Context: Podophyllotoxin is a natural product that inhibits the polymerization of tubulin and has served as a prototype for the development of diverse antitumor agents in clinical use, such as etoposide, teniposide and etopophos. Reumacon, another semisynthetic derivative, reached its clinical phase for the treatment of rheumatoid arthritis. Objective: This study investigated the analgesic and anti-inflammatory properties of three compound derivatives from podophyllotoxin. Materials and methods: During a phytochemical study performed on Juniperus thurifera Linne (Cupressaceae) leaves, among other products, several cyclolignans, such as podophyllotoxin, deoxypodophyllotoxin, deoxypicropodophyllotoxin and thuriferic acid were isolated. These compounds, obtained afterwards through semisynthesis, were assayed as analgesic and anti-inflammatory agents. Additionally, the cytotoxic activity of thuriferic acid was evaluated in three cancer cell lines, P-388, A-549 and HT-29, and these data were compared with previous cytotoxicity results obtained for the other three compounds. Results: Analgesic activity results showed that deoxypicropodophyllin is as effective as deoxypodophyllotoxin to inhibit nociceptive perception induced by acetic acid in mice (77.8% ± 4.1% and 71.3% ± 6.5%, respectively), while its cytotoxicity [1.01 × 10⁻⁷ (GI₅₀ M)] is 100-fold less. Other set of experiments showed that thuriferic acid, a derivative of podophyllotoxin a thousand times less citotoxic [1.21 × 10⁻⁵ (GI₅₀ M)] than deoxypodophyllotoxin, caused significant inhibition of paw edema development in the carrageenan-induced inflammation test (63.4% ± 3.3%), effect comparable to those of deoxypodophyllotoxin (66.3% ± 4.4%), and the standard drug indomethacin (61.5% ± 2.5%). Conclusion: We conclude that deoxypicropodophyllotoxin and thuriferic acid are effective in reducing edema formation. However, deoxypicropodophyllin is more related with analgesic activity than anti-inflammatory effect.

Currently, the use of synthetic pesticides is the main method of plant protection applied in agri- and horticulture. However, its excessive use leads to the development of pesticide resistance, a contamination of the environment, toxicity to non-target organisms, and risks for human health. With the ultimate aim of contributing to the develop of a more sustainable pest management, we used the natural product germacrone (compound 1), reported to possess significant insecticidal activity, as starting material for the generation of molecular diversity (2–24). Some of the generated derivatives are natural compounds, such as 1,10-epoxygermacrone (2), 4,5-epoxygermacrone (3), gajutsulactone A (7), germacrol (11), isogermacrone (14), 9-hydroxyeudesma-3,7(11)dien-6-one (19), eudesma-4,7(11),dien-8-one (20), eudesma-3,7(11)-dien-8-one (21) and eudesma-4(15),7(11)-dien-8-one (22). Compounds, 7,11-9,10-diepoxigermacr-4,5-en-8-ol (17), 7,11-epoxieudesma-4,7(11)-dien-8-one (23) and 7,11-epoxieudesma-3,7(11)-dien-8-one (24) are described for the first time. The biocidal activity of most of these compounds was assayed against the tick Hyalomma lusitanicum. The acaricidal effects of compound 24 were four times higher than that of germacrone (1). Compound 2 is an insect antifeedant a thousand times more potent than germacrone against Rhopalosiphum padi, which makes this substance a promising selective antifeedant against this cereal pest.

