Preparation,characterization, and antibacterial activity of plaunotol and plaunoi extracts complexed with hydroxypropyl-β-cyclodextrin

Croton stellatopilosus (Plaunoi) leaves accumulate several diterpenes and possess various pharmacological activities. The present study aimed to prepare, characterize and assess the antibacterial activity of inclusion complexes prepared by mixing plaunotol (PL) or plaunoi extract (PE) with cyclodextrins (CD), including α-CD, β-CD, γ-CD, and hydroxypropyl-β-cyclodextrin (HP-β-CD). The inclusion complexes were characterized using SEM, XRD, DSC, and FT-IR and evaluated for aqueous solubility and thermal stability. The PL and PE lyophilized complexes with HP-β-CD were further evaluated for their antibacterial activity against acne-causing bacteria. The minimum inhibitory concentration (MIC) and the minimum bactericidal concentration (MBC) of PL, PE, and the inclusion complexes evaluated using the agar dilution method revealed that the MIC and MBC values of the inclusion complexes were lower than those of PL or PE alone. Interestingly, the complexes had a synergistic activity with clindamycin after testing with checkerboard assay. The hydrogel containing the inclusion complex and clindamycin were assessed for antibacterial activity using the agar well diffusion method. The results indicated that the hydrogels showed significant inhibition of bacterial growth. In conclusion, the prepared solid dispersion of PL or PE with HP-β-CD could enhance antibacterial activity by increasing the drug solubility. The hydrogels containing PL or PE complex and clindamycin could be considered as a candidate for the treatment of acne vulgaris.     

胃痛宁片质量标准的研究

目的 建立胃痛宁片的质量标准.方法 采用TLC法对处方中龙胆粉进行定性鉴别,采用HPLC法测定蒲公英提取物中咖啡酸的质量分数.结果 在薄层色谱中可检出龙胆苦苷的特征斑点;咖啡酸回归方程为A=42.128 6ρ-19.133 2(r2=1),在6.29～ 62.9 μg/mL范围内线性关系良好,平均加样回收率为96.4％,RSD为0.28％(n=6).结论 所建立的定性方法专属性强,定量方法简便、准确,能有效地控制胃痛宁片的质量.     

Antihyperglycemic Effect of Methanol Extract of Syzygium polyanthum (Wight.) Leaf in Streptozotocin-Induced Diabetic Rats

Syzygium polyanthum (S. polyanthum), a plant belonging to Myrtaceae, is widely used in Indonesian and Malaysian cuisines. Diabetic patients in Indonesia also commonly use it as a traditional medicine. Hence, this study was conducted to investigate the antihyperglycemic effect of the methanol extract (ME) of S. polyanthum leaf and its possible mechanisms of action. To test for hypoglycemic activity, ME was administered orally to normal male Sprague Dawley rats after a 12-h fast. To further test for antihyperglycemic activity, the same treatment was administered to glucose-loaded (intraperitoneal glucose tolerance test, IPGTT) and streptozotocin (STZ)-induced diabetic rats, respectively. Hypoglycemic test in normal rats did not show significant reduction in blood glucose levels (BGLs) by the extract. Furthermore, IPGTT conducted on glucose-loaded normal rats also did not show significant reduction of BGLs. However, repeated administration of metformin and three doses of ME (250, 500 and 1000 mg/kg) for six days caused significant reduction of fasting BGLs in STZ-induced diabetic rats. The possible mechanisms of action of S. polyanthum antihyperglycemic activity were assessed by measurement of intestinal glucose absorption and glucose uptake by isolated rat abdominal muscle. It was found that the extract not only inhibited glucose absorption from the intestine but also significantly increased glucose uptake in muscle tissue. A preliminary phytochemical qualitative analysis of ME indicated the presence of tannins, glycosides, flavonoids, alkaloids and saponins. Additionally, Gas Chromatography-Mass Spectrometry (GC-MS) analysis detected squalene. In conclusion, S. polyanthum methanol leaf extract exerts its antihyperglycemic effect possibly by inhibiting glucose absorption from the intestine and promoting glucose uptake by the muscles.     

D-004 ameliorates phenylephrine-induced urodynamic changes and increased prostate and bladder oxidative stress in rats

Background

Lower urinary tract symptoms (LUTS) in patients with benign prostatic hyperplasia (BPH) mainly depend on alpha1-adrenoreceptors (α₁-ADR) stimulation, but a link with oxidative stress (OS) is also involved. D-004, a lipid extract of Roystonea regia fruits, antagonizes ADR-induced responses and produces antioxidant effects. The objective of this study was to investigate whether D-004 produce antioxidant effects in rats with phenylephrine (PHE)-induced urodynamic changes.

Methods

Rats were randomized into eight groups (ten rats/group): a negative vehicle control and seven groups injected with PHE: a positive control, three treated with D-004 (200, 400 and 800 mg/kg) and three others with tamsulosin (0.4 mg/kg), grape seed extract (GSE) (250 mg/kg) and vitamin E (VE) (250 mg/kg), respectively.

