Self-assembled natural small molecule diterpene acids with favorable anticancer activity and biosafety for synergistically enhanced antitumor chemotherapy

Four new self-assembled natural small molecule tricyclic diterpene acids with favorable anticancer activity were discovered for construction of biocompatible antitumor drugs for highly efficient, safe, and synergistic antitumor chemotherapy.

New Labdanes with Antimicrobial and Acaricidal Activity: Terpenes of Callitris and Widdringtonia (Cupressaceae)

In spite of the evidence for antimicrobial and acaricidal effects in ethnobotanical reports of Callitris and Widdringtonia, the diterpene acids from Widdringtonia have never been described and no comparison to the Australian clade sister genus Callitris has been made. The critically endangered South African Clanwilliam cedar, Widdringtonia wallichii (syn. W. cedarbergensis), of the Cederberg Mountains was once prized for its enduring fragrant timbers and an essential oil that gives an aroma comparable to better known Mediterranean cedars, predominantly comprised by widdrol, cedrol, and thujopsene. In South Africa, two other ‘cedars’ are known, which are called W. nodiflora and W. schwarzii, but, until now, their chemical similarity to W. wallichii has not been investigated. Much like Widdringtonia, Callitris was once prized for its termite resistant timbers and an ‘earthy’ essential oil, but predominantly guaiol. The current study demonstrates that the essential oils were similar across all three species of Widdringtonia and two known non-volatile diterpene acids were identified in leaves: the pimaradiene sandaracopimaric acid (1) and the labdane Z-communic acid (2) with a lower yield of the E-isomer (3). Additionally, in the leaves of the three species, the structures of five new antimicrobial labdanes were assigned: 12-hydroxy-8R,17-epoxy-isocommunic acid (4), 8S-formyl-isocommunic acid (5), 8R,17-epoxy-isocommunic acid (6), 8R-17R-epoxy-E-communic acid (7), and 8R-17-epoxy-E-communic acid (8). Australian Callitris columellaris (syn. C. glaucophylla) also produced 1 and its isomer isopimaric acid, pisiferal (9), and pisiferic acid (10) from its leaves. Callitris endlicheri (Parl.) F.M.Bailey yielded isoozic acid (11) as the only major diterpene. Diterpenes 4–6, pisiferic acid (10), spathulenol, and guaiol (12) demonstrated antimicrobial and acaricidal activity.

Comparative Quantitative Analysis of Diterpene Acids in Raw Material of Salvia officinalis, Salvia tesquicola and Salvia nutans

The quantitative analysis of diterpene acids in raw materials of closely related species of genus Salvia was carried out. The objects of present research were Salvia officinalis L., Salvia tesquicola Klokov and Pobed., Salvia nutans L., which grow in neighboring south (Samara and Orenburg) regions. During analysis different raw materials, such as herbs and leaves, were studied. It was determined that total amount of diterpene acids varies from 1,04% to 1,32% in leaves of different species of Salvia and from 1,13% to 1,67% in herbs of different species of Salvia. The raw material of Salvia nutans contains minimal amount of diterpene acids, but in the raw material of Salvia tesquicola the quantitative analysis shows different results, which depend on the region. The medical raw material of Salvia officinalis, which is cultivated in Samara region, includes sufficient amount of diterpene acids.