Study On The Chemical Constituents And Identification Of Decocted Pieces Of Descurainiae Semen

"Tinglizi" is sourced from the ripe seed of Descurainia sophia (L.) Webb.ex Prantl. and Lepidium apetalwn Willd., family Brassicaceae (Cruciferae), named "nantinglizi" (Descurainiae Semen, short for DSS below) and "beitinglizi" (Lepidii Semen, short for LSS below) respectively. In the theory of Traditional Chinese Medicine, it is bitter and pungent in flavor, extreme cold in nature and attributive to the lung and bladder meridians. It has the power to purge lung-fire, relieve dyspnea, promote diuresis and reduce edema, and it is mainly indicated in a case with phlegm-fluid accumulation, cough with excessive sputum, dyspnea with being unable to lie, and general swelling. It can be also used for edema, pleural effusion and ascites, and dysuria. Descurainiae Semen was initially recorded in "Shen Nong Ben Cao Jing" and listed as low-grade medicine. It has been widely applied in clinic and exerted obvious therapeutic effects, and mainly indicated for pleural effusion, pulmonary edema, asthma, and various types of cardiac failure caused by heart disease, etc.It is indicated that the processed Descurainiae Semen has been dominating in clinical application since it was initially recorded in "Shen Nong Ben Cao Jing". In the long-term medical practice, the roasted one has gradually the mainstream of various medicinal specifications, and recorded as the standard processing method by China pharmacopeia (2010 edition). It is required to stir-bake until the emergence of cracking according to the method of simple parching without adjuvants, and the parching degree is documented as mild parching, slight parching, parching medicinal materials until they become yellowish, purplish, incense. In terms of its processing effect, as described in the textbook, the raw DSS has the powerful action of purging lung, promoting diuresis and reducing edema, and is usually indicated for ascites and hyposarca while the roasted DSS is mainly used for cough and dyspnea because roasting can moderate the extremely cold nature and protects lung from drastic damage. Thus it can be seen that some changes appear in the course of processing, which causes the difference of therapeutic effects in cases of the raw and processed ones. Based on this, a series of problems come about, for example, what changed, what transformation happened, how it produced and why it could produce, how the raw and roasted DSS can be identified. Due to the weak research status of DSS, the report on the processing research has been few. It is considered that the difference of therapeutic effect between the raw and processed DSS ought to be related to the change of chemical constituents, which is the internal material basis. To explore the reason of the different effects of the raw and roasted DSS, study on the chemical constituents of DS was deeply conducted in this paper. Moreover, HPLC fingerprints combined with statistical analysis method was applied to discriminate the raw and roasted DSS and find the chemical constituents which were mainly responsible for the differentiation between raw and roasted DSS, thus laying a foundation for illustrating the processing mechanism.This paper is mainly divided into three parts.First, a comprehensive review on DSS was completed mainly from the following four aspects:variety identification, chemical constituents, pharmacological effects and study on processing. Variety identification mainly included textual research, authentication of DSS and adulterant, DSS and LSS. In the aspect of chemical constituents, an overall summary of its five main effective constitutes (thioglycoside and isothiocyanic acid, flavonoid, Cardiac glycosides, phenylpropanoids and organic acid) was performed. Pharmacological effects were systematically summarized, such as improving the function of cardiovascular, cytotoxicity, relieving cough, diuresis, etc. Current status of processing research was also reviewed from the following aspects:historic evolution, processing method, processing effect and changes on the chemical constituents and pharmacological effects after processing.Second, based on multiple modern chromatographic separation technology and packing material for chromatographic column such as silica eel. ODS. polvamide. LH-20, etc., the chemical constituents were deeply studied, and 18 compounds have been isolated from DSS, among which 9 compounds were new and 4 compounds were firstly isolated from DSS. All of them were elucidated by spectrum analysis (’H-NMR,13C-NMR,2D-NMR, MS, UV, IR, etc.) and single crystal diffraction, including descuraic anhydride A (1), descuraic anhydride B (2), descuraic anhydride C (3), descuraic cyclolign anhydride A (4), descuraic cyclolign anhydride B (5), descuraic cyclolign anhydride C (6), descuraic cyclolign anhydride dimer (7), descuraic cyclolign anhydride amide (8), (E)- 2-O-sinapoly-β-D-glucopyranosideå'Œ (E)-2-O-sinapoly-a-L-glucopyranoside (9), sinapic acid (10), 1,2-disinapoyl-β-D-glucopyranoside (11), 1,2-disinapoyl-β-D-glucopyranoside (12), quercetin (13), isorhamnetin-3-O-β-D-glucopyranoside (14), kaempferol 3-O-a-L-arabinopyranoside-7-O-α-L-rhamnopyranoside (15), kaempferol 3-O-[α-L-rhamnopyranosyl-(1â†'2)-α-arabinopyranoside] (16),3β,14β-hydroxy-5β-card-20(22)-enolide-3-O-β-D- glucopy-ranosyl-(1â†'4)-α-L-rhamnopyranoside (17),3β,14β-hydroxy-5β-9-oxo-card-20(22)-enolide,3-O-β-D-glucopyranosyl-(1â†'4)-β-D-digitoxose (18)。Last, the chromatographic fingerprints of the raw and roasted DSS were studied, and analyzed to identify them combined with hierarchical cluster analysis (HCA), principle component analysis (PCA), partial peast squares discriminant analysis (PLS-DA). It is demonstrated that the three methods proved to be satisfactory for matching and discriminating the chromatographic fingerprints of the raw and roasted DSS, and the potential and important components for the discrimination between raw and roasted DSS were also found. What’s more, this method can also be applied in the identification of authenticity. It is indicated that fingerprint combined with statistical analysis can identify DSS and its adulterant Plantagirus semen quickly and effectively. It was found that among 10 batches of Plantagirus semen,7 batches of sample was mixed with DSS.