Exploring the Biological and Phytochemical Potential of Jordan's Flora: A Review and Update of Eight Selected Genera from Mediterranean Region.

Jordan's flora is known for its rich diversity, with a grand sum of 2978 plant species that span 142 families and 868 genera across four different zones. Eight genera belonging to four different plant families have been recognized for their potential natural medicinal properties within the Mediterranean region. These genera include Chrysanthemum L., Onopordum Vaill. Ex. L., Phagnalon Cass., and Senecio L. from the Asteraceae family, in addition to Clematis L. and Ranunculus L. from the Ranunculaceae family, Anchusa L. from the Boraginaceae family, and Eryngium L. from the Apiaceae family. The selected genera show a wide variety of secondary metabolites with encouraging pharmacological characteristics including antioxidant, antibacterial, cytotoxic, anti-inflammatory, antidiabetic, anti-ulcer, and neuroprotective actions. Further research on these genera and their extracts will potentially result in the formulation of novel and potent natural pharmaceuticals. Overall, Jordan's rich flora provides a valuable resource for exploring and discovering new plant-based medicines.

PPARα and γ Activation Effects of New Nor-triterpenoidal Saponins from the Aerial Parts of Anabasis articulata.

Anabasis articulata, traditionally used to treat diabetes, is rich in saponin content. This study was performed to investigate the agonistic effect of its saponins on peroxisome proliferator-activated receptor-α and peroxisome proliferator-activated receptor-γ in human hepatoma (HepG2) cells to explore the possibility of the involvement of these nuclear receptors in the mechanism of the antidiabetic effect of the plant. Chemical investigation of the n-butanol fraction resulted in the isolation of three new and one known 30-noroleanane triterpenoid saponins. The structures of the new compounds were elucidated as 3ß-hydroxy,23-aldehyde-30-norolean-12,20(29)-dien-28-oic acid-28-O-ß-D-glucopyranosyl ester (1: ), 3ß-O-D-galactopyranosyl-23-aldehyde-30-norolean-12,20(29)-dien-28-oic acid-28-O-ß-D-glucopyranosyl ester (2: ), and 3ß-O-D-xylopyranosyl-30-norolean-12,20(29)-dien-28-oic acid 28-O-ß-D-glucopyranosyl ester (3: ), while the known 30-nortriterpenoidal saponin was identified as boussingoside E (4: ). Although, the isolated saponins (1:  - 4: ) did not show > 1.5-fold activation of peroxisome proliferator-activated receptor-γ, but two of them (1: and 3: ) activated peroxisome proliferator-activated receptor-α to the higher extents of 2.25- and 1.86-fold, respectively. These results suggest that the reported antidiabetic action of the isolated saponins may not solely involve the activation of peroxisome proliferator-activated receptor-γ. However, the agonistic activity of the n-butanol fraction of A. articulata (1.71-fold induction) and two of its saponins (1: and 3: ) towards peroxisome proliferator-activated receptor-α may be beneficial in the cardiovascular condition that is closely associated with diabetes and other metabolic disorders.

Structure-Activity Relationships of Antimicrobial Gallic Acid Derivatives from Pomegranate and Acacia Fruit Extracts against Potato Bacterial Wilt Pathogen.

Bacterial wilts of potato, tomato, pepper, and or eggplant caused by Ralstonia solanacearum are among the most serious plant diseases worldwide. In this study, the issue of developing bactericidal agents from natural sources against R. solanacearum derived from plant extracts was addressed. Extracts prepared from 25 plant species with antiseptic relevance in Egyptian folk medicine were screened for their antimicrobial properties against the potato pathogen R. solancearum by using the disc-zone inhibition assay and microtitre plate dilution method. Plants exhibiting notable antimicrobial activities against the tested pathogen include extracts from Acacia arabica and Punica granatum. Bioactivity-guided fractionation of A. arabica and P. granatum resulted in the isolation of bioactive compounds 3,5-dihydroxy-4-methoxybenzoic acid and gallic acid, in addition to epicatechin. All isolates displayed significant antimicrobial activities against R. solanacearum (MIC values 0.5-9 mg/ml), with 3,5-dihydroxy-4-methoxybenzoic acid being the most effective one with a MIC value of 0.47 mg/ml. We further performed a structure-activity relationship (SAR) study for the inhibition of R. solanacearum growth by ten natural, structurally related benzoic acids.

