“Liquid seal to detoxification – drying and puffing” of two stage processing technology design and pharmacodynamic study of aconite (Aconiti Lateralis Radix Praeparata) processed by microwave / 药学学报

Establish a production line with controllable process and high intelligence, contribute to improve the quality and production efficiency of aconite processed by microwave, and promote the transformation and application of aconite processed by microwave. According to the principle of aconite detoxification and the characteristics of industrial microwave equipment, an industrial production line of aconite processed by microwave was established with diester alkaloids and monoester alkaloids as indicators, and pilot production was carried out. At the same time, the content of active constituents and efficacy were compared with that of the main processed products, such as Shengfupian, Baifupian and Heishunpian. The results showed that the industrial production of aconite processed by microwave can be divided into two stages: "Liquid seal to detoxification - drying and puffing". The content of monoester alkaloids in 10 batches of aconite processed by microwave was 0.071%-0.166% and the content of diester alkaloids was 0.004%-0.016%, which met the relevant requirements of the Chinese Pharmacopoeia in 2020. Compared with Heishunpian and Baifupian, the retention rate of the effective components of aconite processed by microwave was higher. Pharmacological experiments showed that aconite processed by microwave not only retained the anti-inflammatory and analgesic activities of Heishunpian and Baifupian, but also significantly increased the levels of leukocytes and lymphocytes in mice with liver cancer chemotherapy, enhanced the CD4/CD8 ratio in spleen cells of mice (P < 0.05), thus regulating the body's immunity. However, this effect of Baifupian was weak, while Heishunpian and Shengfupian had no such effect. Through the above research, this study established microwave processing line with controllable process and high intelligence, as well produced the aconite processed by microwave with low toxicity and stable quality. It laid a foundation for the industrialized continuous production and clinical positioning of aconite by microwave processed, and provided scientific support for the development and application of microwave technology in the field of traditional Chinese medicine. All animal experiments in this study were reviewed and approved by the Experimental Animal Ethics Committee of Chengdu University of Traditional Chinese Medicine before being carried out (Approval No. 2020-28).

Optimization of extraction of flavonoids from Lonicera rupicola and analysis of its effects in resisting inflammation, relieving pain, enhancing immunity, and inhibiting pyroptosis / 中国中药杂志

The present study optimized the extraction of flavonoids from Lonicera rupicola Hook. f. et Thoms(LRH) and explored its pharmacological effects, such as resisting inflammation, relieving pain, enhancing immunity, and inhibiting pyroptosis, aiming to provide data support and scientific basis for the development and utilization of LRH. Response surface methodology(RSM) was applied to optimize the extraction of flavonoids from LRH based on the results of single-factor experiments. Anti-inflammatory and analgesic effects of LRH flavonoids were evaluated via inflammation and pain models in mice, such as xylene-induced ear swelling, carrageenan-induced footpad swelling, writhing caused by acetic acid, and paw licking. The effect of LRH flavonoids on the carbon clearance index of monocytes and serum immunoglobulin A(IgA) and IgM levels was analyzed on the immunosuppression model induced by cyclophosphamide in mice. The anti-oxidative effect in vivo of LRH flavonoids on liver superoxide dismutase(SOD), catalase(CAT), and malondialdehyde(MDA) levels was determined based on the chronic/subacute aging model in mice induced by D-galactose. The levels of cysteinyl aspartate specific proteinase-1(caspase-1), interleukin-1β(IL-1β), and IL-18 in the supernatant of J774 A.1 mononuclear phagocytes were detected to evaluate the effect of LRH flavonoids on the pyroptosis of mononuclear phagocytes in mice induced by the combination of lipopolysaccharide(LPS) and adenosine triphosphate(ATP). Meanwhile, the effect of LRH flavonoids on the cAMP-PKA signaling pathway was also explored. The optimum conditions for the extraction of LRH flavonoids are listed below: extraction temperature of 65 ℃, the ethanol concentration of 50%, extraction time of 60 min, a material-liquid ratio at 1∶25, and the yield of LRH flavonoids of 0.553%. RSM determined the multiple quadratic regression equation model of response value and variables as follows: the yield of LRH flavonoids=0.61-0.48A+0.1B+0.029C-0.014D+0.32AB+0.04AC-0.012AD-0.02BC+0.037BD-0.031CD-0.058A~2-0.068B~2-0.069C~2-0.057D~2. LRH flavonoids could effectively inhibit ear swelling and footpad swelling, reduced acetic acid-induced writhing, and delayed the paw licking response time in mice. Additionally, LRH flavonoids could improve the carbon clearance index in immunosuppressed mice, potentiate the activities of SOD and CAT and reduce MDA levels in the liver of aging mice induced by D-galactose, and effectively inhibit macrophage pyroptosis by decreasing the levels of caspase-1, IL-1β, and IL-18. The results reveal that LRH flavonoids possess excellent pharmacological activities such as resisting inflammation and oxidation, relieving pain, and enhancing immunity. They can inhibit pyroptosis by enhancing the cAMP-PKA signaling pathway. The results of this study can underpin the pharmacological research, development, and utilization of LRH.

