Current Bioactive Compounds - Volume 22, Issue 1, 2026

Globally large numbers of people are suffering from brain disorders for instance neurodegenerative disorders whereas treatments remain inadequate. The blood-brain barrier (BBB) serves as a major obstacle in transporting active therapeutic agents into the brain. Herbal medicines have the potency to treat these brain diseases however, it is having some limitations like poor brain permeability, and slow bioavailability.

The objective of this study was to assess the neuroprotective effects of andrographolide-loaded β-cyclodextrin-lactose nanoparticles on spatial learning and memory in experimental models, aiming to enhance cognitive function and brain health.

Swiss Albino mice (25-30 g, 2-3 weeks, both sexes) were sourced from Galgotias University, India (Reg. No. 94090). Andrographolide (AGL), a diterpenoid from Andrographis paniculata, was encapsulated in β-cyclodextrin (β-CD) combined with lactose using the solvent evaporation method, optimized via Design-Expert software. To improve neuronal uptake, lactose was added to β-CD using the heating method, confirmed by 1H NMR spectra. The AGL-loaded β-CD-lactose nanoparticles were characterized for particle size, zeta potential, and entrapment efficiency, and their effects on brain tissue were assessed biochemically and histopathologically.

Developed nanoparticles had particle size 247.9 ± 3.2 nm, PDI 0.5 ± 0.02, and zeta potential 26.8 ± 2.5 mV, while entrapment efficacy between 74 ± 0.45% to 82 ± 0.32% and in-vitro drug release from the nanoparticles had 79.48 ± 0.74% in 24 hours. TEM analysis showed spherical morphology. Furthermore, behavioural assay and acute toxicity of nanoparticles were also analyzed which indicate that nanoparticles can reach into the brain and are safe for further use.

The lactose-modified β-cyclodextrin nanoparticles significantly improved the neuroprotective effect of AGL, offering an effective strategy for drug delivery to the brain and potential treatment for neurodegenerative disorders.

Alkaloids are naturally occurring nitrogen-containing chemicals in plants, fungi, and mammals. These chemicals protect plants from herbivores and pathogens and have a wide range of biological actions, making them useful in pharmacology and medicine. Alkaloids offer potent therapeutic effects, including antifungal, local anaesthetic, anti-inflammatory, antineoplastic, pain-killing, neuropharmacological, and antibacterial properties. Morphine is commonly used to relieve pain, quinine for malaria, and vincristine for cancer. Because of their considerable therapeutic potential, alkaloids have become a focus of study in the development of medications to treat infections, inflammation, neurological diseases, and cancer.

The primary goal of this research is to isolate, purify, and validate amide alkaloids from the seeds of Piper guineense, a West African species while contrasting traditional alkaloid extraction methods with novel techniques such as molecular distillation, membrane separation, molecular imprinting, and high-speed counter-current chromatography. The study aims to address the challenges posed by conventional methods' high cost and low yield, by providing insights into more efficient, scalable, and advanced technologies for alkaloid extraction and purification, which are critical for the advancement of complementary and Chinese medicine.

The seeds of Piper guineense were extracted using a Soxhlet device with methanol as the solvent. The extracted extract was purified and separated into amide alkaloids using column chromatography. Thin-layer chromatography (TLC) was used to confirm the presence of alkaloids. The isolated compounds were examined and characterized using an array of spectrum methods, including Mass spectra, FTIR, and NMR spectroscopy. Natural substances with nitrogen in the exocyclic outlook, such as mescaline, serotonin, and dopamine, were recognized as amines rather than alkaloids in the investigation.

The synthesized chemicals, including Piperine, Wisanine, Piperlonguminine, Propiverine, and Piperidine, were satisfactorily characterized using FTIR, NMR, mass spectrometry, and HPLC. The FTIR spectra showed distinct peaks which were consistent with conventional standards, demonstrating the effective synthesis. NMR research, performed with a BRUKER AVANCE NEO-500 MHz spectrometer, revealed information on the chemical surroundings of the protons, confirming the molecular structure. Mass spectroscopy was done using a MICROMASS Q-TOF micro-mass spectrometer to precisely measure molecular weights and identify fragmentation patterns, verifying the existence of important functional groups and assuring the structural integrity of the compounds.

