[Influence of processing factors on honey-fried Codonopsis Radix].

The present study investigated the influence of heating and honey addition on the appearance, chemical component content, and pharmacological activity of Codonopsis Radix decoction pieces in the honey-frying process, and explored the processing mechanism of honey-fried Codonopsis Radix. The color, sweetness, and content of macromolecular components(e.g., oligosaccharides and polysaccharides) and small molecular components(e.g., lobetyolin and atractylenolide Ⅲ) of raw Codonopsis Radix, fried Codonopsis Radix, honey-mixed Codonopsis Radix, and honey-fried Codonopsis Radix were determined, and the antioxidant activities in vitro of their water extract, polysaccharide extract, and oligosaccharide extract were compared. The results showed that in terms of color and sweetness, compared with the raw Codonopsis Radix, the fried Codonopsis Radix slightly changed, the honey-mixed Codonopsis Radix changed significantly, and the honey-fried Codonopsis Radix changed with high significance. In terms of the content of lobetyolin, atractylenolide Ⅲ, and polysaccharides, the samples were ranked as raw Codonopsis Radix > fried Codonopsis Radix > honey-mixed Codonopsis Radix > honey-fried Codonopsis Radix, which indicated that heating and honey addition could reduce the content of these three components. In terms of the content of oligosaccharides, the samples were ranked as honey-fried Codonopsis Radix ≈ honey-mixed Codonopsis Radix > fried Codonopsis Radix ≈ raw Codonopsis Radix, indicating that honey addition could increase the content of oligosaccharides. In terms of antioxidant activity in vitro, ABTS radical scavenging ability of water extract, polysaccharides, and oligosaccharides of honey-fried Codonopsis Radix was most potent, while the change of antioxidant activity in vitro of each extract in the other three processed products was different. In short, both heating and honey addition can affect the appearance, chemical component content, and antioxidant activity in vitro of Codonopsis Radix decoction pieces, but the effect of the combination of the two factors is the best. The comprehensive analysis of the effects of heating and honey addition on Codonopsis Radix decoction pieces indicates that honey addition followed by heating at high temperature is the necessary condition for honey-fried Codonopsis Radix to enhance its activity.

Gallic Acid Inhibits Mesaconitine-Activated TRPV1-Channel-Induced Cardiotoxicity.

Aconiti Kusnezoffii Radix (Caowu) is often combined or processed with Chebulae Fructus (Hezi) to achieve attenuation purposes in Mongolian medicine. Mesaconitine (MA), a main bioactive ingredient of Caowu, is also famous for its high cardiotoxicity while exerting good anti-inflammatory and analgesic properties. Gallic acid (GA), one of the leading chemical components in Hezi, possesses cardiac protection. This study aimed to clarify the detoxification effects of GA from Hezi on MA-induced cardiotoxicity and whether the detoxification mechanism is related to the TRPV1 channel. Cell viability was determined by methyl thiazol tetrazolium (MTT), and lactate dehydrogenase (LDH) leakage rate was determined by ELISA. Hoechst 33258, JC-1, DCFH-DA, and Fluo-3 AM staining were conducted to detect apoptosis, mitochondrial membrane potential, reactive oxygen species (ROS), and Ca2+ respectively; TRPV1 channel current was recorded by whole-cell patch-clamp technology to observe the effect of GA and MA alone or in combination on TRPV1 channel. The results showed that GA exhibited pronounced detoxification effects on MA-induced cardiotoxicity. GA significantly inhibited the MA-induced decrease in cell viability; suppressed the MA-induced LDH leakage rate, apoptosis, and the release of ROS and Ca2+; and alleviated the reduction of mitochondrial membrane potential. We found that MA-induced cardiotoxicity was significantly attenuated in H9c2 cells pretreated with the TRPV1 antagonist BCTC. In the whole-cell patch-clamp experiment, the TRPV1 channel current increase was caused by the GA and MA treatment, whereas it was reduced by the cotreatment of GA and MA. Our data demonstrate that GA in Hezi can reduce MA-induced cardiotoxicity by inhibiting intracellular Ca2+ influx, restoring mitochondrial membrane potential, and reducing apoptosis. The detoxification mechanism may be related to the desensitization of the TRPV1 channel by the combined application of MA and GA.

Changes of Mineralogical Properties and Biological Activities of Gypsum and Its Calcined Products with Different Phase Structures.