The phytochemical investigation and evaluation of the antioxidant activity of the leaves, bark, and roots of Cochlospermum angolense Welw ex Oliv—a valued plant that is widely used in traditional Angolan medicine—hold significant importance. Compounds were extracted from the aforementioned plant using acetone and ethanol and identified by HPLC-ESI-MSn. Both extracts demonstrated notable abilities to scavenge 2,2-diphenyl-1-picrylhydrazyl, nitric oxide, and superoxide radicals, as well as to inhibit lipid peroxidation. A HPLC analysis revealed a diverse array of bioactive compounds, including flavonoids, phenols, alkaloids, quinones, and terpenes, which help neutralize free radicals and protect cells against oxidative stress, thereby contributing to the prevention of various diseases. Moreover, the acetone and ethanol extracts proved to be excellent sources of antioxidants. For the first time, the present study identified new compounds never reported in this species, such as (+)-abscisic acid, angustine B, pinobanksin, dihydrogenistein, (−)-8-prenylnaringenin, isoquercetin, samandarine, dihydromyricetin, and eupatoriocromene, in the leaves, bark, and roots, marking a significant advance in the chemical characterization of C. angolense. These findings enhance our understanding of the bioactive phytochemicals and antioxidant properties of C. angolense and open new avenues for future therapeutic and pharmacological research, further supporting its traditional use in Angolan medicine.

Context: Since there is still a great need to search for plant species with antinociceptive and anti-inflammatory activities, Diploptropis purpurea (Rich.) Amshoff (Fabaceae) is studied for the first time. Objective: This evaluates the analgesic and anti-inflammatory activities of the stem methanol extract of Diplotropis purpurea (MEDP). Material and methods: The anti-inflammatory and analgesic effects of MEDP of D. purpurea were evaluated in vivo. The antinociceptive activity was assessed in CD1 male mice were treated by oral gavage with 500 mg/kg of MEDP 30 min before submitting to acetic acid-induced abdominal writhing, hot-plate, and formalin tests. Paws oedema induced by carrageenan, histamine or serotonin were performed in male Sprague–Dawley rats to determinate the anti-inflammatory activity. Results: Oral administration of MEDP produced significant antinociceptive effects on the inflammatory phase in the formalin test [12.0 s versus 72.5 s in carboxymethyl cellulose (CMC) control group]. MEDP produced an analgesic effect in the hot-plate model, although the effect was modest compared to tramadol (40 and 60%, respectively). The oral administration of MEDP in a dose of 500 mg/kg showed maximum inhibition (75.1%) after 0.5 h in carrageenan-induced oedema, but it did not modify histamine or serotonin-induced oedemas. Discussion and conclusion: In the peripheral nociception model, acetic acid-induced abdominal writhing, the MEDP did not show a protective effect, but its analgesic effects were evident in the inflammatory phase of the formalin test and in the hot-plate model. These results show that the anti-inflammatory effect was accompanied by a reduction in the perception of painful stimuli.

Extractos metanólicos de seis plantas pertenecientes a la familia Fabaceae, Albizia adinocephala (J.D.Sm.) Britt. & Rose, Dalbergia brownei (Jacq.) Schinz, Diplotropis purpurea (Rich.) Amshoff, Machaeriumsp., Macroptilium lathyroides (L.) Urb. y de Ormosia coccinea (Aubl.) Jacks, fueron evaluados por el método de dilución en agar en busca de propiedades antimicrobianas. Albizia adinocephala mostró una marcada actividad frente a cepas de Staphylococcus aureus y Staphylococcus aureus resistente a la meticilina (SARM) a concentraciones de 250 y 125 µg/mL, respectivamente; a 500µg/mL, inhibió marcadamente a Escherichia coli y Bacillus subtilis. La actividad de Ormosia coccinea frente a Klebsiella pneumoniae y Staphylococcus aureus fue marcada a 250µg/mL y demostró una actividad entre moderada y marcada frente a cepas resistentes de Klebsiella pneumoniae productora de carbapenemasa (KPC) y SARM (1000 y 500 µg/mL, respectivamente). Machaerium sp. produjo una marcada actividad frente a todas las cepasGram positivas empleadas, resaltando su capacidad para inhibir a SARM (1000µg/mL). De Diplotropis purpurea y Macroptilium lathyroides es preciso resaltar su actividad frente a Klebsiella pneumoniae y Bacillus subtilis, respectivamente. Debido a su capacidad para inhibir SARM, Albizia adinocephala, Machaerium sp. y Ormosia coccinea, que además inhibió KPC, son las especies más interesantes para futuros estudios biodirigidos encaminados a aislar e identificar los principios bioactivos.