Two New Prostaglandin-Like Compounds from Callicarpa arborea Roxb and Their NLRP3 Inflammasome Activation Inhibitory Activity.

Two new prostaglandin-like compounds callicarboric acids A-B (1-2), along with six known compounds (3-8) were isolated from the stems of Callicarpa arborea Roxb. Their structures were determined with the help of modern spectroscopic techniques such as NMR, UV, IR, HR-ESI-MS, ECD, and ORD with the assistance of quantum chemical calculations. Compound 1 exhibited remarkable anti-NLRP3 inflammasome activation potential, demonstrating an IC50 value of 0.74 µM. Additionally, by reducing GSDMD-NT production, inhibiting caspase-1 activation, and suppressing IL-1ß secretion, it effectively mitigated NLRP3 inflammasome-induced pyroptosis in J774A.1 cells. These findings indicate that compound 1 possesses the capability to be a valuable candidate for further research and development as an NLRP3 inflammasome inhibitor.

Three New Clerodane Diterpenoids and Their NLRP3 Inflammasome Activation Inhibitory Activity from Callicarpa arborea Roxb.

Three new compounds callicarpenoids A-C (1-3), were isolated from the stems of Callicarpa arborea Roxb together with fifteen known compounds (4-18). The structures of these compounds were elucidated using advanced spectroscopic techniques, including 1D and 2D NMR, UV, IR, HR-ESI-MS, ECD, ORD, and quantum chemical calculations. Compound 3, a rare rearranged diterpenoid with a fused 5/6-ring system demonstrated strong potential as an inhibitor of the NLRP3 inflammasome activation with an IC50 value of 3.153 µM. It effectively reduced GSDMD-NT production, inhibited caspase-1 activation, and suppressed IL-1ß secretion, thereby mitigating NLRP3 inflammasome-induced pyroptosis in J774A.1 cells. These findings suggest that compound 3 warrants further research and development as a promising NLRP3 inflammasome inhibitor.

Wulfenioidins D-N, Structurally Diverse Diterpenoids with Anti-Zika Virus Activity Isolated from Orthosiphon wulfenioides.

Eleven diterpenoids, wulfenioidins D-N (1-11), classified into five distinct carbon skeletons with one unreported framework, and four modified abietane diterpenoids were isolated from the whole plant of Orthosiphon wulfenioides. The structures and absolute configurations were characterized by spectroscopic methods, single-crystal X-ray diffraction, and electronic circular dichroism analyses. Compounds 3 and 5 exhibited activity against Zika virus (ZIKV) with EC50 values of 8.07 and 8.50 µM, respectively, and showed no significant cytotoxicity toward Vero cells at 100 µM. Western blot and immunofluorescence experiments showed that compounds 3 and 5 interfered with the replication of the ZIKV by inhibiting the expression of the ZIKV envelope (E) protein.

Callicarpanes A-L, Twelve New Clerodane Diterpenoids with NLRP3 Inflammasome Inhibitory Activity from Callicarpa integerrima.

Twelve new clerodane diterpenoids named callicarpanes A-L (1-12), together with eight known compounds (13-20), were isolated from Callicarpa integerrima. Their structures were determined by comprehensive spectroscopic data. The calculated chemical shifts were used to identify relative configurations using DP4+ analysis. The absolute configurations (AC) were assigned based on quantum chemical calculations and X-ray single-crystal diffraction methods. Compounds 1, 3, 5, 9, 10, 12, 15, 16, and 19 showed significant inhibitory activity for NLRP3 inflammasome activation, with the IC50 against lactate dehydrogenase (LDH) release ranging from 0.08 to 4.78 µM. Further study revealed that compound 10 repressed IL-1ß secretion and caspase-1 maturation in J774A.1 cell as well as blocked macrophage pyroptosis.

Callintegers A and B, Unusual Tricyclo[4.4.0.09,10]tetradecane Clerodane Diterpenoids from Callicarpa integerrima with Inhibitory Effects on NLRP3 Inflammasome Activation.

Callintegers A (1) and B (2), unprecedented clerodane norditerpenoids based on a novel carbon skeleton, were isolated from Callicarpa integerrima. Compounds 1 and 2 possess a novel 6/6/6-fused tricyclic ring system. Their structures and absolute configurations were determined by quantum chemical calculations, spectroscopic analysis, and single-crystal X-ray diffraction methods. Biological evaluation showed that compound 2 inhibited IL-1ß secretion in a dose-dependent manner with an IC50 value of 5.5 ± 3.2 µM. Caspase-1 maturation and IL-1ß secretion were also reduced, indicating that compound 2 impaired NLRP3 inflammasome activation.

