ABSTRACT
ObjectiveBased on the experience of traditional quality evaluation， the quality of Atractylodis Macrocephalae Rhizoma（AMR） with different production methods such as direct seeding， transplanting after seedling raising， topping and non-topping， and difference in growth years was compared. MethodVernier caliper was used to measure the trait data of AMR in different production methods. Paraffin sections of AMR with different production methods were made by saffron solid green staining， and the microstructure was observed. The contents of water-soluble and alcohol-soluble extracts in AMR with different production methods were determined according to the 2020 edition of Chinese Pharmacopoeia. The content of water-soluble total polysaccharides in AMR with different production methods was detected by sulfuric acid-anthrone method. Fiber analyzer was used to detect the content of fiber components in AMR with different production methods. The contents of monosaccharides， oligosaccharides and some secondary metabolites in AMR with different production methods were detected by ultra performance liquid chromatography（UPLC）， and the differences of chemical components were compared by multivariate statistical analysis methods such as principal component analysis（PCA） and partial least squares-discriminant analysis（PLS-DA）. ResultIn terms of traits， the 3-year-old AMR with direct seeding and without topping was close to the high-quality AMR with "phoenix-head and crane-neck， strong sweetness and clear aroma" recorded in ancient materia medica， followed by the 3-year-old AMR with topping after transplanting， while the 2-year-old AMR with topping after transplanting with high market circulation rate was generally fat and strong with mild odor. In the microscopic aspect， the arrangement of xylem vessels and fiber bundles in the 3-year-old samples formed two obvious rings. Compared with the 2-year-old samples cultivated in Bozhou and Zhejiang， the 3-year-old samples without topping after transplanting had more wood fibers. In terms of chemical composition， the contents of 70% ethanol extract， fructose， glucose， sucrose， 1-kestose， atractylenolide Ⅰ， chlorogenic acid， neochlorogenic acid， cryptochlorogenic acid and other components in 3-year-old AMR with direct seeding and without topping were significantly higher than those in the other three samples（P<0.05）. The contents of cellulose， 70% ethanol extract， sucrose， atractylenolide Ⅰ， atractylone and other components in 3-year-old AMR with topping after transplanting were significantly higher than those in the 2-year-old AMR with high market circulation rate（P<0.05）， while the contents of water-soluble extract and water-soluble total polysaccharides in 2-year-old samples with topping after transplanting were significantly higher than those in the 3-year-old AMR with topping after transplanting， direct seeding and without topping（P<0.05）. ConclusionUnder the current mainstream production mode， too much manual intervention makes AMR heavily enriched in polysaccharides and increased the yield， but the accumulation of sweet substances， fragrant substances and fiber substances is insufficient， which affects its quality. The current quality standard of AMR has some shortcomings in guiding the high quality production of it， it is suggested to revise the quality standard of AMR， supplement the quantitative analysis of secondary metabolites， and strengthen the production of imitation wild AMR.
ABSTRACT
ObjectiveBased on the traditional quality evaluation methods summarized in previous dynasties， this paper systematically contrasted cultivated Astragali Radix（CA） and wild-simulated Astragali Radix（WA） from the aspects of character， microstructure and chemical composition by modern technological means. MethodThe collected CA and WA were compared in characters and microscopic characteristics in cross section， and comparative analysis were performed on the contents of cellulose， extracts， carbohydrate， total flavonoids， total saponins， etc. Then ultra-high performance liquid chromatography-quadrupole-time-of-flight mass spectrometer（UPLC-Q-TOF-MS） and desorption electrospray ionization mass spectrometry imaging（DESI-MSI） were used to comparatively analyze the secondary metabolites and their spatial distributions in the xylem and phloem of CA and WA. ResultIn terms of characters， the characters and sectional features of WA was consistent with the characteristics of high-quality Astragali Radix， while the CA was quite different from the traditional high-quality Astragali Radix. In terms of microscopy， the phellem layer of CA was thin， and the section fissures were mostly distributed through the cambium in a long strip shape without obvious growth ring characteristics. The cork layer of WA was thick， and the cracks in the section were distributed in the center of the xylem and the outer edge of the phloem in an irregular cavity shape. The cambium was tight without cracks， and had obvious characteristics of a growth ring. In terms of chemical composition， the contents of water-soluble extract， 80% ethanol extract and sucrose of CA was significantly higher than those of WA， while the contents of total saponins， lignin and hemicellulose were significantly lower than those of WA. And the contents of 100% ethanol extract， total polysaccharides and total flavonoids in both of them were generally similar， but slightly higher in WA. The contents of 2 kinds of monoacyl-substituted flavonoid glycosides in the xylem of WA was significantly higher than those of CA， while the contents of 2 kinds of flavonoid aglycones and one flavonoid glycoside were on the contrary. The contents of 7 saponins in phloem of WA were significantly higher than those of CA. ConclusionThere are significant differences between CA and WA in characters， microstructure and chemical components， in which CA has a fast growth rate and a short planting period， and the primary metabolites such as water-soluble extracts and sucrose are more enriched， which is the reason for its firm texture and sweetness being significantly higher than those of WA. However， the contents of lignin， hemicellulose and some secondary metabolites in WA are significantly higher than those in the CA， which are close to the traditional description of characters and quality. Based on the results of this study， it is suggested to strengthen the production of WA， improve the supply capacity of WA， and gradually upgrade the current standard. It is recommended to increase the contents of monoacyl-substituted flavonoid glycosides， total saponins and other indicators that can characterize different production methods， so as to guide the high-quality production of Astragali Radix.
