Apoptotic Potential and Antitumor Efficacy of Trilliumoside A: A New Steroidal Saponin Isolated from Rhizomes of Trillium govanianum.

Natural product-derived molecules exhibit potential as anticancer agents. Trilliumoside A, a new steroidal saponin, was obtained from rhizomes of Trillium govanianum, and its anticancer activity was investigated in the presented study. Trilliumoside A was investigated in a panel of cell lines, and it exhibited promising cytotoxic activity on the A549 cells (human lung cancer cells) with an IC50 of 1.83 µM. The mechanism of cell death induced by Trilliumoside A in A549 cells and its anticancer potential in murine tumor models (EAC and EAT) were presented in the current research. Trilliumoside A was found to induce apoptosis in A549 cells by increasing the expression of various apoptotic proteins, such as Bax, Puma, cytochrome C, cleaved PARP, and cleaved caspase 3. Additionally, Trilliumoside A regulates the expression of p53, CDK2, and Cyclin A by decreasing the mitochondrial membrane potential, elevating reactive oxygen species, and stopping the growth of A549 cells in the synthesis phase (S) of the cell cycle. Trilliumoside A showed a considerable reduction in the tumor volume, the amount of ascitic fluid, and the total cell number without affecting the body weight of animals. Our results demonstrate that Trilliumoside A inhibits the proliferation of human lung cancer cells by inducing DNA damage, arresting the cell cycle, and activating the mitochondrial signaling pathway. The study demonstrated the potential of Trilliumoside A as a potential anticancer agent.

Biotransformation of eugenol by an endophytic fungus Daldinia sp. IIIMF4010 isolated from Rosmarinus officinalis.

Natural value-added compounds produced from biological sources have attained immense significance in medicinal, food, flavourings, and agrochemical industries. Further, biotransformation is a powerful tool used to produce value-added compounds cost-effectively and selectively. In the present study, biotransformation of eugenol using an endophytic fungus Daldinia sp. IIIMF4010 isolated from the fresh leaves of the plant Rosmarinus officinalis leads to the production of two known value-added compounds. The biotransformation reaction of eugenol (50 mM) resulted in the production of eugenol-ß-D-glucopyranoside (6.2%) and vanillin (21.8%). These biotransformed products were further characterized by liquid chromatography-mass spectroscopy (LC-MS) and nuclear magnetic resonance (NMR).

In-vitro anti-sickling potential of baicalin and naringenin isolated from Oroxylum indicum and Citrus aurantium on human sickle red blood cells.

Sickle cell disease (SCD) is a rare inherited disorder in which red blood cells (RBCs) under oxidative stress have altered sickle shape resulting in clinical complications. In this study, a library of pure natural products were screened to see their effectiveness in preventing sickling induced in blood samples of SCA patients, ex-vivo. The results indicated that baicalin (1) and naringenin (2), reduced sickling by 46.03 and 37.48 percent, respectively, compared to positive control, 4-hydroxybenzoic acid (4-HBA), which inhibited RBC sickling by 56.87 percent. As a result of this screening, two compounds, baicalin (1) and naringenin (2), have been identified as potent sickling inhibitors. Study has clearly shown promising role of flavonoids for the management of SCD crisis for that not effective therapy is available. These phytochemicals or plant extracts can be explored further as an alternative anti-sickling remedy, owing to their high efficacy in the management of SCD crisis.

Trilliumosides K and L, two novel steroidal saponins from rhizomes of Trillium govanianum, as potent anti-cancer agents targeting apoptosis in the A-549 cancer cell line.

Two novel steroidal saponins, trilliumosides K (1) and L (2), were isolated from the rhizomes of Trillium govanianum led by bioactivity-guided phytochemical investigation along with seven known compounds: govanoside D (3), protodioscin (4), borassoside E (5), 20-hydroxyecdysone (6), 5,20-hydroxyecdysone (7), govanic acid (8), and diosgenin (9). The structure of novel compounds 1-2 was established using analysis of spectroscopic data including 1D and 2D nuclear magnetic resonance (NMR) and high resolution mass spectrometry (HR-ESI-MS) data. All isolated compounds were evaluated for in vitro cytotoxic activity against a panel of human cancer cell lines. Compound 1 showed significant cytotoxic activity against the A-549 (Lung) and SW-620 (Colon) cancer cell lines with IC50 values of 1.83 and 1.85 µM, respectively whereas the IC50 value of Compound 2 against the A-549 cell line was found to be 1.79 µM. Among the previously known compounds 3, 5, and 9, the cytotoxic IC50 values were found to be in the range of 5-10 µM. Comprehensive anti-cancer investigation revealed that Compound 2 inhibited in vitro migration and colony-forming capability in the A-549 cell line. Additionally, the mechanistic analysis of Compound 2 on the A-549 cell line indicated distinctive alterations in nuclear morphology, increased reactive oxygen species (ROS) production, and decreased levels of mitochondrial membrane potential (MMP). By upregulating the pro-apoptotic protein BAX and downregulating the anti-apoptotic protein BCL-2, the aforementioned actions eventually cause apoptosis, a crucial hallmark in cancer research, which activates Caspase-3. To the best of our knowledge, this study reports the first mechanistic anti-cancer evaluation of the compounds isolated from the rhizomes of T. govanianum with remarkable cytotoxic activity in the desired micromolar range.