白英中甾体类总生物碱的含量测定研究

目的:建立白英中甾体类总生物碱含量的测定方法。方法:采用醇提-酸醇水解法提取白英中的总生物碱,分离得到甾体类总生物碱,用紫外-可见分光光度法,以澳洲茄胺为对照,溴甲酚绿为显色剂,在412 nm处测定吸光度值,计算白英中甾体总生物碱的含量。结果:澳洲茄胺在1.6μg/m L~9.6μg/m L范围内与吸光度值呈良好的线性关系(r=0.999 5),平均回收率为88.70%~102.2%(n=9),RSD为3.09%~4.96%,不同来源的白英药材中甾体总生物碱的含量有一定的差异。结论:该方法准确、简单、灵敏,适合测定白英药材中甾体类总生物碱的含量,并且可为白英的质量评价提供理论参考。     

3种抗真菌生药活性成分对两种真菌细胞遗传物质的影响

目的　研究抗真菌生药活性成分对真菌细胞遗传物质的影响,以期发现其抗真菌的作用机理。方法　把对照组及用药组真菌细胞进行激光扫描共聚焦显微镜观察并作细胞扫描图像分析,从而定量描述细胞形状、面积和DNA,RNA含量。结果　用药组细胞形态及DNA,RNA含量发生不同变化。结论　澳洲茄胺、紫檀　和白鲜碱直接或间接影响了真菌细胞遗传物质的正常合成以至不能完成正常细胞周期,从而抑制真菌生长甚至导致死亡。     

Anticonvulsant activity of solasodine isolated from Solanum sisymbriifolium fruits in rodents

Context: Solanum sisymbriifolium Lam. (Solanaceae), commonly known as sticky nightshade, is traditionally used for central nervous system (CNS) disorders. Although solasodine has been isolated from this plant, little is known about its anticonvulsant and CNS depressant actions.

Objective: We investigated anticonvulsant and CNS depressant effects of solasodine isolated from S. sisymbriifolium using several experimental models.

Materials and methods: Swiss albino mice (n?=?6) were employed for pentylenetetrazole (PTZ) and picrotoxin (PCT)-induced convulsions and thiopental-induced sleep time. Different groups of Wistar albino rats (n?=?6) were subjected to maximal electroshock (MES) test. Solasodine, a steroidal glycoalkaloid, was isolated from dried fruits of S. sisymbriifolium and identified by GC-MS.

Results: The results showed that intraperitoneal (i.p.) injection of solasodine (25?mg/kg) significantly delayed (p < 0.01) latency of hind limb tonic extensor (HLTE) phase in the PCT-induced convulsions. In the MES model, solasodine significantly reduced (p < 0.001) duration of HLTE at 25, 50, and 100?mg/kg, i.p. in a dose-dependent manner. Interestingly, solasodine did not produce any significant reduction in PTZ-induced convulsions. Prior treatment of solasodine (25, 50, and 100?mg/kg, i.p.) significantly potentiated thiopental-provoked sleep in a dose-dependent manner (p < 0.001).

Discussion and conclusion: Our study, for the first time, shows potent anticonvulsant and CNS depressant activities of solasodine. It is likely that solasodine, in part, is responsible for the anticonvulsant and sedative properties of S. sisymbriifolium. The future study should focus on the exact mechanism of action of solasodine.     

Antifertility plant products: testicular cell population dynamicsfollowing solasodine (C27H43O2N) administration in rhesus monkey (Macaca mulatta)

Solasodine obtained from the Solanum xanthocarpum berries was administered to Rhesus monkeys for 150 days to evaluate their effect on testicular cell population dynamics. Solasodine brings about an interference with spermiogenesis at the stage XII of late spermatids. The spermatids were decreased by 69% (P less than 0.001). No significant change was found in the population of spermatogonia/primary and secondary spermatocytes. The production of immature and mature Leydig cells were decreased by 60.4% and 41.6% respectively. A significant decrease in cauda sperm count (Control: 83.1 +/- 6.3; Solasodine 1.21 +/- 0.3 million/ml) was noticed. The testicular protein, sialic acid and glycogen contents were depleted following solasodine treatments to rhesus monkeys. Bioassay studies showed the antiandrogenic nature of the compound.     