ABSTRACT
By reviewing the research history on quality comparison between wild and cultivated Chinese crude drugs， this paper systematically combed the relevant research reports since the 1950s， and summarized and analyzed the results of existing comparative studies， and found that the existing comparative research on the quality of wild and cultivated Chinese crude drugs were mainly focused on several aspects， including characteristics， microstructures， chemical compositions， pharmacodynamic effects， and genetic diversity. Among these， comparative studies of chemical compositions have been the dominant approach， with a particular emphasis on comparing the contents of index components. However， research on pharmacodynamic effects remained relatively limited. Due to various factors such as sample quantity， sample origin， growth period and cultivation methods， the differences in quality between wild and cultivated Chinese crude drugs vary significantly. In general， most wild Chinese crude drugs exhibited higher quality than cultivated products， with significant differences in their characteristics. The contents and proportions of some chemical components underwent noticeable changes， particularly with a marked increase in the proportion of primary metabolites after cultivation. The quality of cultivated Chinese crude drugs is closely related to the cultivation practices employed. Chinese crude drugs produced through wild nurturing， simulated wild planting， ecological cultivation， and other similar methods demonstrate quality levels comparable to those of wild Chinese crude drugs. Based on the analysis results， it is recommended to explicitly specify the cultivation practices and cultivation period of cultivated Chinese crude drugs in comparative studies of the quality between wild and cultivated Chinese crude drugs. Multiple technical approaches， including characteristics， microscopy， non-targeted metabolomics combined with quantitative analysis of differential components， and bioefficacy evaluation， should be employed to comprehensively assess the quality disparities between wild and cultivated Chinese crude drugs. Moreover， research efforts should be intensified to investigate the changes in pharmacodynamic effects resulting from differences in plant cell wall composition， primary metabolites， and secondary metabolites， in order to guide the production of high-quality Chinese crude drugs.
ABSTRACT
Oxalicine B ( 1) is an α-pyrone meroterpenoid with a unique bispirocyclic ring system derived from Penicillium oxalicum. The biosynthetic pathway of 15-deoxyoxalicine B ( 4) was preliminarily reported in Penicillium canescens, however, the genetic base and biochemical characterization of tailoring reactions for oxalicine B ( 1) has remained enigmatic. In this study, we characterized three oxygenases from the metabolic pathway of oxalicine B ( 1), including a cytochrome P450 hydroxylase OxaL, a hydroxylating Fe(II)/α-KG-dependent dioxygenase OxaK, and a multifunctional cytochrome P450 OxaB. Intriguingly, OxaK can catalyze various multicyclic intermediates or shunt products of oxalicines with impressive substrate promiscuity. OxaB was further proven via biochemical assays to have the ability to convert 15-hydroxdecaturin A ( 3) to 1 with a spiro-lactone core skeleton through oxidative rearrangement. We also solved the mystery of OxaL that controls C-15 hydroxylation. Chemical investigation of the wild-type strain and deletants enabled us to identify 10 metabolites including three new compounds, and the isolated compounds displayed potent anti-influenza A virus bioactivities exhibiting IC50 values in the range of 4.0-19.9 μmol/L. Our studies have allowed us to propose a late-stage biosynthetic pathway for oxalicine B ( 1) and create downstream derivatizations of oxalicines by employing enzymatic strategies.