Results

Effects on urinary total volume (UTV), volume voided per micturition (VM), malondialdehyde (MDA) and carbonyl groups (CG) concentrations in prostate and bladder homogenates were study outcomes. While VM and UTV lowered significantly in the positive control as compared to the negative control group, the opposite occurred with prostate and bladder MDA and CG values. D-004 (200-800 mg/kg) increased significantly both VM and UTV, lowered significantly MDA in prostate and bladder homogenates, and reduced GC levels only in the prostate. Tamsulosin increased significantly VM and UTV, but unchanged oxidative variables. GSE and VE unchanged the UTV, whereas VE, not GSE, modestly but significantly attenuated the PHE-induced decrease of VM.

Conclusions

Single oral administration of D-004 (200-800 mg/kg) was the only treatment that ameliorated the urodynamic changes and reduced increased oxidative variables in the prostate of rats with PHE-induced prostate hyperplasia.     

Protective effects of Eugenia jambolana extract versus N‐acetyl cysteine against cisplatin‐induced damage in rat testis

To assess the protective effects of Eugenia jambolana extract (EJE) or N‐acetyl cysteine (NAC) on testis, cisplatin (CIS, 5 mg kg^?1 bw, single dose) was administered either alone or along with EJE (25 mg kg^?1 bw, alternate day) or NAC (150 mg kg^?1 bw, Day 1 and 4) for 7 days. Significant alterations in serum LH, FSH and testosterone were observed in CIS group which were effectively modulated by EJE or NAC supplementation. Upregulation of 3β‐HSD gene indicated the rise in functional Leydig cells. This was further confirmed from the identical improvement in hCG‐stimulated testosterone production in isolated Leydig cells. Reduction in oxidative stress was associated with restoration of total antioxidant capacity and glutathione levels, and activation of antioxidant enzymes, SOD, catalase, glutathione s‐transferase (GST) and glutathione reductase (GR). CIS‐induced apoptosis of germ and Leydig cells was contained by both NAC and EJE intervention by effective modulation of apoptotic markers in the extrinsic, intrinsic and other pathways of metazoan apoptosis. Taken together, the study findings establish the potential of EJE as a therapeutically better antioxidant than NAC for use in curtailing the adverse effects of anticancer drugs on testicular function.     

红花标准汤剂的质量评价

目的:建立红花标准汤剂的质量控制方法。方法:收集有代表性的14批红花,制备红花标准汤剂,计算出膏率、指标成分转移率和溶液pH等参数,评价工艺的稳定性;建立指标成分含量测定和指纹图谱方法,采用UPLC-Q-TOF/MS对主要色谱峰进行结构确认,明确红花标准汤剂中的主要化学成分。结果:标准汤剂出膏率32.6%,羟基红花黄色素A的转移率61.2%,pH 4.1;标准汤剂中羟基红花黄色素A平均质量浓度3.6 g·L~(-1),指纹图谱相似度均0.9,标准汤剂的主要成分为黄酮类。结论:建立了系统评价红花标准汤剂的质量评价方法,为所有源于红花水煎液的制剂的质量标准制定提供参考,所得红花标准汤剂的指标成分转移率高、质量均一性良好。     

栀子标准汤剂的质量评价方法考察

目的:建立栀子标准汤剂的质量评价方法,为所有源于栀子水提液的制剂的质量标准制定提供参考。方法:制备15批栀子标准汤剂,测定其出膏率、指标成分转移率和pH;建立栀子标准汤剂的UPLC指纹图谱并对主要色谱峰进行质谱鉴定,离子化模式为正、负离子,离子源温度150℃,脱溶剂气体为高纯度氮气,温度550℃,流速800 L·h~(-1),毛细管电压1.0 kV,锥孔电压30 V,扫描范围m/z 50~1 200。结果:栀子标准汤剂的平均出膏率28.4%,栀子苷转移率77.7%,p H均为4。所有样品的指纹图谱相似度均0.99,栀子标准汤剂的主要成分为栀子苷。结论:建立的栀子标准汤剂的质量评价方法稳定可行、重复性好,该评价方法灵敏、准确,为所有源于栀子水煎剂的制剂的质量控制提供参考。     

眼树莲的化学成分分析

目的:对萝藦科眼树莲Dischidia chinensis全株的化学成分进行分离纯化并对分离得到的单体化合物进行结构鉴定。方法:眼树莲全株干重5.0 kg,粉碎,用95%乙醇室温浸提3次,过滤,合并滤液后经真空减压浓缩得粗浸膏,将其分散于水中成悬浊液,依次用石油醚、乙酸乙酯和正丁醇萃取。运用小孔树脂(MCI),硅胶柱色谱,LH-20羟丙基葡聚糖凝胶(Sephadex LH-20)等柱色谱方法对眼树莲乙酸乙酯萃取物经行分离纯化,应用TLC跟踪监测,分离得到纯度较高的单体化合物。依据各个化合物的理化常数和波谱数据分析对各单体化合物的化学结构进行进一步鉴定。结果:从眼树莲中分离鉴定了10个化合物,分别为β-香树素(1),羽扇豆醇(2),β-香树素乙酸酯(3),3-表木栓醇(4),香草醛(5),4-羟基-3,5-二甲氧基苯甲醛(6),2-羟基-1-(4-羟基-3-甲氧基-苯基)-丙基-1-酮(7),1-(4-hydroxy-3-methoxyphenyl)-1-methoxypropan-2-ol(8),pavonisol(9),S(+)-dehydrovomifoliol(10)。结论:化合物1~10均为首次从眼树莲中分离得到。