甾体生物碱澳洲茄胺的研究进展

澳洲茄胺是来源于茄属植物的一种甾体生物碱,具有多重药理活性,特别是较强的抗肿瘤活性。综述近年来有关其药理活性、作用机制及其合成研究的进展,并对该类化合物作为抗肿瘤药物的开发潜力和发展前景进行展望。     

Antispermatogenic/antiandrogenic properties of solasodine (C27H43O2N) obtained from solanum xanthocarpum berries on the male genital tract of dog (Canis-familiaris). A Histophysiological approach

Chronic administration of solasodine (20 mg/kg alt. day for 30 days) caused testicular lesions resulting in a severe impairment of spermatogenic elements. The epididymides were devoid of spermatozoa. Total protein, sialic acid and glycogen contents of the testis and epididymis were reduced significantly whereas the testicular cholesterol was elevated. Acid Phosphatase enzyme activity of the testes was low after solasodine treatment. Serum enzymes (SGPT, alkaline phosphatase) serum protein, triglycerides, non esterified fatty acid levels were in normal range when compared with their own controls. Cholesterol and phospholipid levels were elevated after solasodine treatment to intact dogs. Reduced androgen production was reflected in low levels of sialic acid in the testes and epididymides and reduced Leydig cell nuclei. Castration alone brought about reduction in size of the epididymis. Castration followed by solasodine treatment caused epididymal degeneration. Simultaneous administration of TP to solasodine treated castrated dogs failed to stimulate the epididymal growth. Antispermatogenic/antiandrogenic activity of the compound solasodine is discussed. Solasodine administration in dogs definitely rendered the male infertile as evidenced by the absence of sperms in the cauda epididymis and ductus deferens.     

Phytochemical study of Solanum lycocarpum (St. Hil) unripe fruit and its effects on rat gestation

Solanum lycocarpum, St. Hil (Solanaceae) is a common native shrub in the Brazilian cerrado. The fruits are used in folk medicine as a hypoglycaemic agent in the management of diabetes, obesity and to decrease cholesterol levels. In this study the glycoalkaloids, solamargine and solasonine, were isolated from unripe fruits of S. lycocarpum. To evaluate the effects of the fruits on gestation, pregnant rats (n=25) were fed from day 6 to 22 with chow containing 10% of dried and ground unripe fruits. The control group (n=21) received regular chow. During and after the treatment period the dams showed reduced body weight and slower body weight gain, even with no change in food and water intake, evidencing mild maternal toxicity. Gestation was not significantly impaired, although experimental fetuses presented reduced body length at birth. Also, 20% of the treated dams showed one or two dead pups at birth. On day 22 of gestation and on post-natal day 1, the levels of metabolites of the sex hormones oestradiol, progesterone and testosterone were measured in faeces by radioimmunoassay. On post-natal day 1, tissue portions from the dams were collected for histopathological evaluation. No alterations were detected in either study. The results suggest that S. lycocarpum fruit did not impair gestation, however, it did promote mild maternal toxicity and mild fetotoxic effects if ingested as a food source during the gestation period. This study has implications for pregnant women, who employ phytotherapeutic formulations under the impression that they are harmless.     

A functional drug delivery platform for targeting and imaging cancer cells based on Pluronic F127

Functional polymeric micelles play an important role in the efficient delivery of therapeutic drugs into tumours. In this study, a functional drug delivery platform with ligands for targeting and fluorescent imaging was designed based on Pluronic F127 (PF127). Using folic acid (FA) and fluorescein isothiocyanate (FITC) to chemically conjugate with PF127, two functional polymers, Pluronic F127-FA (PF127-FA) and Pluronic F127-FITC (PF127-FITC), were synthesized. Solasodine-loaded micelles were then prepared via the thin-film hydration method. By employing A549 and HeLa cells, the results of in vitro cell assays performed using confocal laser scanning microscopy and flow cytometry suggested that the proposed micelles could provide the desired specific targeting and fluorescent imaging functions. In addition, the results of in vitro cytotoxicity experiments showed that the growth inhibition rates of A549 and HeLa cells treated with solasodine-loaded micelles were remarkably higher than those of cells treated with free solasodine. Solasodine-loaded micelles exhibited a more distinct inhibitory effect against HeLa cells than against A549 cells. Thus, an effective drug delivery system for targeting and imaging cancer cells was developed.     

薄层扫描法测定龙葵中澳洲茄胺的含量

 目的：探讨龙葵中澳洲茄胺的含量测定。方法：采用薄层扫描法进行含量测定。结果：龙葵全草中澳洲茄胺含量为0．0928％，果实中含量为1．16％。结论：本法灵敏，稳定，可用于龙葵的质量控制。     

Antinociceptive activity of steroid alkaloids isolated from Solanum trilobatum Linn.

Solasodine (1) was isolated for the first time from the roots of Solanum trilobatum Linn., a member of the Solanaceae, and assessed for its presumed antinociceptive activity using several experimental murine models, viz. the writhing, formalin, and hot plate tests. When used at doses of 2, 4, and 8 mg/kg, this steroidal alkaloid caused a significant and dose-dependent decrease in the nociception induced by an intraperitoneal injection of acetic acid (p < 0.001). It also led to a significant reduction of the painful sensation caused by formalin in both phases of the formalin test (p < 0.001). Furthermore, the alkaloid produced a significant increase in the reaction time in the hot plate test (p < 0.001). These results suggest that solasodine elicited antinociceptive activity through both central and peripheral mechanisms.