As a TCM, Hedyotis diffusa Willd. has been using to treat malignant tumors, and many studies also showed that the extracts from Hedyotis diffusa Willd. possessed evident antitumor activities. Therefore, we carried out chemical study on Hedyotis diffusa Willd. and investigated the cytotoxicity of the obtained compounds on a panel of eight tumor cell lines. As a result, four new compounds were isolated from Hedyotis diffusa Willd., including three iridoid glycosides of Shecaoiridoidside A–C (1–3) and a cerebroside of shecaocerenoside A (4). Also, six known iridoid compounds (5–10) were also obtained. The cytotoxicity of all compounds against human tumor cell lines of HL-60, HeLa, HCT15, A459, HepG2, PC-3, CNE-2, and BCG-823 were also evaluated in vitro. New compound 3 exhibited evident cytotoxicity to all tumor cell lines except the Hela, and the IC₅₀ values are from 9.6 µM to 62.2 µM, while new compound 4 showed moderate cytotoxicity to all the cell lines, and the IC₅₀ values are from 33.6 µM to 89.3 µM. By contrast, new compound 1 and known compound 9 showed moderate cytotoxicity to HCT15, A459, and HepG2 selectively. Known compound 7 also exhibited moderate cytotoxicity to HCT15 and A459 selectively.

Valeriana plants are members of the Caprifoliaceae family, which include more than 200 species worldwide. We summarized previous reports on traditional clinical applications, bioactivities, and phytochemistry of Valeriana by searching electronic databases of Science Direct, Web of Science, PubMed, and some books. Some Valeriana species have been used as traditional medicines, demonstrating calming fright and tranquilizing mind, promoting Qi and blood, activating blood circulation and regulating menstruation, dispelling wind and eliminating dampness, regulating Qi-flowing to relieve pain, and promoting digestion and checking diarrhea, and treating diseases of the nervous, cardiovascular, and digestive systems, inflammation, gynecology, and others. Pharmacology studies revealed the effects of Valeriana, including sedative, hypnotic, antispasmodic, analgesic, antidepressant, anxiolytic, anticonvulsant, antiepileptic, neuroprotective, antibacterial, antiviral, cytotoxic, and antitumor effects as well as cardiovascular and cerebrovascular system improvements. More than 800 compounds have been isolated or identified from Valeriana, including iridoids, lignans, flavonoids, sesquiterpenoids, alkaloids, and essential oils. Constituents with neuroprotective, anti-inflammatory, cytotoxic, and sedative activities were also identified. However, at present, the developed drugs from Valeriana are far from sufficient. We further discussed the pharmacological effects, effective constituents, and mechanisms directly related to the traditional clinical applications of Valeriana, revealing that only several species and their essential oils were well developed to treat insomnia. To effectively promote the utilization of resources, more Valeriana species as well as their different medicinal parts should be the focus of future related studies. Clinical studies should be performed based on the traditional efficacies of Valeriana to facilitate their use in treating diseases of nervous, cardiovascular, and digestive systems, inflammation, and gynecology. Future studies should also focus on developing effective fractions or active compounds of Valeriana into new drugs to treat diseases associated with neurodegeneration, cardiovascular, and cerebrovascular, inflammation and tumors. Our review will promote the development and utilization of potential drugs in Valeriana and avoid wasting their medicinal resources.

Three new germacrane-type sesquiterpenoids, heishuixiecaoline A–C (compounds 1–3), were isolated along with ten known compounds 4–13 from fraction of Valeriana amurensis roots and rhizomes effective against Alzheimer’s disease (AD). The structures of 1–3 were elucidated on the basis of their spectroscopic data. We also investigated the protective effect of compounds 1–13 on the neurotoxicity of PC12 cells induced by amyloid-beta (Aβ_25–25), respectively. As a result, germacrane-type sesquiterpenoids 1–4 and lignans 5–7 were seen to afford protection against Aβ-induced toxicity in PC 12 cells. This study will contribute to revealing the chemical basis for the therapeutic effect of V. amurensis against AD.

Four new withanolides named dmetelins A–D (compounds 1–4), along with the known compound 7α,27-dihydroxy-1-oxo-witha-2,5,24-trienolide (5) were isolated from the leaves of Datura metel L. (Solanaceae). Their structures were elucidated on the basis of detailed analysis of 1D and 2D NMR and mass spectrometry data. All the compounds were evaluated for their inhibitory effects on lipopolysaccharide (LPS)-induced nitric oxide (NO) production in RAW264.7 cells. Compounds 1, 4 and 5 showed significant inhibitory activities, and compounds 2 and 3 showed moderate inhibitory activities with IC₅₀ values of 17.8, 11.6, 14.9, 33.3 and 28.6 μM, respectively.