Anti-inflammatory and analgesic activity analysis of Yinlian Tongfeng granules based on network Pharmacology / 药学实践杂志

Objective To explore the anti-inflammatory and analgesic mechanism of Yinlian Tongfeng granules by network pharmacology. Methods Three main active components of Yinlian Tongfeng granules were collected from TCMSP database to predict its effective targets. Based on the network information of active components and targets, the anti-inflammatory and analgesic related targets were established by using protein-protein interaction information. The enrichment analysis of KEGG biological pathway and go function enrichment were carried out to construct the active component-target-signal pathway network and explain the main mechanism of anti-inflammatory and analgesic. Results 37 targets were closely related to anti-inflammation and analgesic effects of Yinlian Tongfeng granules, mainly on Prostaglandin endoperoxide synthase 2(PTGS2), interleukin-6 (IL-6), interleukin-10 (IL-10) and tumor necrosis factors (TNF). The mechanism of action may relate to the regulation of nuclear transcription factor B signaling pathway(NF-κB). Conclusion The study predicted the anti-inflammatory and analgesic mechanism of Yinlian Tongfeng granules, and provided theoretical basis for further verification and interpretation of its mechanism.

Research progress on biological activities and mechanism of betulinic acid and their derivatives / 中草药

Betulinic acid is a natural pentacyclic pentane triterpenoid, usually isolated from the bark of Betula platyphylla, or in the form of free glycosides and glycosyl derivatives in various plants. A variety of derivatives can be obtained by modifying its chemical structure. Betulinic acid and its derivatives have certain regulatory effects in anti-tumor, antiviral, anti-inflammatory, analgesic, inhibition of cerebral nerve and vascular injury, and treatment of other common diseases. The category, pharmacological activities and related mechanisms of betulinic acid and its derivatives are reviewed in this paper, in order to provide a theoretical reference for the future application.

Anti-inflammatory and analgesic activity analysis of Qizhi Weitong Granules based on network pharmacology / 中草药

Objective: The target of anti-inflammatory and analgesic active components of Qizhi Weitong Granules was predicted by network pharmacology method, and the effect of multi-component-multi-target-multi-pathways on TCM-complexation theory was analyzed. Methods: The main chemical constituents of six Chinese medicines in Qizhi Weitong Granules were collected based on the TCMSP Chinese Medicine System Biological Analysis Database and analyzed by LC-MS. The main target of each component was predicted by TCMSP search and Pharmmapper software. The relationship between drug, target and inflammatory pain target was established by DIP database and protein interaction information. In order to elucidate the main mechanism of anti-inflammatory and analgesic effects of Qizhi Weitong Granules, the network of “drug-target-disease” was constructed and the target of anti-inflammatory and analgesic effects of Qizhi Weitong Granules were analyzed by network characteristics. Results: Through the network analysis, a total of 44 inflammatory targets were closely related to Qizhi Weitong Granules, of which 20 were directly targeted, mainly for the action of proteases such as COX-2 and iNOS. The mechanism may be related to the regulation of TNF signaling pathway, NOD-like receptor signaling pathways, VEGF signaling pathways and other signaling pathways closely related to inflammation. Conclusion: The anti-inflammatory and analgesic effects of Qizhi Weitong Granules reflect the multi-component, multi-target and multi-pathway characteristics of traditional Chinese medicine. This study provides a scientific basis for further understanding the anti-inflammatory and analgesic mechanism of Qizhi Weitong Granules and explains the scientificity of the traditional Chinese medicine compatibility theory.

