Evaluations of Anticancer Effects of Combinations of Cisplatin and Tirucallane‐Type Triterpenes Isolated from Amphipterygium adstringens (Schltdl).

Evaluations of Anticancer Effects of Combinations of Cisplatin and Tirucallane-Type Triterpenes Isolated from Amphipterygium adstringens (Schltdl).


Abstract

The cytotoxic activity of combinations of masticadienonic (AMD) or 3αOH-hydroxy-masticadienonic (3αOH-AMD) acids with cisplatin (CDDP) was evaluated against PC3 prostate and HCT116 colon cancer cell lines. Combinations A (half the IC50 value), B (IC50 value), and C (twice the IC50 value) were tested at a 1 : 1 ratio. All AMD plus CDDP combinations demonstrated increased cytotoxic effect, as determined by the sulforhodamine B test, in both cell types. The best combination was B, which showed 93 % and 91 % inhibition of the proliferation of PC3 and HCT116 cells, respectively. It also increased apoptosis in the PC3 cell lines, as evaluated by flow cytometry. However, in vivo tests showed no additional activity from the AMD plus CDDP combinations. These results showed that the increased cytotoxic activity of the combinations in vitro did not reflect in vivo tests. All combinations of 3αOH-AMD plus CDDP exerted antagonistic effects in both cell types.

Evaluation of Cytotoxicity and Antifungal Activity of Friedelanes from Salacia elliptica Roots

Evaluation of Cytotoxicity and Antifungal Activity of Friedelanes from Salacia elliptica Roots


Abstract

Plants from Salacia genus are used in traditional medicine for a wide range of diseases. Previous studies reported bioactive pentacyclic triterpenoids from S. elliptica leaves and branches. In this study, the novel pentacyclic triterpenoid 7α,15α-dihydroxyfriedelan-3-one (1) was obtained from the roots of Salacia elliptica, along with seven known compounds: friedelan-3-one (2), friedelan-3β-ol (3), friedelan-1,3-dione (4), friedelan-3,15-dione (5), 15α-hydroxyfriedelan-3-one (6), 15α,26-dihydroxyfriedelan-3-one (7), and 26-hydroxyfriedelan-3,15-dione (8). Additionally, one steroid, spinasterol (9), was also identified. The chemical structures of all compounds were established through 1H and 13C-NMR. Compound 1 was analysed by additional 2D experiments (HMBC, HSQC, COSY, and NOESY) for complete elucidation. Furthermore, the cytotoxicity of compounds 2, 3, 6, 7 and 8 against the A549 lung cancer cells model was evaluated. The flow cytometry analysis revealed a significant cytotoxic activity similar to that exhibited by the triterpenoid lupeol. Additionally, compounds 2, 3, 6, and 7 were tested for in vitro antifungal activity against Candida, Cryptococcus and Sporothrix strains. However, all compounds showed no activity at the tested concentrations.

Antifungal Activity of Cadinane‐Type Sesquiterpenes from Eupatorium adenophorum against Wood‐Decaying Fungi

Antifungal Activity of Cadinane-Type Sesquiterpenes from Eupatorium adenophorum against Wood-Decaying Fungi


Abstract

The present study aimed to evaluate the antifungal activities of Eupatorium adenophorum against four strains of wood-decaying fungi, including Inonotus hispida, Inonotus obliquus, and Inonotus cuticularis. Bioguided isolation of the methanol extract of E. adenophorum by silica gel column chromatography and high-performance liquid chromatography afforded six cadinane-type sesquiterpenes. Their structures were identified by nuclear magnetic resonance and MS analyses. According to the antifungal results, the inhibition rate of the compound was between 59.85 % and 77.98 % at a concentration of 200 μg/mL. The EC50 values ranged from 74.5 to 187.4 μg/mL.

Exploring the Therapeutic Properties of Alga‐Based Silver Nanoparticles: Anticancer, Antibacterial, and Free Radical Scavenging Capabilities

Exploring the Therapeutic Properties of Alga-Based Silver Nanoparticles: Anticancer, Antibacterial, and Free Radical Scavenging Capabilities


