An innovative extraction strategy for herbal medicine by adopting p-sulphonatocalix[6]/[8]arenes.

INTRODUCTION: Alkaloids exist in various herbal medicine widely and exhibit diverse biological and pharmacological activities. p-Sulphonatocalix[6]arenes (SC6A) and p-sulphonatocalix[8]arenes (SC8A) are water-soluble supramolecular macrocycles and are applied to the extraction of alkaloids from herbal products. OBJECTIVE: In this study, an innovative method of SC6A/SC8A assisted extraction of the alkaloids from herbs was established. METHODS: SC6A and SC8A were designed to extract 27 alkaloids from seven herbal medicines. Based on the significant solubilisation and extraction effect, Stephaniae Tetrandrae Radix (Fangji, FJ) was selected to obtain the optimal extraction process by adopting single factor test and orthogonal experiment. Then, the alkaloids and SC6A/SC8A were separated by one-step alkalisation and SCnA were reused. The host-guest complexes between alkaloids and SCnA were determined by competitive fluorescence titration, differential scanning calorimetry (DSC), Fourier-transform infrared (FTIR) and proton nuclear magnetic resonance (1 H-NMR) analysis. RESULTS: The optimum condition for SC6A assisted extraction was 5:1:80 (g/g/mL) for herbs/SC6A/solution ratio, 355-250 µm particle size and ultrasonicate 0.5 h, whilst 10:1:40 (g/g/mL) for herbs/SC8A/solution ratio, 355-250 µm particle size and ultrasonicate 0.5 h for SC8A assisted extraction. The total yield of alkaloids (fangchinoline and tetrandrine) from FJ was increased by 4.87 times and 5.97 times with SC6A and SC8A. Moreover, a good reusability of SC6A/SC8A was achieved by alkalisation dissociation. Host-guest complexes were determined by competitive fluorescence titration at a molar ratio of 1:1 between most alkaloids (25/27, except evodiamine and rutaecarpine) and SC6A/SC8A. The complex structure was proved by DSC, FTIR and 1 H-NMR analysis. CONCLUSION: The study provided an effective eco-friendly and energy-saving extraction method of alkaloids from herbal medicine.

An eco-friendly extraction and purification method of nuciferine from Folium nelumbinis with p-sulfonatocalix[6]arenes.

INTRODUCTION: Folium nelumbinis is used as vegetable, functional food and herbal medicine in Asia. p-Sulfonatocalix[6]arene (SC6A) is a water-soluble supramolecular macrocycle and has never been applied to the extraction of herbal products. OBJECTIVE: In this study, SC6A-assisted extraction of nuciferine from Folium nelumbinis has been carried out to develop an eco-friendly extraction process with high extraction efficacy and easy operation. METHODS: Single-factor experiments were adopted to obtain the optimal conditions for the SC6A-assisted extraction of nuciferine from Folium nelumbinis, and then nuciferine and SC6A were separated easily by one-step alkalization. The host-guest complexes between nuciferine and SC6A were analyzed by competitive fluorescence titration, DSC, FT-IR and 1 H-NMR. RESULTS: The optimal SC6A/Folium nelumbinis/solution ratio for extraction was 0.4:1:20 (g/g/mL), with a granulometric fraction below 180 µm and an extraction time of 1 h with soaking. The purity and recovery of nuciferine extracted with SC6A were increased 29.24 and 35.73 times compared with extraction with aqueous solution, respectively. Moreover, a good reusability of SC6A in the extraction of nuciferine was demonstrated. Competitive fluorescence titration, DSC, FT-IR and 1 H-NMR characterization indicated that SC6A could form host-guest complexes with nuciferine at a ratio of 1:1. CONCLUSION: The study provided an eco-friendly, safe and effective nuciferine extraction method, which can be used for the development of nutrition supplements containing nuciferine.

[Chemistry and biology research on bitter-taste Chinese materia medica with function of regulating glycolipid metabolism].

The bitter taste is one of the important properties among five flavors of Chinese materia medica (CMM), characterized by downbearing and discharging, drying dampness, and consolidating Yin. In common CMM, bitter-taste CMM accounts for a large proportion, indicating the importance of it. Through the efficacy of clearing away heat and dampness, reducing fire and removing toxin, bitter-taste CMM has achieved good results in treating diabetes in clinical application, proving their definite therapeutic effect on regulating glucose and lipid metabolism (main features of diabetes). At present, there are many reports about the chemical constituents and pharmacological effects of CMM on diabetes, but there are few reviews on the chemistry and biology of bitter-taste CMM. This study summarized the properties and compatibility characteristics of bitter-taste CMM for treating diabetes, and mainly analyzed the chemistry and biology basis of bitter-taste CMM with function of regulating glycolipid metabolism, laying foundation for further researches on properties theory of CMM.