Triterpenes as uncompetitive inhibitors of α-glucosidase from flowers of Punica granatum L.

The α-glucosidase and maltase inhibitory effects of Punica granatum L. flowers (PGF) were investigated. The methanol extract (PGFMe), n-hexane extract (PGFH), chloroform extract (PGFC) and the remaining water fraction (PGFW) were assayed for their α-glucosidase and maltase inhibitory effects. PGFW showed potent α-glucosidase inhibition with IC50 of 0.8 µg/mL followed by PGFMe (IC50 of 4.0 µg/mL) then PGFC (IC50 of 5.21 µg/mL) in comparison to acarbose (0.9 µM). Due to its selectivity towards α-glucosidase, PGFC was subjected to bioactivity-guided isolation of its main active constituents. Five known compounds (1-5) were identified as ß-sitosterol (1), oleanolic acid (2), ursolic acid (3), p-coumaric acid (4) and apigenin (5). Ursolic and oleanolic acids showed potent α-glucosidase inhibition (IC50 of 39.0 and 35.0 µM, respectively), while they did not show significant maltase inhibition. Kinetic study using the double Lineweaver-Burk plot revealed that ursolic acid uncompetitively inhibited α-glucosidase in comparison with acarbose as a competitive inhibitor.

Anti-estrogenic activity of mansonone G and mansorin A derivatives.

CONTEXT: Mansonone G and mansorin A are major bioactive constituents from Mansonia gagei Drumm (Sterculiaceae) wood, and their mild anti-estrogenic activity was reported previously by the authors. OBJECTIVE: In order to increase the potency of their anti-estrogenic effect and to clarify their binding way to estrogen receptor on a molecular level, several derivatives of both compounds will be prepared and a docking study of the original compounds and their derivatives on estrogen receptor alpha (ERα) was carried out. MATERIALS AND METHODS: The original compounds were isolated from the heartwood of M. gagei. Nine alkyl derivatives were prepared by acetylation, methylation, or adding a basic side chain to the free hydroxyl group of both compounds. The estrogenic/anti-estrogenic activities of the derivatives compared to the original compounds were carried out using ERα competitive binding screen and yeast two-hybrid assay expressing ERα and ERß using concentrations ranging from 10 to 100 µM. RESULTS: Acetyl mansonone G showed a 10-fold increase in its binding ability to ERα compared to mansonone G with an IC50 630 µM. Similarly, methyl mansonone G and acetyl mansonone G showed 50% and 35% inhibition of 17ß-estradiol-induced ß-galactosidase activity at 10 µM in the yeast expressing ERα, and 42% and 30%, respectively, at 10 µM in the yeast expressing ERß. Virtual docking of acetyl mansonone G to ERα showed that it binds, with its acetyl oxygen, in a similar way to the 17ß-OH of estradiol. DISCUSSION AND CONCLUSION: The phenolic hydroxyl group in mansonones and mansorins was not essential for binding to estrogen receptors. In addition, acetyl mansonone G could represent a promising starting material for the synthesis of anti-estrogenic agents.

HCV-NS3/4A protease inhibitory iridoid glucosides and dimeric foliamenthoic acid derivatives from Anarrhinum orientale.

Four new compounds were isolated from the methanol extract of the aerial parts of Anarrhinum orientale: 6'-O-cinnamoylmussaenosidic acid (1), 6'-O-cinnamoyl-8-O-(6'''-O-cinnamoylglucopyranosyl)mussaenosidic acid (2), (2E,6E)-8-{[(2E,6E)-8-hydroxy-2,6-dimethylocta-2,6-dienoyl]oxy}-2,6-dimethylocta-2,6-dienoic acid (3), and (2E,6E)-8-{[(2E,6E)-8-acetoxy-2,6-dimethylocta-2,6-dienoyl]oxy}-2,6-dimethylocta-2,6-dienoic acid (4). The known 8-O-cinnamoylmussaenosidic acid (5) was also identified. All five compounds were tested for inhibition of the hepatitis C virus (HCV) protease. Compounds 1 and 5 exhibited moderate activity, while 2 and 3 showed weak effects. No inhibitory activity on the human serine protease was observed for any of these compounds, which may infer the selectivity toward the viral protease. A computational docking study of the isolated compounds against HCV protease was used to formulate a hypothetical mechanism for the inhibitory activity of the active compounds on the enzymes tested.