Abstract

The current study was designed to evaluate the antioxidant, anticancer and antimicrobial activities of silver nanoparticles (AgNPs) biosynthesized by Spirulina platensis extract. The biosynthesized silver nanoparticles were characterized using Fourier transform infrared (FT-IR) analysis, scanning electron microscopy (SEM), transmission electron microscopy (TEM) and X-ray diffraction (XRD) analysis. The antioxidant activity of the biosynthesized AgNPs were determined via DPPH radical scavenging assay while its anticancer activity was determined using the MTT assay. The antimicrobial activity of the biosynthesized AgNPs were analyzed by disc diffusion method. Spirulina platensis acts as a reducing and capping agent. The efficacy of silver nanoparticles (AgNPs) in inhibiting the growth of Gram-negative bacteria, specifically Acetobacter, Klebsiella, Proteus vulgaris, and Pseudomonas aeruginosa, was assessed by the utilisation of the diffusion method. The study aimed to evaluate the efficacy of biosynthesized silver nanoparticles (AgNPs) against many strains of Pseudomonas aeruginosa bacteria. The findings of the study revealed that when administered in doses of 50 μl, 75 μl, and 100 μl, the largest observed zone of inhibition corresponded to measurements of 10.5 mm, 14 mm, and 16 mm, respectively. A zone of inhibition with dimensions of 8 mm, 10.5 mm, and 12 mm was detected during testing against Acetobacter at concentrations of 50 μl, 75 μl, and 100 μl, respectively. The findings also indicate that there is a positive correlation between the concentration of AgNP and the DPPH scavenging ability of silver nanoparticles. The percentage of inhibition observed at concentrations of 500 μg/ml, 400 μg/ml, 300 μg/ml, 200 μg/ml, and 100 μg/ml were recorded as 80±1.98, 61±1.98, 52±1.5, 42±1.99, and 36±1.97, respectively. In addition, it was observed that the silver nanoparticles exhibited the greatest antioxidant activity at a concentration of 500 g/ml, with a measured value of 80.89±1.99. The IC-50 values, representing the inhibitory concentration required to achieve 50 % inhibition, were found to be 8.16, 19.15, 30.14, 41.13, and 63.11 at inhibition levels of 36±1.97, 42±1.99, 52±1.5, 61±1.98, and 80±1.98, respectively.

Structurally Diverse Sesquiterpenoids with NO Production and α‐Glucosidase Inhibitory Activities from the Fruits of Schisandra chinensis

Structurally Diverse Sesquiterpenoids with NO Production and α-Glucosidase Inhibitory Activities from the Fruits of Schisandra chinensis


Abstract

Chemical fractionation of the AcOEt partition, generated from the EtOH extract of the fruits of Schisandra chinensis, afforded a series of sesquiterpenyl constituents including two new cadinanes, a new eudesmane, two new widdranes (a handling artefact and a new natural product), a new bisabolane and two new natural cuparane enantiomers, along with 15 known structurally related analogs. Structures of the new compounds were unambiguously characterized by interpretation of detailed spectroscopic data including ESI-MS and 1D/2D NMR, with their absolute configurations being established by electronic circular dichroism (ECD) calculation and induced ECD experiment. The inhibitory effects of all the isolates against α-glucosidase and lipopolysaccharide (LPS) induced nitric oxide (NO) production in murine RAW264.7 macrophages, as well as their antibacterial and cytotoxic potential, were evaluated, with selective compounds showing moderate α-glucosidase and NO inhibitory activity. Notably, canangaterpene III exhibited the most significant NO inhibitory effect with an IC50 value of 31.50±1.49 μM.

A New Harziane Diterpene, Harziaketal A, and a New Sterol, Trichosterol A, from the Marine‐Alga‐Epiphytic Trichoderma sp. Z43

A New Harziane Diterpene, Harziaketal A, and a New Sterol, Trichosterol A, from the Marine-Alga-Epiphytic Trichoderma sp. Z43


Abstract

One new diterpene, harziaketal A (1), and one new highly degraded sterol, trichosterol A (2), along with three known compounds, including one diterpene, harzianone (3), and two steroids, (22E,24R)-5α,6α-epoxy-ergosta-8(14),22-dien-3β,7α-diol (4) and isoergokonin B (5), were isolated from the culture of the marine-alga-epiphytic fungus Trichoderma sp. Z43 by silica gel column chromatography (CC), Sephadex LH-20 CC, and preparative thin-layer chromatography (TLC). Their structures and relative configurations were assigned by nuclear magnetic resonance (NMR) and high resolution electrospray ionisation mass spectrometry (HR-ESI-MS) data, and the absolute configuration of 1 was established by X-ray diffraction. Compound 1 features a hemiketal unit situated at the four-membered ring of harziane-type diterpenes for the first time, while 2 represents the rare occurrence of sterols with rings A and B being degraded. Compounds 1 and 2 displayed weak inhibition against the tested phytoplankton (Amphidinium carterae, Heterocapsa circularisquama, Heterosigma akashiwo, and Prorocentrum donghaiense) with half maximal inhibitory concentration (IC50) ranging from 14 to 53 μg/mL.

