Triterpenoids are the most representative group of phytochemicals, as they comprise more than 20,000 recognized molecules. These compounds are biosynthesized in plants via squalene cyclization, a C30 hydrocarbon that is considered to be the precursor of all steroids. Due to their low hydrophilicity, triterpenes were considered to be inactive for a long period of time; however, evidence regarding their wide range of pharmacological activities is emerging, and elegant studies have highlighted these activities. Several triterpenic skeletons have been described, including some that have presented with pentacyclic features, such as oleanolic and ursolic acids. These compounds have displayed incontestable biological activity, such as antibacterial, antiviral, and antiprotozoal effects, which were not included in a single review until now. Thus, the present review investigates the potential use of these triterpenes against human pathogens, including their mechanisms of action, via in vivo studies, and the future perspectives about the use of compounds for human or even animal health are also discussed.

https://downloads.hindawi.com/journals/ecam/2015/620472.pdf

Antimicrobial Activity of Oleanolic and Ursolic Acids: An Update

Antitussive, expectorant and anti-inflammatory activities of four alkaloids isolated from Bulbus of Fritillaria wabuensis

Pharmacological evaluation of Alstonia scholaris: Anti-tussive, anti-asthmatic and expectorant activities

Antitussive, expectorant and anti-inflammatory alkaloids from Bulbus Fritillariae Cirrhosae

To discover new anti-cancer agents with multi-effect and low toxicity, a series of ligustrazine derivatives were synthesized using several effective anti-tumor ingredients of Shiquandabu Wan as starting materials. Our idea was enlightened by the "combination principle" in drug discovery. The ligustrazine derivatives' anti-tumor activities were evaluated on the HCT-8, Bel-7402, BGC-823, A-549 and A2780 human cancer cell lines. In addition the angiogenesis activities were valued by the chick chorioallantoic membrane (CAM) assay. 1,7-bis(4-(3,5,6-Trimethylpyrazin-2-yl)-3-methoxyphenyl)-1,6-heptadiene-3,5-dione (4) and 3 α,12 α-dihydroxy-5β-dholanic acid-3,5,6-trimethylpyrazin-2-methyl ester (5) not only displayed antiproliferative activities on these cancer cells, but also dramatically suppressed normal angiogenesis in CAM. The LD₅₀ value of the compound 5 exceeded 3.0 g/kg by oral administration in mice.

https://www.mdpi.com/1420-3049/17/5/4972/pdf

Synthesis and biological evaluation of new ligustrazine derivatives as anti-tumor agents.

Structural analysis and antitussive evaluation of five novel esters of verticinone and bile acids.

The purpose of this work was to search for potential drugs with potent antitussive and expectorant activities as well as a low toxicity, but without addictive properties. Cholic acid-verticinone ester (CA-Ver) was synthesized based on the clearly elucidated antitussive and expectorant activities of verticinone in bulbs of Fritillaria and different bile acids in Snake Bile. In our previous study, CA-Ver showed a much more potent activity than codeine phosphate. This study was carried out to investigate the central antitussive mechanism and the addictive evaluation of CA-Ver. Testing on a capsaicin-induced cough model of mice pretreated with naloxone, a non-selective opioid receptor antagonist, was performed for the observation of CA-Ver's central antitussive mechanism. We then took naloxone-induced withdrawal tests of mice for the judgment of CA-Ver's addiction. Lastly, we determined the opioid dependence of CA-Ver in the guinea pig ileum. The test on the capsaicin-induced cough model showed that naloxone could block the antitussive effect of CA-Ver, suggesting the antitussive mechanism of CA-Ver was related to the central opioid receptors. The naloxone-urged withdrawal tests of the mice showed that CA-Ver was not addictive, and the test of the opioid dependence in the guinea pig ileum showed that CA-Ver had no withdrawal response. These findings suggested that CA-Ver deserved attention for its potent antitussive effects related to the central opioid receptors, but without addiction, and had a good development perspective.

/pdf/addictive-evaluation-of-cholic-acid-verticinone-ester-a-4j2y19byq9.pdf

Addictive evaluation of cholic acid-verticinone ester, a potential cough therapeutic agent with agonist action of opioid receptor.

Two new triterpenoids, 1 and 2, were isolated from the hepatoprotective AcOEt fraction of the roots of Actinidia chinensis, together with eight known 12-en-28-oic acids of oleanane or ursane type, 3-10. The two new compounds were elucidated as 2alpha,3beta-dihydroxyurs-12-en-28,30-olide (1) and 2alpha,3beta,24-trihydroxyurs-12-en-28,30-olide (2), on the basis of spectroscopic (IR, NMR, and MS) analyses. The chemotaxonomic significances of some triterpenoids were also discussed.

Hui Wang

Papers

Structural analysis and antitussive evaluation of five novel esters of verticinone and bile acids.

Addictive evaluation of cholic acid-verticinone ester, a potential cough therapeutic agent with agonist action of opioid receptor.

Triterpenoids from the Roots of Actinidia chinensis