Six new abietane diterpenoids (1-6) and five undescribed iridoids (7-11) have been isolated from the aerial parts of Caryopteris mongolica. The intricate structural characterization of these compounds was meticulously undertaken using an array of advanced spectroscopic techniques. This process was further enhanced by the application of DP4+ probability analyses and electronic circular dichroism (ECD) calculations. Following isolation and structural elucidation, the cytotoxicity of these compounds was evaluated. Among them, compound 3 stood out, displaying significant cytotoxic activity against HeLa cells with an IC₅₀ value of 7.83 ± 1.28 μmol·L^-1. Additionally, compounds 1, 2, 4, 9, and 10 manifested moderate cytotoxic effects on specific cell lines, with IC₅₀ values ranging from 11.7 to 20.9 μmol·L^-1.
Humans ; Abietanes/chemistry* ; HeLa Cells ; Lamiaceae/chemistry* ; Circular Dichroism ; Diterpenes/chemistry* ; Molecular Structure

Clinopodium chinense, a traditional folk medicinal herb, has been used to treat abnormal uterine bleeding(AUB) for many years. Saponins and flavonoids are the main active components in C. chinense. To study the pharmacokine-tics of multiple components from the total extract of C. chinense(TEC), we established a sensitive and rapid method of ultra-perfor-mance liquid chromatography coupled with tandem mass spectrometry(UPLC-MS/MS) for simultaneous determination of five compounds in the plasma of AUB rats. After validation, the AUB model was established with SD female rats which got pregnant on the same day by gavage with mifepristone(12.4 mg·kg~(-1)) and misoprostol(130 μg·kg~(-1)). The established method was applied to the detection of hesperidin, naringenin, apigenin, saikosaponin a, and buddlejasaponin Ⅳb in AUB rats after the administration of TEC. The pharmacokinetic parameters were calculated by DAS 2.0. The five compounds showed good linear relationship within the detection range. The specificity, accuracy, precision, recovery, matrix effect, and stability of the method all matched the requirements of biolo-gical sample detection. The above 5 compounds were detected in the plasma of AUB rats after the administration of TEC. The C_(max) va-lues of hesperidin, naringenin, apigenin, saikosaponin a, and clinoposide A were 701.6, 429.5, 860.7, 75.1, and 304.1 ng·mL~(-1), respectively. All the compounds owned short half-life and quick elimination rate in vivo, and the large apparent volume of distribution indicated that they were widely distributed in tissues. Being rapid, accurate, and sensitive, this method is suitable for the pharmacokinetic study of extracts of Chinese herbal medicines and provides a reference for the study of pharmacodynamic material basis of C. chinense in treating AUB.
Administration, Oral ; Animals ; Apigenin/analysis* ; Chromatography, High Pressure Liquid/methods* ; Chromatography, Liquid ; Drugs, Chinese Herbal/chemistry* ; Female ; Flavonoids/analysis* ; Hesperidin ; Lamiaceae ; Mifepristone ; Misoprostol ; Oleanolic Acid/analogs & derivatives* ; Plant Extracts/chemistry* ; Rats ; Saponins ; Tandem Mass Spectrometry/methods* ; Uterine Hemorrhage

The aim of this paper was to evaluate the key production processes of Schizonepetae Herba formula granules based on the new model of combining characteristic chromatogram with quantitative transfer relationship. The rationality of production process design was evaluated by studying the intermediates in different processes of formula granules, analyzing the loss of index component pulegone in each step, and establishing the characteristic chromatogram. The content of pulegone in 10 batches of standard decoction ranged between 0.067% and 0.124%(70%-130% of the average value), and the transfer rate of pulegone was 44.58%-93.97%. After the improvement of the production process, the content of pulegone in Schizonepetae Herba formula granules was 0.093%, and the transfer rate of pulegone was 68.38%, which was consistent with the parameters range of standard decoction. This study emphasized the integrality of the research process of traditional Chinese medicine(TCM) formula granules, and provided a new idea for the quality control of TCM with content determination as the main evaluation index for a long time.
Chromatography, High Pressure Liquid ; Drugs, Chinese Herbal/chemistry* ; Lamiaceae/chemistry* ; Medicine, Chinese Traditional ; Quality Control

Six compounds were isolated from the aerial part of cultivated Clerodendranthus spicatus in Hainan with various chromatographic techniques,and their structures were determined as:1-dehydroxy-1-oxo-rupestrinol(1),N-trans-feruloyltyramine(2),methyl 3,4-dihydroxyphenyllactate(3),caffein acid(4),methyl caffeate(5) and ethyl caffeate(6),via analysis of physicochemical properties and spectroscopic evidence.Compound 1 was a new compound,while compounds 2 and 3 were isolated from C.spicatus for the first time.Biological activity results showed that compounds 2-4 exhibited α-glucosidase inhibitory activity with different inhibition ratio.
China ; Glycoside Hydrolase Inhibitors ; isolation & purification ; pharmacology ; Lamiaceae ; chemistry ; Molecular Structure ; Phytochemicals ; isolation & purification ; pharmacology ; Sesquiterpenes, Eudesmane ; isolation & purification ; pharmacology