Quantification of Phytochemicals and Metal Ions as well as the Determination of Volatile Compounds, Antioxidant, Antimicrobial and Antacid Activities of the Mimosa pudica L. Leaf: Exploration of Neglected and Under‐Utilized Part

Quantification of Phytochemicals and Metal Ions as well as the Determination of Volatile Compounds, Antioxidant, Antimicrobial and Antacid Activities of the Mimosa pudica L. Leaf: Exploration of Neglected and Under-Utilized Part


Abstract

Mimosa pudica L. (MP) is well-known plant in traditional medicinal system, especially in India. Unfortunately, leaves of MP are less explored. To determine the food and nutritional value of the neglected part of Mimosa pudica L. (MP), that is MP leaves, phytochemicals and metal ions of MP were quantified by newly developed HPLC and ICPOES-based methods. The content of phytochemicals observed using HPLC analysis for chlorogenic acid, catechin, and epicatechin was 141.823 (±8.171), 666.621 (±11.432), and 293.175 (±12.743) μg/g, respectively. Using GC/MS/MS analysis, fatty acid like oleic acid were identified. In ICP-OES analysis, a significant content of Na, K, Ca, Cu, Fe, Mg, Mn, and Zn was observed. The observed TPC and TFC for MP leaf extracts was 44.327 (±1.041) mg GAE/ g of wt. and 214.217 (±4.372) mg QCE/ g of wt., respectively. The DPPH assay depicted a strong antioxidant activity of MP leaf extracts with IC50 values of 0.796 (±0.081) mg/mL and a TEAC value of 0.0356 (±0.0003). A significant antacid activity (666 mg MP+400 mg CaCO3 >400 mg CaCO3 ≫666 mg Gelusil) of MP leaves was noticed. The methanolic extract of MP leaves demonstrated anti-microbial activity against Staphylococcus aureus (15±2mm), Pseudomonas aeruginosa (12±2mm) and Escherichia coli (10±2mm). In silico studies confirmed the in vitro results obtained for antioxidant, antiacid, and anti-microbial activities. In addition, in silico studies revealed the anti-cancerous and anti-inflammatory potential of the MP leaves. In summary, this study demonstrated the medicinal significance of MP leaves and the conversion of agro-waste or the under-utilized part of MP into pharmaceutical potent materials. Consequently, the present study highlighted that MP leaves alone have medicinal importance with good nutritional utility and possess large promise in the pharma industry along with improving bio-valorization and the environment.

Isocucurbic Acid Derivatives and Soluble Epoxide Hydroxylase Inhibitors from the Flowers of Chrysanthemum indicum L.

Isocucurbic Acid Derivatives and Soluble Epoxide Hydroxylase Inhibitors from the Flowers of Chrysanthemum indicum L.


Abstract

Soluble epoxide hydrolase (sEH) inhibitory activity guided fractionation and isolation of two new isocucurbic acid derivatives (1 and 2) and nine known compounds (311) from the flowers of Chrysanthemum indicum L. Their structures were elucidated on the basis of spectroscopic data interpretation and comparison with those reported in previous studies. Luteolin (3), acacetin-7-O-β-D-glucopyranoside (6), and methyl 3,4-di-O-caffeoylquinate (10) displayed sEH inhibitory activities with IC50 values ranging from 13.7±3.6 to 20.8±0.4 μM. Enzyme kinetic analysis revealed that 3, 6, and 10 were non-competitive inhibitors with K i values of 14.8±0.5, 31.2±0.8, and 3.9±0.2 μM, respectively. Additionally, molecular docking studies indicated compound 10 had the ability to form six hydrogen bonds at sEH active site, resulting binding energy as low as −9.58 Kcal/mol.

Distinctive Arbutin‐Containing Markers: Chemotaxonomic Significance and Insights Into the Evolution of Proteaceae Phytochemistry

Natural products isolation studies of eight endemic Tasmanian Proteaceae species – Agastachys odorata, Persoonia juniperina, Hakea megadenia, Hakea epiglottis, Orites diversifolius, Orites acicularis,Orites revolutus, and Telopea truncata – and three endemic Australian Proteaceae species Banksia serrata, Banksia praemorsa, and Banksia marginata were undertaken.Two previously unreported glycoside-derived natural products were identified, in addition to four other tremendously rare arbutin esters. The results of this study provide further evidence consistent with the proposal that these distinctive arbutin esters represent markers that can provide valuable insights into the chemical evolution of plant species within the family Proteaceae.

Stimuli‐Responsive and Multifunctional Nanogels

Nanogels represent promising drug delivery systems in the biomedical field, designed to overcome challenges associated with standard treatment approaches. Stimuli-responsive nanogels, often referred to as intelligent materials, have garnered significant attention for their potential to enhance control over properties such as drug release and targeting. Furthermore, researchers have recently explored the application of nanogels in diverse sectors beyond biomedicine including sensing materials, catalysts, or adsorbents for environmental applications. However, to fully harness their potential as practical delivery systems, further research is required to better understand their pharmacokinetic behaviour, interactions between nanogels and bio distributions, as well as toxicities. One promising future application of stimuli-responsive multifunctional nanogels is their use as delivery agents in cancer treatment, offering an alternative to overcome the challenges with conventional approaches. This review discusses various synthetic methods employed in developing nanogels as efficient carriers for drug delivery in cancer treatment. The investigations explore, the key aspects of nanogels, including their multifunctionality and stimuli-responsive properties, as well as associated toxicity concerns. The discussions presented herein aim to provide the readers a comprehensive understanding of the potential of nanogels as smart drug delivery systems in the context of cancer therapy.