ABSTRACT
Huaihuasan， first recorded in Puji Benshifang by XU Shu-wei from the Southern Song dynasty， consists of four herbs， namely Sophorae Flos （fried）， Platycladi Cacumen （smashed with pestle and baked）， Schizonepetae Spica， and Aurantii Fructus （cut into pieces after the removal of pulp and then fried yellow with wheat bran）. At present， Huaihuasan and its modified formulas vary in clinical usages and dosages， and the resulting outcomes have been investigated. However， there are few reviews uncovering its historical evolution. On this basis， this review systematically combed and verified the historical evolution， dose conversion between ancient and modern times， efficacy， and indications of Huaihuasan， as well as the origin and processing of the contained herbs. The findings have demonstrated that Huaihuasan is composed of four herbs， with the original plants and medicinal parts basically the same as those recorded in the 2020 edition of Chinese Pharmacopoeia. Sophorae Flos refers to the dried flower and bud of Sophora japonica in family Leguminosae， Platycladi Cacumen the dried branch and leaf of Platycladus orientalis in family Cupressaceae， Schizonepetae Spica the dried flower spike of Schizonepeta tenuifolia in family Labiatae， and Aurantii Fructus the dried immature fruit of Citrus aurantium in family Rutaceae or its cultivated varieties. On account of the efficacy in clearing intestine， stopping bleeding， dispersing wind， and moving Qi， Huaihuasan has been mainly used to treat intestinal diseases such as bloody defecation and perianal abscess. In modern clinical practice， it is mainly applicable to patients with hematochezia and bleeding due to internal hemorrhoid， ulcerative colitis， or anal fissure. It was suggested that the raw medicinal materials should be decocted and processed according to the methods described in the 2020 edition of Chinese Pharmacopoeia. Following the conversion formula of one Qian=4 g， this paper determined the dosages of Sophorae Flos （fried）， Platycladi Cacumen （smashed with pestle and baked）， Schizonepetae Spica， and Aurantii Fructus （cut into pieces after the removal of pulp and then fried yellow with wheat bran） all to be 2 g， with the total dosage being 8 g. Such comprehensive analysis based on ancient books and modern literature has provided a more scientific reference for the clinical application， research， and development of this classical formula.
ABSTRACT
The screening of active components of traditional Chinese medicine has always been the focus and difficulty in modern research of Chinese medicine preparations. With the continuous development of life science, omics and computer technology, the virtual screening technology for active components of traditional Chinese medicine has gradually come into people's vision. Molecular docking technology is an important method for screening active components of traditional Chinese medicine. It not only has a short cycle and strong operability, but also avoids the disadvantage of poor stability in pharmacological experiments. Safflower extract can effectively alleviate the symptoms of myocardial ischemia, but its active components are not clear. In this study, with use of the molecular docking technology, the active components in safflower against myocardial ischemic were virtually screened based on the screening method of active components. Forty-six chemical components and 5 target proteins which showed high correlation with myocardial ischemia were obtained from the existing database and related literature reports. With the molecules of three commercially available drugs diltiazem, trimetazidine and verapamil as positive control molecules, the compomnents were docked with 5 target proteins. Active components were screened according to docking scores and interactions between molecules and targets, and then the active ingredients can be inferred. Fourteen chemical components were screened to have the most potential anti-myocardial ischemic activity, and all of them were flavonoids. Therefore, it can be inferred that the flavonoid components are the most potential anti-myocardial ischemic components in safflower. The screening of active anti-myocardial ischemia components in safflower was completed in this study, laying the foundation for subsequent researches.