vitro by human chorionic gonoadotrophin (HCG). In the present study we
further examined localization of mRNAs for tPA, uPA, LHR, androgen receptor
(AR), as well as inhibin subunits alpha, betaA and betaB in rhesus monkey
epididymis. Using in-situ hybridization with digoxygenin-labelled cRNA
probes, we have demonstrated that tPA and PAI-1 mRNAs were localized in
epithelial cells of adult monkey epididymis. uPA mRNA was localized in the
same areas, but to a much smaller extent. tPA, uPA and PAI-1 mRNAs were
greatly expressed in the caput and corpus of adult epididymis than in other
regions. In-vitro experiments showed that both tPA and uPA activities in
epididymal cells were dramatically stimulated by HCG, but not by follicle
stimulating hormone (FSH). LHR (but not FSH receptor) and AR mRNAs were
localized in the epithelial cells of the epididymis. However, LHR mRNA was
detected in both adult and immature infant monkeys, whereas AR was found
only in the adult. Inhibin alpha, betaA and betaB mRNAs were also detected
in this organ, betaA mRNA being more strongly expressed in the caput than
in other regions of the epididymis. We suggest that LH and androgen may be
the key hormones in coordination with the PA-PAI-1 system in regulating
epididymal differentiation and sperm maturation.
相似文献
7.
Bradshaw Catherine P. Pas Elise T. Musci Rashelle J. Kush Joseph M. Ryoo Ji Hoon 《Prevention science》2021,22(7):986-1000
Prevention Science - This study examined the impact of a state policy requiring that any school with a habitual truancy rate of 8% or higher to be trained in Tier 1 school-wide Positive Behavioral... 相似文献
8.
An antioxidant lignan and other constituents from the root bark of Hibiscus syriacus 总被引:2,自引:0,他引:2
A new lignan named as hibiscuside, (+)-pinoresinol 4-O-[beta-glucopyranosyl (1--->2)-alpha-rhamnoside] (1), and a known lignan, syringaresinol (2) were isolated from the root bark of Hibiscus syriacus together with two feruloyltyramines (3,4) and three known isoflavonoids (5,6,7). The structures of these compounds have been established on the basis of their NMR, mass UV spectra. Among these phenolic compounds, 6"-O-acetyldaidzin (5), 6"-O-acetylgenistin (6), and 3-hydroxydaidzein (7) with IC(50) values of 8.2, 10.6, and 4.1 microM, respectively, significantly inhibited lipid peroxidation in rat liver microsomes. Hibiscuside (1), E- and Z-N-feruloyl tyramines (3,4) exhibited moderate antioxidant activity. 相似文献
9.
Kwanhoon Choi Jeongyeon Yoon Hyun Kyo Lim Sungwoo Ryoo 《The Korean journal of physiology & pharmacology》2014,18(2):95-101
Cardiovascular disease is the prime cause of morbidity and mortality and the population ages that may contribute to increase in the occurrence of cardiovascular disease. Arginase upregulation is associated with impaired endothelial function in aged vascular system and thus may contribute to cardiovascular disease. According to recent research, Korean Red Ginseng water extract (KRGE) may reduce cardiovascular disease risk by improving vascular system health. The purpose of this study was to examine mechanisms contributing to age-related vascular endothelial dysfunction and to determine whether KRGE improves these functions in aged mice. Young (10±3 weeks) and aged (55±5 weeks) male mice (C57BL/6J) were orally administered 0, 10, or 20 mg/mouse/day of KRGE for 4 weeks. Animals were sacrificed and the aortas were removed. Endothelial arginase activity, nitric oxide (NO) generation and reactive oxygen species (ROS) production, endothelial nitric oxide synthase (eNOS) coupling, vascular tension, and plasma peroxynitrite production were measured. KRGE attenuated arginase activity, restored nitric oxide (NO) generation, reduced ROS production, and enhanced eNOS coupling in aged mice. KRGE also improved vascular tension in aged vessels, as indicated by increased acetylcholine-induced vasorelaxation and improved phenylephrine-stimulated vasoconstriction. Furthermore, KRGE prevented plasma peroxynitrite formation in aged mice, indicating reduced lipid peroxidation. These results suggest KRGE exerts vasoprotective effects by inhibiting arginase activity and augmenting NO signaling and may be a useful treatment for age-dependent vascular diseases. 相似文献
10.
A prospective,multicenter phase II study of continuous infusion of FLAG for patients older than 60 yr with resistant acute myeloid leukemia: a comparison with intensive younger patients’ trial
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Hawk Kim Je‐Hwan Lee Young‐Don Joo Sung Hwa Bae Jung‐Hee Lee Dae‐Young Kim Won‐Sik Lee Hun‐Mo Ryoo Jae‐Cheol Jo Yunsuk Choi Kyoo‐Hyung Lee CoOperative Study Group A for Hematology 《European journal of haematology》2016,96(2):188-197
Relapsed or refractory acute myeloid leukemia (R/R AML) in elderly (≥60 yr old) patients were eligible. Induction chemotherapy consisted fludarabine and cytarabine (ARAC) as a 24‐hr CI without idarubicin (C‐FLAG), which was compared with the results of C‐FLAG with idarubicin (CI‐FLAG2) in younger patients’ trial. A total of 33 and 68 patients were enrolled in C‐FLAG and CI‐FLAG2, respectively. CR, CRp, and CRi were achieved in 10 (30.3%), 3 (9.1%), and 2 (6.1%), respectively. When comparing outcomes between C‐FLAG and CI‐FLAG2, there were no difference in terms of CR rate (P = 0.572) and objective response rate (ORR; P = 0.899). Favorable predictors on ORR in C‐FLAG were PB WBC ≤ 20K/uL at salvage (P = 0.024) and early evaluation peripheral BLAST = 0% (P = 0.013) on multivariate analysis. The overall survival of patients who achieve CR/CRp/CRi showed significantly prolonged survival compared with patients who did not in C‐FLAG (P < 0.001) and was a favorable predictor of longer survival by multivariate analysis (P = 0.009). Median overall survival was 3.19 (95% CI, 2.05–4.33) months and similar with that of CI‐FLAG2 (P = 0.841). Attenuated salvage regimen C‐FLGA in elderly patients was as effective as more intensive younger patients’ regimen CI‐FLAG2 in terms of response and survival although elderly patients had more unfavorable clinical characteristics. 相似文献