ABSTRACT
OBJECTIVE To prepare Gambogic acid （GA） nanocapsules （GA-LNCs） and Neogambogic acid （NGA） nanocapsules（NGA-LNCs），and to evaluate their antidiabetic activities. METHODS Using water as the aqueous phase ，medium- chain triglyceride as the oil phase and polyethylene glycol monostearate as the surfactant ，GA-LNCs and NGA-LNCs were prepared by phase inversion method. Using entrapment efficiency and drug-loading amount as index ，the formulation technologies of above 2 nanocapsules were optimized by simplex lattice design. Its physical and chemical properties were investigated. The diabetic mice model was established. GA-LNCs and NGA-LNCs （1.92 and 2.42 mg/kg respectively ）were given intragastrically ，once a day ，for consecutive 6 weeks. The fasting blood glucose of mice ，the activities of superoxide dismutase （SOD）and glutathione peroxidase （GSH-Px），the contents of malondialdehyde （MDA），total cholesterol （TC），triglyceride （TG），high-density lipoprotein cholesterol（HDL-C）and low-density lipoprotein cholesterol （LDL-C）were all detected. RESULTS The optimal formulation of 2 kinds of nanocapsules included 60％ water，10％ medium-chain triglyceride ，30％ polyethylene glycol monostearate （total amount of the three was 2 g）and 35 mg GA or NGA . The encapsulation efficiencies of GA-LNCs and NGA-LNC obtained by the optimal formulation were （92.01±0.68）％ and（93.12±2.11）％；the drug-loading amount were （0.99±0.21）％ and（1.21±0.22）％， respectively. GA-LNCs and NGA-LNCs were yellow ，homogeneous and transparent liquid without precipitation. They were spherical in microscopic shape ， and had obvious shell- Δ 基金项目：吉林省科技发展计划项目（No.20200404090YY）；吉 membrane structure. The particle sizes were （28.11 ± 9.76） 林省教育厅科学技术研究项目（No.JJKH20210372KJ） ＊硕士研究生 。研究方向 ：植物药 。E-mail：zhanhe0108@163. and（22.06±6.84）nm；Zeta potential were （－4.09±1.00） com and（－17.40±1.32）mV，and polydispersity were 0.93±0.06 # 通信作者：讲师，博士。研究方向：中药有效成分治疗疾病的作 and 0.74±0.12. The results of animal experiments showed that 用机制。E-mail：chenweijia_jlau@163.com both GA-LNCs and NGA-LNCs could sig nificantly increase 中国药房 2022年第33卷第9期 China Pharmacy 2022Vol. 33 No. 9 ·1075· the activities of SOD and GSH-Px and the seru m content of HDL-C （P＜0.05 or P＜0.01）in model mice ，and significantly decreased the fasting blood glucose and the serum contents of MDA ， TC， TG and LDL-C （P＜0.05 or P＜0.01）. CONCLUSIONS GA-LNCs，NGA-LNCs prepared in this study are good in physical and chemical properties and have good anti-diabetes activity.
ABSTRACT
Garcinia, a kind of dry resin secreted by Garcinia hanburyi Hook. F. G., is a traditional Chinese medicine with various biological functions such as detoxification, anti-inflammatory, and anthelmintic activities. Recent studies suggest that garcinia has potential anticancer activity. Increasing evidences indicate that the main active monomer gambogic acid isolated from garcinia can inhibit the growth of various cancer cells. Neogambogic acid is an isolated compound with a similar chemical structure as gambogic acid. Preliminary studies show that the neogambogic acid can selectively inhibit the growth of various cancer cells, and has a broader antitumor activity and lower toxicity than gambogic acid. In this review, we summarize the advances made in the investigation of the anti-tumor effect of neogambogic acid in recent years.
Subject(s)
Animals , Humans , Antineoplastic Agents, Phytogenic , Chemistry , Garcinia , Chemistry , Neoplasms , Drug Therapy , Plant Extracts , Chemistry , Xanthenes , ChemistryABSTRACT
Garcinia, a kind of dry resin secreted by Garcinia hanburyi Hook. F. G., is a traditional Chinese medicine with various biological functions such as detoxification, anti-inflammatory, and anthelmintic activities. Recent studies suggest that garcinia has potential anticancer activity. Increasing evidences indicate that the main active monomer gambogic acid isolated from garcinia can inhibit the growth of various cancer cells. Neogambogic acid is an isolated compound with a similar chemical structure as gambogic acid. Preliminary studies show that the neogambogic acid can selectively inhibit the growth of various cancer cells, and has a broader antitumor activity and lower toxicity than gambogic acid. In this review, we summarize the advances made in the investigation of the anti-tumor effect of neogambogic acid in recent years.
Subject(s)
Animals , Humans , Antineoplastic Agents, Phytogenic , Chemistry , Garcinia , Chemistry , Neoplasms , Drug Therapy , Plant Extracts , Chemistry , Xanthenes , ChemistryABSTRACT
Objective To develop a double-wavelength HPLC method for the simultaneous determination of neogambogic acid,gambogic acid,( +)-catechin and L-epicatechin in Litong pill. Methods The quantitative analysis was carried out on C18 column(250 mm×4.6 mm,5 μm).A linear elution of methanol-acetonitrile(4: 1)and 0.2% phosphoric acid solution was adopted at the flow rate of 1.1 mL·min-1 ,with the detection wavelength set at 360 nm for neogambogic acid and gambogic acid,and at 280 nm for(+)-catechin and L-epicatechin. Results The linear ranges of neogambogic acid,gambogic acid,(+)-catechin and L-epicatechin were 5.85-117.00 μg·mL-1(r= 0.999 5),8.95-179.00 μg·mL-1(r= 0.999 8),6.90-138.00 μg·mL-1(r= 0.999 7),and 5.30-106.00 μg·mL-1(r = 0.999 9),respectively.The average recoveries were 97.82%(RSD= 1.21%),98.72%(RSD = 1.30%),96.96%(RSD = 0.84%)and 99.26%( RSD = 1.46%)for neogambogic acid, gambogic acid,(+)-catechin and L-epicatechin,respectively. Conclusion The method is simple,accurate,reproducible and may be used for the simultaneous determination of neogambogic acid,gambogic acid,(+)-catechin and L-epicatechin in Litong pill.