ABSTRACT
By reviewing ancient materia medica， prescription books， medical books and modern literature， this article makes a systematic textual research on the name， origin， commercial specification， producing area， harvesting and processing of Scutellariae Radix used in famous classical formulas according to the historical development， in order to provide a reference for the development and utilization of famous classical formulas. Scutellariae Radix was first named as Qian， Qin and so on， while Huangqin was used as the official name in ancient literature， as well as many aliases such as Fuchang， Huangwen and Dufu. The main origin of Scutellariae Radix in the past dynasties was Scutellaria baicalensis， and other Scutellaria plants were also used for Scutellariae Radix at different times. The medicinal parts of Scutellariae Radix in all dynasties are roots， since the Northern and Southern dynasties， it has gradually differentiated into Ziqin and Kuqin with different efficacy according to their different growth stages and characteristics， and continued to this day. At present， most of Scutellariae Radix are Ziqin in the market， due to the influence of cultivation cost， index component content requirements and other factors. The production area of Scutellariae Radix recorded in ancient literature was wide and gradually expanded from the Yangtze River basin to the northward. Since modern times， Chengde city of Hebei province has been respected as a geo-authentic area， now S. baicalensis is cultivated in a wide area， spreading over north and northeast China. Scutellariae Radix was mostly used as raw products in the early period， and a variety of processed products appeared in the Ming dynasty. Development continues to this day， Scutellariae Radix mainly includes raw products and wine-processed products. According to the research conclusion， it is suggested that S. baicalensis should be used as Scutellariae Radix in famous classical formulas， and the selection of its commercial specifications and processed products can be comprehensively determined according to the requirements of original prescription and the clinical effect.
ABSTRACT
By reviewing ancient materia medica， prescription and medical books， combined with modern literature， the paper made textual research on the name， origin， producing area， quality evaluation， harvesting and processing methods of Angelicae Pubescentis Radix and Notopterygii Rhizoma et Radix， so as to provide a basis for the selection and use of these two herbs in the development of famous classical formulas. Through textual research， it can be found that Angelicae Pubescentis Radix and Notopterygii Rhizoma et Radix were mixed together in the early history of China， but the distinction was first made during the Southern and Northern dynasties， and since then there have been constant controversies， and it is not until contemporary times that they are distinguished clearly. In the past dynasties， Duhuo and Qianghuo were used as the rectification of names， some aliases and trade names were also seen. Angelica biserrata is the mainstream origin of Angelicae Pubescentis Radix in the past dynasties， and there are many plants belonging to Angelica， Heracleum and Aralia， which are also used as this medicine. However， the origin of Notopterygii Rhizoma et Radix used in the past dynasties is mostly Notopterygium incisum or N. franchetii， which is relatively uniform. The producing areas of Angelicae Pubescentis Radix and Notopterygii Rhizoma et Radix are mostly concentrated in the western and northwestern regions of China， among which Angelicae Pubescentis Radix is mainly produced in Hubei， Chongqing， Sichuan， Shaanxi and other places， and the border area between Hubei and Chongqing is the geo-authentic area. Notopterygii Rhizoma et Radix is mainly produced in Sichuan， Gansu， Qinghai， Shaanxi and others with the western and northern Sichuan and southern Gansu as the geo-authentic areas. Angelicae Pubescentis Radix and Notopterygii Rhizoma et Radix in the past dynasties were harvested in spring and autumn， especially in February and August of the lunar calendar. Angelicae Pubescentis Radix with strong main roots， few branches， firm texture and strong aroma is superior， and Notopterygii Rhizoma et Radix with strong rhizomes， tightly raised knots， purple-brown skin， tight cross-section， strong aroma and silkworm-like shape is superior. The processing methods of Angelicae Pubescentis Radix and Notopterygii Rhizoma et Radix are mostly cut after cutting the reeds， and the raw product is used as medicine. Based on the above research results， it is recommended that the roots of A. biserrata should be used for Angelicae Pubescentis Radix and the roots of N. incisum should be used for Notopterygii Rhizoma et Radix in the development of famous classical formulas， and raw products should be used in the formulas that do not specify processing requirements.