Szechwan lovage rhizome (SLR, the rhizome of Ligusticum chuanxiong Hort., Chuanxiong in Chinese transliteration) is one Chinese materia medica (CMM) commonly used to activate blood circulation and remove blood stasis. SLR is applicable to most blood stasis syndromes. It has significant clinical efficacy in relation to human diseases of the cardiocerebrovascular system, nervous system, respiratory system, digestive system, urinary system, etc. Apart from China, SLR is also used in Singapore, Malaysia, the European Union, and the United States of America. However, the current chemical markers in pharmacopeia or monography for the quality assessment of SLR are not well characterized or specifically characterized, nor do they fully reflect the medicinal efficacy of SLR, resulting in the quality of SLR not being effectively controlled. CMM can only have medicinal efficacy when they are applied in vivo to an organism. The intensity of their pharmaceutical activities can more directly represent the quality of CMM. Therefore, the chemical constituents and pharmacological actions of SLR are reviewed in this paper. In order to demonstrate the medicinal efficacy of SLR in promoting blood circulation and removing blood stasis, bioassay methods are put forward to evaluate the pharmaceutical activities of SLR to improve hemorheology, hemodynamics, and vascular microcirculation, as well as its anti-platelet aggregation and anticoagulation properties. Through comprehensive analyses of these pharmaceutical properties, the quality and therapeutic value of SLR are ascertained.

Chuanxiong (CX, Ligusticum chuanxiong), Japanese Chuanxiong (JCX, Cnidium officinale), Fuxiong (FX, Ligusticum sinense ‘Fuxiong’), and Jinxiong (JX, Ligusticum sinense ‘Jinxiong’) are aromatic herbs used in China, Japan, and other regions. Their morphology and aromatic odor are similar, resulting in confused and mixed uses. This study compares the volatile compositions of these herbs for defining their medical uses. Headspace solid-phase microextraction–gas chromatography–triple quadrupole–mass spectrometry was employed to separate, identify, and quantify the compounds in the volatile gas of the four herbs. A total of 128 volatile compounds were identified and quantified in 23 these herbal samples. The sums of 106, 115, 116, and 120 compounds were detected in the volatile gas of CX, JCX, FX, and JX, with the mean contents of 4.80, 7.12, 7.67, and 12.0 μg/g, respectively. Types and contents of the main compounds were found to be different in the volatile gas of these herbs. The orthogonal partial least squares discriminant analysis and hierarchical clustering analysis showed the four herbs located in different confined areas or clusters. It is concluded that the volatile compositions in the four herbs are generally similar, but the contents of main volatile compounds are different. These herbs should be clearly differentiated in medical use.

Background/Objectives: Tall Gastrodia Tuber (tuber of Gastrodia elata, Tianma) is an important herb with therapeutic effects on multiple central nervous system diseases. Although some chemical compounds with their bioactivities have been reported, there are still unrevealed bioactive compounds. This study focuses on discovering new compounds with pharmacological effects in Tianma. Methods: Compounds were isolated from ethyl acetate extract of Tianma by column chromatography and semi-preparative HPLC. Their chemical structures were elucidated by spectroscopic analysis including two-dimensional NMR (DEPT90/135, COSY, HSQC, HMBC), HR-ESI-MS, and IR, compared with reported data. Meanwhile, the protective effects against glutamate-induced excitotoxicity of two phenolic glucosides and two rare phenolic nucleosides were screened by a HT-22 cell model. Results: Fourteen compounds were identified, comprising six new natural products and eight known compounds. The six new compounds were named gastrotribenzyloside A (1), gastrotribenzyloside B (2), gastrotribenzyloside C (3), gastrotetrabenzyloside D (4), gastronucleoside B (5) and gastronucleoside C (6). Compounds 1–4 were phenolic glucosides. Compounds 5 and 6 were the first discovery of phenolic nucleosides substituted by multiple benzyl groups in Tianma. A bioactive experiment indicated that the two phenolic glucosides 1 and 2 did not exhibit protective effects against glutamate-induced excitotoxicity of HT-22 cells, while both of the phenolic nucleosides 5 and 11 significantly relieved the cell viability reduction caused by glutamate. Conclusions: Six new phenolic glucosides and phenolic nucleosides are discovered in Tianma. These phenolic nucleosides are potential bioactive components exhibiting cytoprotective effects against excitotoxicity. They deserve further in vivo studies to verify their bioactivity and investigate the mechanism.