Rapid characterization of the absorbed chemical constituents of Tangzhiqing formula following oral administration using UHPLC-Q-TOF-MS.

Tangzhiqing formula, a Chinese herbal formula, is used for the treatment of type II diabetes and prediabetes. Although its effectiveness has been certified by clinical use, its absorbed chemical constituents are not comprehensively represented. Thence, in order to reveal potential bioactive components and metabolism of Tangzhiqing formula, an ultra-high performance liquid chromatography with quadrupole time-of-flight mass spectrometry method was developed. A total of 86 absorbed components, including 38 prototype compounds and 48 metabolites, were identified in rat plasma, urine, and feces after oral administration of Tangzhiqing formula. This was the first systematic study on the chemical constituents and metabolic profiling of Tangzhiqing formula. The results indicated that alkaloids and flavonoids were main absorbed components, and glucuronidation and sulfation were the major metabolites. Moreover we concluded that alkaloids and flavonoids first underwent demethylation and hydrolysis reactions before biotransformed to phase II metabolites. This study provided valuable data for safety estimation of Tangzhiqing formula, which will be advantageous for clinical application.

[In vitro transdermal behavior of effective constituents in Chonghe gel].

Chonghe gel originated from the Chinese ancient prescription, can be used for the treatment of diabetic foot. This experiment was to study the transdermal absorbability of paeoniflorin and osthole in Chonghe gel . Franz diffusing cells method was adopted for the in vitro model of rat belly skins. Paeoniflorin and osthole in the receiving liquid, skins and gel were determined by HPLC. The receiving liquid were screened, and Chonghe gel and Chonghe ointment were compared by transdermal absorbability. Result showed that ethanol-normal saline (2: 8) solution was the appropriate receiving liquid. The penetration rates of paeoniflorin and osthole were 78.07, 7.08 microg x cm(-2) x h(-1). respectively. In 24 h, the accumulated penetration rates were (31.51 +/- 1.33)%, (12.38 +/- 1.28)%, respectively. The retention rates of paeoniflorin and osthole in skin were (0.92 +/- 0.45)%, (4.81 +/- 1.03) %, respectively. The retention of osthole in skins was a drug reservoir. Transdermal behavior of effective constituents in Chonghe gel was more efficient than that in ointment. In vitro, the transdermal behavior of paeoniflorin in Chonghe gel was close to a Weibull process, while the behavior of osthole was close to Higuchi process.

[Present situation and prospect of quality standardization of Chinese patent medicines].

This article reviews rectification and protection of Chinese patent medicines, establishment and improvement of the new drug approval, and historical evolution of the pharmacopoeia of the People's Republic of China. The article analyzes the present situation and the challenges of quality standardization of Chinese patent medicines in the new era. The article also points out strategies and guidelines to be taken to promote the globalization of Chinese patent medicines and compliance with the international standards.

[Effects of Qilan Tangzhining capsule on glucose and lipid metabolism in rats with diabetes mellitus and hyperlipemia].

OBJECTIVE: To study the effects of Qilan Tangzhining capsule on glucose and lipid metabolism in diabetes mellitus and hyperlipemia. METHOD: Rats were fed with high sugar and fat food for 2 months, then 2% streptozocin (STZ, 30 mg kg(-1)) was injected intraperitoneally to induce hyperglycemia and hyperlipemia. After the model rats were administrated drugs, the blood glucose, the serum lipids, and the histopathology of the liver and pancreas were observed. RESULT: Qilan Tangzhining capsule could decrease the FBG and the serum TC, TG, LDL-C, increase HDL-C, and improve the histopathologic injury of the liver and pancreas. CONCLUSION: Qilan Tangzhining capsule can not only adjust the blood glucose and lipid, but also improve the histopathology injury of the liver and pancreas.

[Effects of Guanyu capsule on the behavior and cerebral cortex monoamine neurotransmitters in depressive model of olfactory bulb damage rats].

OBJECTIVE: To investigate the behavioral changes and the levels of monoamine neurotransmitters in the anterior cortex in the olfactory bulb damage rats after being treated with Guanyu capsules (GYC). METHOD: Open-field test and step-down passive avoidance test were used to observe the behavior in model rats. HPLC-ECD was used to analyze the influences of GYC on the levels of monoamine neurotransmitters. RESULT: In the model rats, there was a characteristic hyperactivity in the Open-field and learning deficits in step-down passive avoidance (P < 0.01). The contents of 5-HT reduced, and the rate of DOPAC/DA increased significantly (P < 0.01). GYC 1.2, 0.6 g x kg(-1) could correct behavioral changes increase the contents of 5-HT, and decrease DOPAC/DA level (P < 0.01). CONCLUSION: GYC can correct behavioral changes in rats model of olfactory bulb damage, and regulating 5-HT and DA metabolism in cortex is one of the antidepressive mechanisms of GYC.