Green synthesis, characterization, and antibacterial activity of silver nanoparticles using stem extract of Zanthoxylum armatum.

In this study, we report the green synthesis of silver nanoparticles (AgNPs) using Zanthoxylum armatum stem extract. The characteristic absorption at 385 nm suggested synthesis of AgNPs which was further confirmed by SEM, with a size in the range of 46.66 nm to 60.12 nm and a spherical shape, having an FCC structure, analyzed by XRD. FTIR analysis revealed the presence of phenol and secondary alcohol groups over the AgNPS. The elemental composition was further investigated by FESEM-EDX analysis which revealed the presence of silver in the synthesis nanoparticles. The synthesized silver nanoparticles exhibited antimicrobial activity against tested microorganisms with a zone of inhibition of 21 mm for Staphylococcus aureus, 17 mm for Pseudomonas aeruginosa, 18 mm for Salmonella enteric, and 18 mm for Escherichia coli. Overall, the results showed that the green silver nanoparticles could be safe, as they are capable of potential antimicrobial activity against S. aureus.

Green synthesis, characterization, antibacterial activity of metal nanoparticles and composite oxides using leaves extract of Ocimum basilicum L.

Nanoparticles plays a key role in the development of novel antibacterial substances against various pathogenic microorganisms. These nanoparticles due to their smaller size could be very effective as they can improve the antibacterial activity through lysis of bacterial cell wall. In the present research work, ZnO, MgO, NiO, AlO nanoparticles, and MgNiO, and AlZnO composite oxides were synthesized by green method from Ocimum basilicum leaves extract. The nanoparticles formed were evaluated using FTIR, XRD, EDX, and SEM to confirm the formation of NPs and to determine the morphology, elemental composition, shape and size, composition, and nature of bonds present in the NPs. Further, the NPs were tested for their antibacterial activity. In particular, ZnO NPs showed a good inhibitory effect against Pseudomonas aeruginosa with 20 mm zone of inhibition. Hence, the process reported herein could be optimized for large-scale preparation of NPs. RESEARCH HIGHLIGHTS: Green synthesis of ZnO, MgO, NiO, AlO nanoparticles, and MgNiO, and AlZnO composite oxides using Ocimum basilicum leaves extract NPs were characterized by various established characterization techniques like FTIR, XRD, EDX, and SEM. NPs showed antibacterial activity which was investigated by agar well diffusion method against Bacillus cereus, Escherichia coli, Klebsiella pneumoniae, Pseudomonas aeruginosa, and Staphylococcus aureus. The method proved to be very simple, cost-efficient, and convenient.

Phytochemical screening, green synthesis of gold nanoparticles, and antibacterial activity using seeds extract of Ricinus communis L.

In the current research study, the phytochemical tests of the Ricinus communis L methanolic extract detected the presence of coumarin, reducing sugar, emodines, terpenoids, flavonoids, and steroids while water extract showed the presence of alkaloids, terpenoids, steroids, and soluble starch. The methanolic extract was further subjected to synthesize Au nanoparticles. The synthesized nanoparticles were confirmed by UV-Vis through the appearance of a peak at 550 nm which correspond to the existence of Au nanoparticles. The size and morphology of synthesized nanoparticle were further studied by the dynamic light scattering technique which shows that nanoparticles were in the range of 100 nm which were further confirmed by transmission electron microscopy. The synthesized nanoparticles and extracts were tested against different bacterial strains. The results revealed that methanolic extract showed maximum inhibition of 19.5 mm against Klebsiella pneumoniae and 20.33 mm against Bacillus cereus while water extract showed maximum inhibition of 18.16 mm against Pseudomonas aeruginosa and 19.33 mm against B. cereus. On the other hand, Au nanoparticles showed maximum inhibition of 18.5 mm against Escherichia coli.

The Effect of AlI3 Nanoadditive on the Thermal Behavior of PMMA Subjected to Thermoanalytical Py-GC-MS Technique.

Thermal degradation of polymethylmethacrylate (PMMA) was studied by using inorganic salt of aluminum triiodide (AlI3). The composites of PMMA were prepared with AlI3 by changing the concentration of the AlI3 additive from 2% to 10% (w/w). The PMMA composites with AlI3 were characterized by TGA, DTG, SEM, FTIR, HBT, and Py-GC-MS techniques. The FTIR peaks of PMMA composite at 1316, 786, and 693 cm-1 justify the chemical association between PMMA and AlI3. TGA study shows that the stability of PMMA is enhanced by the addition of the AlI3 additive. SEM analysis represented that there is a relationship between polymer and additive when they are mixed at the molecular level. The horizontal burning test (HBT) also confirmed that the AlI3 additive produced the flame retarding properties in PMMA polymer. The burning rate of composite with 10% of AlI3 additive decreases five times as much as compared to pure PMMA polymer. Py-GC-MS analysis deduced that PMMA composite produced less toxic and environment-friendly substances (CO2) by the influence of AlI3 additive as compared to neat PMMA.