Raw gypsum (RG) and calcined gypsum (CG) are widely used in traditional Chinese medicine (TCM). RG is usually taken orally to resolve heat and diminish inflammation, while CG is only used externally to treat ulcerations and empyrosis. Calcination at different temperatures, three phase CG structures, namely, bassanite, anhydrite III, and anhydrite II, may be generated. We herein investigated the relationship between the phase structure and the efficacy of CG and the optimum phase structure for CG. RG has a compact structure, small pore size, weak anti-inflammatory effect, but no antibacterial effect, and has almost no effect on the repair of scalds. CG150 (bassanite) has a loose texture, large pore size and specific surface area, and certain antibacterial and anti-inflammatory effects, but it has a poor repair effect on scalds. CG750 (anhydrite II) has a compact structure, small pore size and specific surface area, and low antibacterial and anti-inflammatory effects, but it has a certain repair effect on scalds. Only CG350 (anhydrite III) has good performance in texture, pore size, specific surface area, antibacterial, anti-inflammatory, and scald repair. Our research has proved that the mineral properties and biological activities of CG are different due to different phase structures. CG350, namely, anhydrite III, is considered by our research to be the optimal phase structure as CG.

Influence of Different Dosage Forms on Pharmacokinetics of 6 Alkaloids in Raw Aconiti Kusnezoffii Radix (Caowu) and Chebulae Fructus- (Hezi-) Processed Caowu by UPLC-MS/MS.

PURPOSE: To study the pharmacokinetics of the 6 alkaloids (aconitine, mesaconitine, hypaconitine, benzoylaconine, benzoylmesaconine, and benzoylhypaconine) in raw Aconiti Kusnezoffii Radix (Caowu) (RC) and Chebulae Fructus- (Hezi-) processed Caowu (HC) in the rats being, respectively, administrated with RC and HC in the dosage forms of powder and decoction and to demonstrate the mechanism of detoxification of HC. METHODS: The rats were randomly divided into 4 groups and, respectively, given RC powder, HC powder, RC decoction, and HC decoction by intragastric administration. The contents of the 6 alkaloids in the plasma of the rats were detected at different time points by the UPLC-MS/MS method, and DAS 3.2.7 software was used to calculate, compare, and analyze the detected pharmacokinetic parameters. RESULTS: Compared with those of the RC powder, the values of AUC0-t and C max of the HC powder were all reduced, whereas the values of t 1/2z and T max were mostly increased. Compared with those of the RC powder, the values of AUC0-t , C max, and t 1/2z of the RC decoction were decreased and the value of T max of the RC decoction was increased. Compared with those of the RC decoction, the values of AUC0-t , t 1/2z , and C max of the diester diterpenoid alkaloids of the HC decoction were all increased. However, there was no marked difference between the pharmacokinetic parameters of the HC powder and the HC decoction. CONCLUSIONS: A decrease in the level of absorption and in the rate of elimination of the alkaloids can be detected when HC is administrated in the dosage form of the powder, explaining that in traditional Mongolian medicine (TMM), the purpose of using HC in the dosage forms of pills and powder is for decreasing the toxicity and prolonging the efficacy duration of HC. Decocting can greatly decrease the plasma concentration of the diester diterpenoid alkaloids in RC and increase their rate of elimination. The influence of decocting on RC is greater than that on HC, explaining the rationality of the steaming and boiling methods for processing Caowu and the rationality of boiling Caowu for a longer time beforehand in preparing an herb decoction containing Caowu in TCM.

[Chemical variation in Aconti Kusnezoffii Radix before and after processing based on UPLC-Orbitrap-MS].

Some Chinese herbal medicine needs to be processed before it can be used as medicine, especially toxic Chinese medicine. Highly toxic Aconti Kusnezoffii Radix(Caowu in Chinese) is widely used in traditional Chinese medicine and Mongolian medicine. In traditional Chinese medicine, Caowu is usually processed by boiling with water(CW) until no white part inside and being tasted without tongue-numbing. In Mongolian medicine, it is usually soaked in Chebulae Fructus(Hezi in Chinese) decoction for several days(CH). Both methods could reduce toxicity according to reports. The biggest difference between CW and CH is that CW needs to be heated for 4-6 h, while CH needs Hezi as processing adjuvants. To explore the toxicity reduction mechanism of CW and CH, we studied the contents of various compounds in Caowu processed by two methods by UPLC-Orbitrap-MS. The results indicated that CW had 14 new ingredients, such as 14-O-anisoylneoline and dehydro-mesaconitine, while N-demethyl-mesaconitine and aconitine disappeared. At the same time, it could significantly decrease the content of diester diterpenoid alkaloids and increase the contents of monoester diterpenoid alkaloids and amine-diterpenoid alkaloids. CH had 9 new ingredients from Hezi, like gallic acid, chebulic acid and shikimic acid. Neither the kinds nor the contents of compositions from Caowu in CH changed little. This suggested that the processing mechanism of CW reduced highly toxic components(diester diterpenoid alkaloids) and increased the content of lowly toxic components(monoester diterpenoid alkaloids and amine-diterpenoid alkaloids). Attenuated principle of CH may be related to the components of Hezi. In this experiment, the conclusion shows that the chemical constituents of CW and CH are essentially different, and the two methods have different toxicity reduction principles.