Ziziphora bungeana is a kind of medicinal plants belongs to Labiatae,and it also a kind of geoherbs in Xinjiang. The main active ingredient linarin has a higher content in inflorescence than in other parts. In this study,high-throughput sequencing technology was used to reveal the transcriptome of the inflorescence of Z. bungeana,77 366 unigenes were acquired,of which 56 375 unigenes were annotated based on search of the database and classification. Through the analysis of metabolic pathways,sixty unigenes were probably encoding some enzymes involved in the flavonoid biosynthesis pathways. The contents of linarin in different parts were determined and the key genes were verified by qRT-PCR. The discovery provides the research basis for further analysis of the enzyme genes involved in the biosynthesis of the major flavonoid components in Z. bungeana.
Flavonoids ; biosynthesis ; Gene Expression Profiling ; High-Throughput Nucleotide Sequencing ; Lamiaceae ; chemistry ; Transcriptome

The aim of this paper was to screen the active targets of Schizonepetae Herba and Saposhnikoviae Radix in the treatment of ulcerative colitis by means of network pharmacology,and to investigate their mechanism of action. The effective components of Schizonepetae Herba and Saposhnikoviae Radix were screened out by traditional Chinese medicine systematic pharmacological( TCMSP)database,with oral bioavilability( OB) ≥30% and drug-like( DL) ≥18% selected as the thresholds. Target PPI network was built between the main components and their corresponding targets. One hundred and eighty-two human genes corresponding to the medicine target sites were obtained from Uniprot database; 3 874 genes corresponding to ulcerative colitis were obtained from Genecard database.A total of 115 intersection genes were screened from disease genes and medicine genes,and the PPI interaction analysis was conducted by using String tool. Disease-target PPI network was drawn by using Cytoscape software,and component-target-disease network was constructed. One hundred and eight nodes and 1 882 connections were found,and then Cytoscape software was used to merge the networks and filter the core network for gene GO function analysis and KEGG pathway enrichment analysis. The mechanism of Schizonepetae Herba and Saposhnikoviae Radix was then verified by animal experiment. Gene GO functional analysis suggested that biological process,molecular functions and cell components were involved,and it was found that ulcerative colitis might be related to transcription factor activity,and cytokine receptor binding,etc. Gene KEGG pathway enrichment analysis showed that the mechanism of ulcerative colitis might be associated with TNF and Toll-like receptors( TLRs) signaling pathway-mediated cytoinflammatory factors interleukin-1( IL-1) and interleukin-6( IL6). The possible mechanism of the effective components of Schizonepetae Herba and Saposhnikoviae Radix in treating ulcerative colitis might be related to intervening the cytokine receptor binding of TNF and TLRs signaling pathways,reducing the transcription of nuclear factor-kappaB( NF-κB),and inhibiting the secretion of intestinal inflammatory factors IL-1 and IL-6.
Animals ; Apiaceae/chemistry* ; Colitis, Ulcerative/drug therapy* ; Databases, Genetic ; Drugs, Chinese Herbal/therapeutic use* ; Humans ; Interleukins/metabolism* ; Lamiaceae/chemistry* ; Medicine, Chinese Traditional ; Phytotherapy ; Plant Roots/chemistry* ; Protein Interaction Mapping ; Signal Transduction ; Software ; Toll-Like Receptors/metabolism*

Through the determination of the growth, physiological and active components of Glechoma longituba, the effect of soil bulk density on growth and quality of G. longituba was explored. Through pot experiment, six different bulk density treatments were set for 0.8, 0.9, 1.0, 1.1, 1.2, 1.3 g·cm⁻³ , the growth index, physiological index and the content of active components were determined. The results showed that the growth indexes and biomass of G. longituba firstly increased and then decreased with the increase of soil bulk density. The dry weight of G. longituba achieved the maximum 5.70 g in the treatment of 1.0 g·cm⁻³ . The photosynthetic pigments, soluble sugars and free amino acids firstly increased and then decreased with the increase of soil bulk density. The suitable soil bulk density was beneficial to the accumulation of photosynthetic pigment, soluble protein and free amino acid synthesis. The content of malondialdehyde increased gradually with the increase of soil bulk density. The contents of ethanol-soluble extractives of G. longituba were greater than 25%, meeting its quality criterionin Chinese Pharmacopoeia 2015, achieved the maximum of 40.66% in the treatment of 1.0 g·cm⁻³ . The total flavonoids content of G. longituba increased gradually with the increase of soil bulk density, triterpenic acid and phenolic acids decreased gradually with the increase of soil bulk density. Soil bulk density has a significant effect on the growth and quality of G. longituba, and it is conducive to the growth and its medicinal quality at the soil bulk density of 1.0 g·cm⁻³.
Flavonoids ; analysis ; Lamiaceae ; chemistry ; growth & development ; Photosynthesis ; Pigments, Biological ; analysis ; Plant Extracts ; analysis ; Soil

OBJECTIVETo examine the relaxant effects of hydro-ethanolic, macerated aqueous (MA) and lipidfree macerated aqueous (LFMA) extract of Tymus vulgaris on tracheal chains of guinea pigs.