Research progress on chemical constituents of marine medicine Ipomoea pes-caprae and their pharmacological activities / 中草药

Ipomoea pes-caprae, the plant of Ipomoea (Convolvulaceae), is the marine medicine growing in the intertidal zone of coasts. It is not only the Jing nationality medicine in the southern coastal areas of China, but also the folk medicine in the tropical and subtropical countries such as Australia, Mexico, Thailand, Brazil, and Pakistan. It is resource-rich and widely used. The main compounds contain resin glycosides, terpenoids, phenolic acid, flavonoids, volatile oils, and steroids. Pharmacological studies have been reported that I. pes-caprae has a variety of pharmacological activities, such as antitumor, antibiosis, anti-inflammatory and analgesic, anticollagenase, anti-oxidation, immun regulation, and other activities. The recent study on chemical composition and pharmacological activities of I. pes-caprae are summarized in this paper to provide reference for the clinical application, quality control and product development of the marine medicine.

Anti-inflammatory and analgesic activities of ethanol extract of Toddalia asiatica / 中成药

AIM To study the anti-inflammatory and analgesic activities of ethanol extract of Toddalia asiatica Lamn.and the mechanism.METHODS Both inflammatory rat model induced by carrageenan and pain model induced by formalin were applied to investigating the analgesic effect of extract of Toddalia asiatica Lam.ELISA kit was used to detect the contents of β-EP,5-HT and PGE2 in serum of carrageenan-treated rats,contents of TNF-αand IL-1β in skin tissue of inflammatory rats,and content of LTB4 in serum of formalin-treated rats;immunohistochemical method was used to observe the SP and FOS protein expressions in rat spinal cord.RESULTS The ethanol extract of Toddalia asiatica Lam.could significantly reduce the rate of toe swelling.In the formalin test,the ethanol extract of Toddalia asiatica Lam.reduced not only the total licking time,but also the content of PGE2,especially in the high dose group.And lowered serum 5-HT contents were observed in all the three dose groups,but a much better performance was found in both the high and low dose groups,and the high dose group's capability in increasing serum β-EP content was also noticed.TNF-α and IL-1β contents in skin tissue were reduced in various dose groups.Middle and high dose groups inhibited FOS protein expression.And the content of LTB4 in serum was obviously decreased in the high dose group.CONCLUSION The anti-inflammatory and analgesic activities of ethanol extract of Toddalia asiatica Lam.may associate with its power in increasing β-EP in serum,decreasing PGE2,5-HT,LTB4 contents,reducing TNF-α,IL-1β contents in skin tissue,and lowering SP and FOS protein expressions in spinal cord.

Research progress on chemical constituents from Bacopa monnieri and their pharmacological activities / 中草药

The revelant literatures about chemical constituents from the plant Bacopa monnieri and their pharmacological activities were consulted and summarized. The plant contains major chemical compounds including triterpenoids and their glycosides, flavonoids, phenylethanoid glycosides and sterols. It has the impact on central nervous system, cardiovascular system, digestive system, respiratory system and endocrine system, in addition to anti-inflammatory, analgesic, anti-oxidation, hypoglycemic, antitumor, anti-microbial and liver and kidney protection and other pharmacological activities. This paper reviewed the chemical compositions and pharmacological activities, and provided a scientific basis for further research and development of the plant.

