Hovendulcisic acid A-D: four novel ceanothane-type triterpenoids from Hovenia dulcis stems with anticancer properties.

Sixteen ceanothane-type triterpenoids, including four new compounds-hovendulcisic acids A-D (1-4) -were purified from the stems of Hovenia dulcis Thunb. The structures of 1-4 were confirmed by comprehensive means including ECD and quantum chemical calculations. Putative biosynthetic pathways of 1-16 were proposed, and 3, 5, and 15 exhibited antitumor activity on A549 and MDA-MB-231 cells.

Natural L-type calcium channels antagonists from Chinese medicine.

L-type calcium channels (LTCCs), the largest subfamily of voltage-gated calcium channels (VGCCs), are the main channels for Ca2+ influx during extracellular excitation. LTCCs are widely present in excitable cells, especially cardiac and cardiovascular smooth muscle cells, and participate in various Ca2+-dependent processes. LTCCs have been considered as worthy drug target for cardiovascular, neurological and psychological diseases for decades. Natural products from Traditional Chinese medicine (TCM) have shown the potential as new drugs for the treatment of LTCCs related diseases. In this review, the basic structure, function of LTCCs, and the related human diseases caused by structural or functional abnormalities of LTCCs, and the natural LTCCs antagonist and their potential usages were summarized.

Hovenianin A Alleviates Hepatic Fibrosis by Inhibiting the PI3K/AKT Pathway in TGF-ß1-Induced HSCs Based on Network Pharmacology and Transcriptomic Analysis.

Hepatic fibrosis is a global health problem, which currently has no FDA approved antifibrotic therapy yet. This study aimed to explore the mechanism of Hovenia genus in the treatment of hepatic fibrosis by an integrative strategy combining network pharmacology analysis, molecular docking, transcriptomics and experimental validation. The traditional Chinese medicine systems pharmacology (TCMSP) database and literatures were used to collect the components of Hovenia genus. Public databases including GeneCards, TTD, PharmGkb were used to acquire the putative targets. The GO and KEGG analysis were applied to explore the underlying mechanisms. Furthermore, The TGF-ß1 induced hepatic stellate cells (HSCs) model were performed to evaluate the anti-hepatic fibrosis activity of Hovenia genus. The RT-qPCR, Western blotting and flow cytometry experiments were used to validate the anti-hepatic fibrosis mechanisms of Hovenianin A. The KEGG analysis of network pharmacology and transcriptomics revealed that the core targets mainly enriched in PI3K-Akt signaling pathways. The cell screening results indicated flavonoids were the main active ingredients of Hovenia. Hovenianin A, a bioactive bisflavonol, was validated to promote the apoptosis of HSCs by inhibiting PI3K-Akt pathway. Molecular docking further corroborated the binding sites between Hovenianin A and AKT1. In summary, Hovenia may have therapeutic effects on liver fibrosis by modulating the PI3K-Akt apoptosis pathway. Our findings may facilitate the development of Hovenia genus, which could help to treat liver fibrosis in the future.

The pharmacology, pharmacokinetics, and toxicity of spinosin: A mini review.

Spinosin, a natural flavone-C-glycoside that is mainly isolated from the seeds of Ziziphus jujuba Mill. var. spinosa. It exerts the effects to ameliorate the neurological disorders, such as hypnosis effects, improvement of cognitive function, sedation effects, and anxiolytic effects, as well as anti-melanogenic effect, cardioprotective effects, and anti-cancer activity. However, the insufficient basic research, unclear mechanisms, and poor bioavailability may limit the prospects of spinosin in clinical utilization. In this review, we comprehensively summarized the latest information on the pharmacology, pharmacokinetics, toxicity, and NMR characteristic of spinosin, to evaluate its potential therapeutic for clinical application, hoping to provide some rational perspective for the innovative agent development and usage of spinosin in future.

Traditional Uses, Phytochemistry, Pharmacology, Quality Control, Industrial Application, Pharmacokinetics and Network Pharmacology of Pogostemon cablin: A Comprehensive Review.

Pogostemonis Herba (PH) is the dried aerial parts of Pogostemon cablin (Blanco) Benth, which is mainly distributed and used in Asian countries. PH is an aromatic damp-resolving drug in traditional Chinese medicine (TCM), which is usually used for the treatment of vomiting, chest tension, tiredness, abdominal pain, diarrhea, and headache. In this review, the summary of chemical constituents in the aerial parts, biological activities, history of uses, quality control methods, industrial applications, pharmacokinetics and network pharmacology are reported. By collating the chemical constituents of various parts of PH, a total of 174 components were identified, including 66 terpenes, 6 pyrones, 40 flavonoids, 21 phenylpropanoids, 9 steroids, 4 polysaccharides and 28 others. Pharmacological research has found that PH possesses multi-pharmacological activities, including regulating the gastrointestinal tract, inhibition of pathogenic microorganisms, and anti-inflammation, which provide more scientific interpretation for the clinical usage of PH. In addition, the shortcomings of the current research on PH and the recommendation of future studies on PH are analyzed. We hope this review can provide some insight for further research and applications of PH in future.