Toonaones A-I, limonoids with NLRP3 inflammasome inhibitory activity from Toona ciliata M. Roem.

Nine undescribed limonoids, 18(13 â†’ 14)-abeo-15ß,21-dihydroxy-24,25,26,27-tetranor-3,7-dioxoapotirucalla-1,9(11),13(17),20(22)-tetraen-23,21-olide (Toonaone A), 21-hydroxy-24,25,26,27-tetranor-3,7,15-trioxoapotirucalla-1,9(11),20(22)-trien-23,21-olide (Toonaone B), 7α,21-dihydroxy-12α-isobutyryl-24,25,26,27-tetranor-3,15-dioxoapotirucalla-1,20(22)-dien-23,21-olide (Toonaone C), 7,8-seco-7-methyl ester-11ß-acetoxy-14ß,15ß-epoxy-21-hydroxy-24,25,26,27-tetranor-3-oxoapotirucalla-1,8(30),20(22)-trien-23,21-olide (Toonaone D), 7,8-seco-7-methyl ester-11ß-acetoxy-14ß,15ß-epoxy-23-hydroxy-24,25,26,27-tetranor-3-oxoapotirucalla-1,8(30),20(22)-trien-21,23-olide (Toonaone E), 7,8-seco-7-methyl ester-11ß-acetoxy-14ß,15ß-epoxy-6ß,21-dihydroxy-24,25,26,27-tetranor-3-oxoapotirucalla-1,8(30),20(22)-trien-23,21-olide (Toonaone F), 7,8-seco-7-methyl ester-14ß,15ß-epoxy-8α,21-dihydroxy-24,25,26,27-tetranor-3-oxoapotirucalla-1,20(22)-dien-23,21-olide (Toonaone G), 7,8-seco-7-methyl ester-14ß,15ß-epoxy-6ß,8α,21-trihydroxy-24,25,26,27-tetranor-3-oxoapotirucalla-1,20(22)-dien-23,21-olide (Toonaone H), 7,8-seco-7-methyl ester-14ß,15ß-epoxy-6ß,8α,21-trihydroxy-24,25,26,27-tetranor-3-oxoapotirucalla-1,20(22)-dien-21,23-diimide (Toonaone I), and five known analogues were isolated from the twigs of Toona ciliata M. Roem. (Meliaceae). Toonaone A possesses the first rare 18(13 â†’ 14)-abeo-limonoid skeleton reported from the genus Toona. Their structures were elucidated using spectroscopic data analyses and quantum chemistry calculations. Biological evaluation showed that toonaone C, toonaone D, toonaone G, toonaciliatavarin F, and toonaciliatavarin G exhibited significant anti-NLRP3 inflammasome activity with IC50 values ranging from 3.74 to 18.7 µM. GMDMD, IL-1ß, and caspase-1 analyses suggested that toonaone D inhibited NLRP3 inflammasome activation and blocked macrophage pyroptosis.

Triterpenoids from Ganoderma gibbosum: A Class of Sensitizers of FLC-Resistant Candida albicans to Fluconazole.

Fungal drug resistance is a major health threat, and reports of clinical resistance worldwide are becoming increasingly common. In a research program to discover new molecules to help overcome this problem, 14 new lanostane-type triterpenoids, gibbosicolids A-G (2-8) and gibbosic acids I-O (9-15), were isolated from the fruiting bodies of Ganoderma gibbosum, along with seven known triterpenoid derivatives. These compounds featured high levels of oxidation, epimerization, and γ-lactonization. Structures were elucidated by comprehensive spectroscopic analyses and HRMS data. Absolute configurations were assigned based on quantum chemical calculations, including calculated chemical shift with DP4+ analysis, coupling constants, and electronic circular dichroism (ECD) methods. Results show that the calculated NMR with DP4+ analysis could not reliably establish the overall spatial configuration of molecules possessing independent and free-rotational stereoclusters. All these compounds significantly increased the sensitivity of fluconazole (FLC)-resistant C. albicans to FLC. Compounds 2, 5, 9, 12, 16, 17, and 21 exhibited strong antifungal activity against FLC-resistant C. albicans when combined with FLC, with MIC50 values ranging from 3.8 to 8.8 µg/mL.