Bioactive isopimarane and 3,4-seco isopimarane diterpenoids from Isodon amethystoides.

Isodon amethystoides (Lamiaceae) is a popular plant in folk medicine in the southern provinces of China. Our phytochemical investigation of the twigs and leaves of this plant led to the discovery of five new diterpenoids with isopimarane and 3,4-seco isopimarane scaffolds [isoamethinols A-E (1-5)], along with the known compound 3,4-seco isopimara-4(18),7,15-triene-3-oic acid methylester (6). The chemical structures of these compounds, including the absolute configurations of the new diterpenoids, were determined by comprehensive spectroscopic analyses and single crystal X-ray diffraction measurements. These compounds were evaluated for their biological activities against a panel of human cancer cell lines, gram-positive bacterial strains and HIV. Notably, the 3,4-seco-isopimarane isoamethinol D (4) showed toxicity to the cervical Hela cancer (Hela) cells with an IC50 value of 27.21 µM and the lung (A549) cancer cells with an IC50 value of 21.47 µM. Compound 4 also exhibited mild antimicrobial activity against the oral bacterial strain Streptococcus mutans. These findings suggested that the diterpenoids with a 3,4-seco-isopimarane diterpenoids isolated from I. amethystoides could provide a novel structure scaffold for the discovery of anticancer and antimicrobial compounds.

Tissues-based chemical profiling and semi-quantitative analysis of bioactive components in the root of Salvia miltiorrhiza Bunge by using laser microdissection system combined with UPLC-q-TOF-MS.

BACKGROUND: The dry root of Salvia miltiorrhiza Bunge (Danshen in Chinese) is an used-widely traditional Chinese herbal medicine with and promising efficacy. This herbal plant has been extensively cultivated in China. Currently, people usually rely on its morphological features to evalaute its pharmaceutical quality. In this study, laser micro-dissection system (LMD) was applied to isolate single fresh tissue of root of S. miltiorrhiza. Under fluorescent microscopic model, five tissues namely cork, cortex, phloem, xylem ray and vessel were well recognized and isolated accurately by LMD, respectively and then the distribution pattern of the major bioactive compounds in various tissues was investigated by ultra-performance liquid chromatography-quadrupole/time of flight-mass spectrometry, which aims to validate the traditional experience on evaluating pharmaceutical quality of Danshen by morphological features. RESULTS: Total 62 chemical peak signals were captured and 58 compounds including 33 tanshinones, 23 salvianolic acids and 2 others were identified or tentatively characterized in micro-dissection tissues. Further semi-quantitative analysis indicated that the bioactive components such as tanshinones and salvianolic acids were mainly enriched in cork tissue. CONCLUSION: In the present study, analysis of metabolic profile in different tissues of roots of S. miltiorrhiza is reported for the first time. The distribution pattern of major bioactive components could enable medicinal vendors and consumers to relatively determine the pharmaceutical quality of Danshen by morphological features.Graphical abstractTissues-based chemical profiling of Danshen.

Phytochemistry and pharmacological activities of the genus Prunella.

Prunella is a genus of perennial herbaceous plants in the Labiatae family. There are approximately 15 species worldwide, distributed widely in the temperate regions and tropical mountains of Europe and Asia. In the genus Prunella, P. vulgaris is the most studied, following a several thousand-year history as a traditional antipyretic and antidotal Chinese herb. Furthermore, since ancient times, P. vulgaris has been widely used as a cool tea ingredient and consumed as a vegetable. The genus Prunella contains triterpenoids and their saponins, phenolic acids, sterols and associated glycosides, flavonoids, organic acids, volatile oil and saccharides. Modern pharmacological studies have revealed that Prunella possess antiviral, antibacterial, anti-inflammatory, immunoregulatory, anti-oxidative, anti-tumor, antihypertensive and hypoglycemic functions. The active components related to these functions are mainly triterpenoids, phenolic acids, flavonoids and polysaccharides. This review mainly summarizes recent advances in traditional usage, chemical components and pharmacological functions.

[Study on UPLC fingerprint of Xiasangju Granules].

OBJECTIVE: To establish a UPLC fingerprint method of Xiasangju Granules. METHODS: UPLC analysis was performed on a Waters ACQUITY UPLC H-Class system and carried out at 30 °C on a Waters Column ACQUITY UPLC BEH C18 (2.1 mm x 50 mm, 1.7 µm). A binary gradient elution system was composed of acetonitrile (phase A)and 0.5% acetic acid solution (phase B). Detection was performed at the wavelength of 320 nm,the mobile flow rate was at 0.4 mL/min. A matrix including 16 variations (characteristic peaks area)and 12 samples was constructed for similarity evaluation, cluster analysis and principle component analysis. RESULTS: The results showed that the collected samples had a good similarity. A specificity fingerprint was produced and 16 characteristic peaks were designated. 12 samples were divided into 6 groups. CONCLUSION: It is a reliable, available and quick method for quality control of Xiasangju Granules.