Preparation of triptolide nano liposome thermosensitive gel and its penetrability through nasal mucosa / 中草药

Objective To prepare nasal triptolide nano liposome thermosensitive gel (TP-NLS-TG) and investigate the in vitro penetrability through nasal mucosa. Methods The triptolide nanoliposomes were prepared by high pressure homogenization method, and the ratio of poloxamer 407 (P-407) and poloxamer 188 (P-188) was selected, using the azone dosage and stirring time as investigation factors. Gelation temperature (GT) and homogeneity of TG (RSD) were used as evaluation indexes, and TP-NLS-TG was prepared by optimized prescription. An isolated mucosal permeability model was established by frog abdominal skin to carry out the in vitro permeation test of TP-NLS-TG in nasal mucosa. Results The best prescription was 12% P-407, 10% P-188, and 3% azone, and swelling time was 4 h. The TP-SLN gelation temperature of the gel was 32 ℃, and the RSD was 0.005%. In the first 8 h, the cumulative infiltration volume per unit area was (9.296 3 ± 0.614 7) μg/cm2, and the release curve in line with the Higuchi mathematical model. Conclusion The triptolide nano liposome gel prepared by the optimum technology has an accurate gelling temperature, and uniform content, which has good permeability, can be absorbed through the frog skin.

Prescription of triptolide nanometer liposomes and its preparation technology / 中草药

Objective: To optimize the preparation method of triptolide-nano-liposomes (TP-NLS). Methods High pressure homogeneous method was used to prepare TP-SLN. According to even design U7(73), the preparation method of TP-SLN was optimized with the factors including weight ratio of phosphorlipid and cholesterol (A), quantity of Poloxamer 188 (B), and homogeneous pressure (C), using the encapsulation efficiency (EE), particle size, and Zeta potential of NLS as indexes. Results: The optimum prescription of TP-NLS was A1B5C7, i.g. lipid matrix a : b was 6 : 1, the dosage of Poloxamer 188 was 1.3 g, and the homogeneous pressure was 70 MPa, high pressure homogeneous method for 15 min. The TP-NLS prepared with the optimal method had good appearance. The EE was 83.52%, the average particle size was 117 nm, and the Zeta potential was 31.7 mV. TP-NLS solution was kept in avoiding light environment at 4℃ for 30 d, and the preservation stability was good. Conclusion: The formula is reasonable and the preparation method of TP-NLS is feasible, which is valuable to further study.

Preparation of triptolide nanometer coating agent / 中草药

Objective: To explore the optimum preparation process of triptolide nanometer coating agent. Methods: Optimum preparation process was investigated by uniform design with the amount of film forming material such as polyethylene glycol 124 (PVA124), carbomer, CMC-Na, and the mixing time as investigating factors, and with uniformity, film-forming ability, and peeling strength as indexes. We conducted sc simulation experiment in vitro to investigate the percutaneous penetration process of triptolide nanometer coating agent. Results: The best way to prepare triptolide nanometer coating agent is that we use glycerol monostearate 1.6 g, glycerin 0.25 g, PVA124 3.9 g, Carbomer 0.6 g, CMC-Na 0.9 g, and mix them in 150 min. With above preparation process, we can achieve better coating agent. JS was 0.350 µg/(cm2·h) and the cumulative permeation quantity in 24 h was 11.534 µg/cm2. Conclusion: Using the optimum preparation process, we can get better triptolide nanometer coating agent, which is uniform, easy coating,good adhesion with skin, strong flexibility, and drying soon.

Reproductive toxicity of triptolide and its mechanism in male rats / 中国中药杂志

The arrenotokous toxicity of triptolide was evaluated, and the rate of sperm abnormality, the changes of the lipid peroxide, the enzyme activity and the hormone in male rats were observed. With the negative and positive control group, the healthy rats were respectively given by gavage triptolide suspension at the dose of 0.025, 0.05, 0.1 mg x kg(-1) for 30 days. Then the rats were killed for the measurement of the indicators in testis and serum, as well as the study on the sperm abnormality. The results showed that the positive control group had significant difference, compared with the negative control group. The content of SOD, LDH, G-6-PD, Na+ -K+ -ATPase, Ca+ -Mg+ -ATPase decreased significantly in 0.05 mg x kg(-1) group, and reduced more obviously with exposure to the dose of 0.1 mg x kg(-1). The levels of GSH-Px and beta-G showed a significant decrease in the testis of rats only at the dose of 0.1 mg x kg(-1). Nevertheless, the MDA levels, the FSH levels and the LH levels showed no significant difference. The deformity rate of sperm increased significantly in 0.05 mg x kg(-1) group and 0.1 mg x kg(-1) group. The results indicated the triptolide had the effect of the lipid peroxidation to damage Spermatogenic cells, Sertolis cells and Leydig cells. At the same time, the triptolide interfered not only with the energy supply process of aerobic and anaerobic glycolysis,but also with the energy utilization in testis by affecting the activities of testis marker enzymes, and produced a damage chain of the male reproductive system

Diterpene constituents of Tripterygium willfordii (II) / 药学学报

In order to study the constituents and pharmacology of Tripterygium plants (Tripterygium willfordii Hook.f), a variety of chromatography methods were used. Four compounds were isolated from Tripterygium plant and their structures were elucidated by UV, IR, MS, HR-MS, 1H NMR, 13C NMR and 2D-NMR techniques. The isolated compounds were named as triptonide (1), neo-triptetraolide (2), 2alpha-hydroxytriptonide (3), and 15-hydroxytriptonide (4), separately. Compounds 3, 4 belong to new diterpenoids, which can inhibit the growth of K562 cells (leukemia cells) and HL60 cells (acute myeloid leukemia cells).

Diterpenes constituents of Tripterygium wilfordii / 药学学报

<p><b>AIM</b>To study the chemical constituents of Tripterygium wilfordii Hook. F.</p><p><b>METHODS</b>Various column chromatographies with silica gel were used for the isolation and purification. The structures of compounds were established on the basis of its IR, MS, UV, 1H NMR, 13C NMR and HRMS, 1H-1H COSY, 1H-13C COSY and NOESY.</p><p><b>RESULTS</b>Four diterpenoids were isolated: 16-hydroxytriptolide (I), triptolidenol (II), tripdiolide (III), 2-epitripdiolide (IV).</p><p><b>CONCLUSION</b>Compound IV is a new diterpenoid.</p>