METHODSThe relaxant effects of five cumulative concentrations of each extract (0.4, 0.8, 1.2, 1.6 and 2.0 g/100 mL) were compared with saline as negative control and five cumulative concentrations of theophylline (0.1, 0.2, 0.4, 0.6 and 0.8 mmol/L) on precontracted tracheal smooth muscle of guinea pig with 60 mmol/L KCl (group 1) and 10 µmol/L methacholine (group 2, n=6 for each group).

RESULTSIn group 1 all concentrations of theophylline, three higher concentrations of hydro-ethanolic, two concentrations of LFMA and last concentration of MA extracts showed significant relaxant effects compared with that of saline (P<0.05 or P<0.01). Two lower concentrations of LFMA and all concentrations of MA except higher one caused contraction compared with saline (P<0.05 or 0.01). In group 2 experiments, all concentrations of theophylline, hydro-ethanolic, MA and LFMA extracts showed significant relaxant effects compared to that of saline (P<0.05 or P<0.01). In both groups, the relaxant effect of all concentrations of hydro-ethanolic extract were significantly higher than most concentrations of others (P<0.05 or P<0.01). The relaxant effect of different concentrations of three extracts were significantly greater in group 2 compared with group 1 experiments (all P<0.01). There were significantly positive correlations between the relaxant effects and concentrations for theophylline and all extracts in both groups (P<0.05 or P<0.01).

CONCLUSIONHydro-ethanolic extract has a potent weaker relaxant effect for other extracts from Tymus vulgaris on tracheal chains of guinea pigs.

Animals ; Bronchodilator Agents ; pharmacology ; Guinea Pigs ; In Vitro Techniques ; Lamiaceae ; chemistry ; Lipids ; chemistry ; Muscle Relaxation ; drug effects ; Muscle, Smooth ; drug effects ; physiology ; Plant Extracts ; pharmacology ; Solubility ; Solutions ; Theophylline ; Trachea ; physiology ; Water ; chemistry

In this paper, an analysis was made on the varieties and standards of labiatae medicinal plants used in Tibetan medicine. The results showed 71 species of labiatae plants in 21 genera (including varieties) recorded in relevant literatures, involving 44 varieties of medicinal materials. Specifically, seven species (9.9%) were intersected with traditional Chinese medicines (TCM), 19 varieties (43%) were recorded in Chinese medicinal material standards at all levels, and 27 species (38%) were source plants. In Tibetan medicine standards and literatures, there are great differences between Tibetan names and translated Chinese names and among varieties of source plants. Apart from a few of varieties intersected with traditional Chinese medicines had complete standards and regulations in Chinese Pharmacopoeia, most of species only had characters, microscopic, physical and chemical identifications in Standards Issued by Ministry of Health-Tibetan Medicine, Tibetan Medicine Standard and local standards. Therefore, the Tibetan medicinal material variety-source specification and quality standard system shall be promoted on the basis of literatures research, investigations for resources and current applications and modern pharmaceutical studies.
Drugs, Chinese Herbal ; chemistry ; pharmacology ; Humans ; Lamiaceae ; chemistry ; classification ; Medicine, Tibetan Traditional ; standards ; Phytotherapy ; standards ; Plants, Medicinal ; chemistry ; classification

An investigation on the chemical constituents of the 90% EtOH extract of Perovskia atriplicifolia led to the isolation of fifteen compounds from the EtOAc fraction. Based on the detailed spectral analysis (MS, 1D and 2D NMR), as well as comparison with the literatures, the structures of compounds 1-15 were determined as cirsimaritin (1), salvigenin (2), syringaldehyde (3), vinyl caffeate (4), 2α, 3α-dihydroxyolean-12-en-28-oicacid (5), 2α, 3α-dihydroxyurs-12-en-28-oicacid (6), niga-ichigoside F1 (2α, 3β, 19α, 23- tetrahydroxyurs - 12-en-28-oicacid- O-β-D- glucopyranoside, 7), sericoside (8), 4-epi-niga-ichigoside F1 (2α, 3β, 19α, 24-tetrahydroxyurs-12-en-28-oicacid O-β-D-glucopyranoside, 9), 2α, 3β, 24-trihydroxyolean-12-en-28-oicacid O-β-D-glucopyranosyl-(1 --> 2) - β-D-glucopyranoside (10), pruvuloside A (11), asteryunnanoside A [2α, 3β, 23-trihydroxyolean-12-en-28-oicacid O-β-D-glucopyranosyl-(1 --> 2)-β- D- glucopyranoside,12], rosmarinic acid methyl ester (13), β-sitosterol (14), and daucosterol (15), respectively. Compounds 1-13 were isolated from the Perovskia genus for the first time. All the compounds were obtained from P. atriplicifolia for the first time.
Drugs, Chinese Herbal ; chemistry ; isolation & purification ; Lamiaceae ; chemistry ; Magnetic Resonance Spectroscopy ; Molecular Structure ; Spectrometry, Mass, Electrospray Ionization