Exploration on extraction and enrichment process of anti-inflammatoryand analgesic active-fraction(ARF)which containsmethyl salicylate glycosides in Dianbaizhu / 国际药学研究杂志

Objective The active ingredient was used as index to optimize the extraction and enrichment process of anti-in-flammatory and analgesic active-fraction(ARF)of Dianbaizhu. Methods Methyl salicylate triglycoside-B was chosen as index com-ponent to extract and enrich methyl salicylate glycosides. Extraction and elution solvents were optimized. The HPLC fingerprint was ob-tained with Thermo Hypersil Gold C18(250 mm×4.6 mm,5μm)column and a gradient elution with the mobile phase consisting of ace-tonitrile(A)-0.2％acetic acid(B)at a flow rate of 1.0 ml/min. And the detection wavelength was set at 294 nm. Results The opti-mized extraction solvent of Dianbaizhu was the 30％ethanol and the optimized elution solvent of ARF enriched by AB-8 macroporous resins was the 35％ethanol. The methodological study on similarity and RSD in ARF HPLC fingerprint of three batches of samples cor-responded to related regulations. Conclusion The extraction and enrichment process of ARF is stable and repeatable.

Pharamacological action in Toddalia asiatica Lam.: Research advances / 国际药学研究杂志

Radix Toddaliae asiaticae which belongs to Toddalia genus of Rutaceae family is a folk medicine in China. Modern pharmacological studies have shown its anti-inflammatory, analgesic, antioxidative, antibacterial, antifungal, cardiovascular prot tive, antitumor activities and so on. The review systematically summarizes pharmacological effects, which can provide references reasonable utilization.

Pharamacological action in Toddalia asiatica Lam.:research advances / 国际药学研究杂志

Radix Toddaliae asiaticae which belongs to Toddalia genus of Rutaceae family is a folk medicine in China. Modern pharmacological studies have shown its anti-inflammatory,analgesic,antioxidative,antibacterial,antifungal,cardiovascular protec?tive,antitumor activities and so on. The review systematically summarizes pharmacological effects,which can provide references for reasonable utilization.

Research progress in chemical constituents, pharmacological activities, clinical practices and quality control of folk medicine Hosta plantaginea / 中草药

The medicinal parts of Hosta plantaginea includes the whole plant, roots, stems, and flowers with a long history used as traditional folk herbal medicine. It has been commonly used for hundreds of years in Mongolia solely or in complex preparation for the treatment of sore throat and other diseases. However, there are few non-systemic studies on anti-inflammatory material basis, mechanisms, and quality control of H. plantaginea so far as well. The crude extracts or pure compounds from H. plantaginea showed anti-inflammatory, analgesic, cytotoxic, anti-microbial, anti-viral, anti-AchE activities, etc. In addition, previous phytochemical studies on H. plantaginea have indicated that steroids, alkaloids, and flavonoids are the major constituents in this plant. In this paper, we have systematically summarized and analyzed the chemical constituents, pharmacological activities, clinical application, and quality control of folk medicine H. plantaginea, which provides the foundation for the rational use and comprehensive development of H. plantaginea.

Study on Active Sites of Anti-inflammatory and Analgesic in Jinxuan Zhike Xunxi San / 中国中医药信息杂志

Objective To explain the material foundation of anti-inflammatory and analgesic effects of Jinxuan Zhike Xunxi San. Methods The foot swelling experiments in rat and xylene-induced ear edema experiments in mouse were adopted to observe the anti-inflammatory effects of the material extracted and purified from Jinxuan Zhike Xunxi San. The hot plate-induced pain experiment for studying the analgesic effect was established. Results The material of supercritical CO2 extract, saponins and flavonoids extract and minerals in Jinxuan Zhike Xunxi San had a inhibiting effect on egg-induced foot swelling in rat, saponins and flavonoids extract had a distinct inhibiting effect on xylene-induced ear edema in mouse. Every extract had obvious analgesic effects on hot plate-induced pain and significantly increased the threshold of pain. Conclusion The active ingredient groups of Jinxuan Zhike Xunxi San are the material of supercritical CO2 extract, saponins and flavonoids extract and minerals.