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The schistosomicidal and cytotoxic activities of norneolignans isolated fromStyrax pohliiare used to relieve fever. The norneolignans homoegonol [2] and homoegonol glucoside [4] provided the best results against S. mansoni adult worms. At 200 μM, compounds 2 and 4 killed 25% and 50% of the parasites in 120 h, while egonol [1], homoegonol gentiobioside [3], and egonol gentiobioside [5] reduced their motor activity to 12.5%, 12.5%, and 37.5% in 120 h, respectively. With respect to the cytotoxic activity, the IC50values were greater than 800 μM for 1, 5, and 3 and 192.5 and 253.1 μM for 2 and 4, respectively. [ABSTRACT FROM PUBLISHER]

• Determination of C-22 stereocenter configuration for two steroidal saponins through NMR techniques. • Quantification of eight steroidal saponins using an UHPLC-ESI-MS • High antileishmanial activity of steroidal saponins from S. paniculatum leaves, against of L. (L.) amazonensis. Solanum paniculatum L. is species whose fruits are widely consumed in Brazil as a tonic beverage with higher content of steroidal saponins. In this work, we developed an analytical method for the quantification of the eight saponins present in the 70 % ethanol extract from the leaves using ultra-high-performance liquid chromatography coupled to mass spectrometry (UHPLC-MS). Besides, the eight spirostanic saponins were screened for in vitro antileishmanial activity against promastigote and amastigote forms of Leishmania (L.) amazonensis. Substances 1 , 2 and 3 were found to be the most active compounds, with inhibitory concentration (IC 50) values of 8.51 ± 4.38, 10.75 ± 6.85 and 10.45 ± 4.21 μM, respectively, against promastigote forms and effective concentration (EC 50) values of >25, 17.73 ± 0.99 and 19.57 ± 0.84 μM, respectively, against amastigote forms. The cytotoxic test with compounds 1–3 evidenced low toxicity in murine macrophage cells, with values above 50 μM at concentration lower than 25 μM. These findings show that saponins 1–3 should be evaluated in further studies for the treatment of cutaneous leishmaniasis. [ABSTRACT FROM AUTHOR]

Propolis is a natural product widely used in folk medicine. Among its various applications, its antiparasitic properties stand out. Due to its great biodiversity, Brazil is a major producer of several types of propolis. This study proposes to evaluate the leishmanicidal properties of the hydroalcoholic extract of propolis collected in the southern region of Brazil (Brown propolis - HEBP) and its main isolated compounds: abietic acid (1), 13-epi-cupressic acid (2), 13-epi-torulosol (3), dehydroabietic acid (4), cis -communic acid (5) and ent -agatic acid (6). In general, the diterpenes did not show activity against the promastigotes of Leishmania ( Leishmania ) amazonensis at the evaluated concentrations. However, the HEBP was very active with an inhibition concentration of 50% at 8.32 µg/mL. Moreover, transmission electron microscopy (TEM) and scanning electron microscopy (SEM) assays showed morphological and structural alterations in promastigote forms of L . ( L. ) amazonensis when incubated with HEBP.

Propolis is a natural product of great economic and pharmacological importance. The flora surrounding the bee communities is a determining factor in the composition of propolis and therefore in its biological and medicinal properties. Brown propolis is one of the most important types of propolis in Brazil, produced in the southeastern region. The ethanolic extract of a brown propolis sample from Minas Gerais state was chemically characterized for the subsequent development of a RP-HPLC method, validated according to the standards of regulatory agencies. The leishmanicidal activity of this extract was assessed. The brown propolis was characterized by the presence of chemical markers reported on green propolis such as ferulic acid, coumaric acid, caffeic acid, cinnamic acid, baccharin, artepillin and drupanin, indicating a probable origin on Baccharis dracunculifolia. The developed method agreed with the parameters established by the validation guidelines, then proved to be reliable for the analysis of this type of propolis. The brown propolis displayed significant activity against Leishmania amazonensis with IC 50 values of 1.8 and 2.4 μg/ml against the promastigote and amastigote forms, respectively. The studied propolis exhibited promising evidence for use as a natural source against L. amazonensis., (© 2023 John Wiley & Sons Ltd.)

Introduction: Propolis is widely used in folk medicine, and many factors can affect its chemical composition, including abiotic factors that can influence plants and bees. Therefore, analytical methods are powerful techniques in the quality control of such products., Objective: Develop and validate an analytical method for quantifying volatile compounds in Brazilian brown propolis, and evaluate its biological activities., Methods: A gas chromatography flame ionisation detector (GC-FID) analytical method was validated, attending the parameters of international validation guidelines as ANVISA 2017 and ICH 2005, for quantification of compounds present in volatile oils from propolis. Evaluation of cytotoxic, antimicrobial, and leishmanicidal activities of the oil., Results: The compounds 1,8-cineole, terpinen-4-ol, α-copaene, β-caryophyllene, γ-muurolene, nerolidol, spathulenol, and γ-palmitolactone were isolated from the volatile fraction of a Brazilian brown propolis and used in the method validation. All the validation parameters of the method were satisfactory. The volatile fraction displayed a significant leishmanicidal activity, with half maximal inhibition concentration (IC 50 ) = 21.3 μg/mL against amastigote forms and IC 50 = 25.1 μg/mL against promastigote forms of Leishmania amazonensis. The oil also displayed an antibacterial effect by inhibiting the growth of Streptococcus mutans and Staphylococcus aureus at 25 μg/mL and 50 μg/mL, respectively, but it was not cytotoxic against AGP-01, He-La and CHO-K1cell lines, with IC 50 > 100 μg/mL., Conclusion: The GC-FID method can be a useful tool in the quality control of propolis material. The southeast brown propolis showed a high chemical complexity in its volatile fraction, which displayed leishmanicidal activity and bactericidal activity., (© 2020 John Wiley & Sons, Ltd.)

Solanum lycocarpum (Solanaceae), a Brazilian medicinal plant known as "wolf fruit," contains about 1.5% of glycoalkaloids in its dried fruits, consisting mainly of solamargine and solasonine. The present work reports the obtainment of the alkaloidic extract of the S. lycocarpum fruit by acid-base extraction and the isolation of the major alkaloid heterosides by chromatographic means, as well as the evaluation of their in vitro schistosomicidal activities. The in vitro schistosomicidal activities of the alkaloidic extract of S. lycocarpum fruits and its isolated steroidal alkaloids were undertaken against adult worms of Schistosoma mansoni. The alkaloidic extract (20, 32, and 50 μg mL(-1)), solasonine (50 μM), solamargine (32 and 50 μM), and equimolar mixture of glycoalkaloids (20, 32, and 50 μM) lead to the separation of all couple worms and extensive disruption on their teguments, such as sloughing, as well as their deaths within 24 h of incubation. In addition, the alkaloidic extract (10 and 15 μg mL(-1)), solasonine (50 μM), solamargine (10, 15, and 20 μM), and equimolar mixtures of glycoalkaloids (10 and 15 μM) reduced the development of eggs produced by the adult worms. Solamargine, containing the sugar chain moiety chacotriose, was more active than the solasonine, which contains solatriose sugar chain moiety. A synergistic effect was also observed for a mixture of solamargine and solasonine. Therefore, the alkaloidic extract of S. lycocarpum, and its major components, solamargine and solasonine, showed promising schistosomicidal activity.