This work effectively extracted, purified, and characterized numerous amide alkaloids from Piper guineense seeds using modern chromatographic and spectroscopic methods. The compounds, which included Piperine, Wisanine, Piperlonguminine, Propiverine, and Piperidine, were validated using FTIR, NMR, mass spectroscopy, and HPLC to ensure structural integrity and composition. The study reveals the efficacy of contemporary extraction and analytical procedures, offering useful insights into how to improve alkaloid purification processes. These discoveries advance our understanding of alkaloid chemistry and have the potential for future uses in alternative medicine and pharmaceutical research.

Marine sponges and sponge-associated fungi are rich sources of bioactive compounds with pharmacological potential. However, the secondary metabolites of Vietnamese marine sponge-derived fungi have been poorly studied.

The aim of this study was to investigate the low-molecular-weight compounds in the extract of Penicillium sp. 1901NT-2.53.1 fungus isolated from the Vietnamese marine sponge Cinachyrella sp., and the antiproliferative activity of the isolated compounds.

The structures of isolated compounds were elucidated using spectroscopic methods. The cell viability effects of the compounds were evaluated using MTT assay. Molecular docking was performed using SwissDock.

UPLC-MS data suggested the presence of beauvericin, citreorosein, benzopyran and chlorotetracycline derivatives, 2-chloro-1,3,8-trihydroxy-6-(hydroxymethyl)anthracene-9,10-dione and ergosterol peroxide in the fungal extract. Chromatographic separation of the extract resulted in the isolation of three derivatives of mycophenolic acid (MPA), namely penicacids G and K and 4-hydroxy-MPA. Penicacid K was isolated from a natural source for the first time. Penicacid G inhibited the viability of human normal HaCaT keratinocytes with IC50 of 88.3 μM and 72.9 μM for 24 h and 48 h of treatment, respectively. Moreover, penicacid G arrested the proliferation of HaCaT keratinocytes. Both penicacids K and G can interact with the active site of IMPDH2, similar to other derivatives of MPA; however, the differences in their structures are important.

Due to the selective action on cancer cells and good druggability, penicacid G may be interesting as an antiproliferative anticancer compound.

Nowadays, medicinal herbs and their phytochemicals have emerged as a great therapeutic option for many disorders. However, poor bioavailability and selectivity might limit their clinical application. Among all approaches, phyto-phospholipid complexes (named phytosomes) have appeared to be a great method to overcome the problems. With the new developments in drug delivery technologies, anticancer drugs ranging from hydrophilic macromolecules to lipophilic drugs can be administered via phytosomes to treat cancer.

In the present review, various drugs targeted by phytosomes to treat varied forms of cancer, like breast cancer, pancreatic cancer, lung cancer, colon cancer, prostate cancer, etc, are discussed.

In this review, recent literature covering phytosomes to treat various forms of cancer, patent applications, and clinical trials involving phytosomes employed to cure mainly cancer are covered.

Phytosomes have proved their potential to cure cancer. They increase the bioavailability of the drug by site-specific drug delivery and can reduce the side effects/toxicity associated with anticancer drugs and also sustain the release of drugs.

The potential of phytosomes to carry the drug may unclutter novel ways for therapeutic intercessions in various tumors.

In recent years, chemical and biological studies have explored medicinal plants to develop new treatments for oxidative stress, inflammation, and diabetes.

This study aims to characterize for the first time the chemical composition of the hexane extract from the roots of Salvia argentea using GC and GC/MS techniques. We also isolated its major compound and evaluated its biological activities, including its antioxidant, anti-inflammatory, antidiabetic, and hemolytic effects, as well as the combination of this major compound with reference drugs.

Antioxidant activity was assessed using DPPH, β-carotene, and phosphomolybdenic tests. The anti-inflammatory effect was measured by the egg albumin denaturation method and protein denaturation inhibition. The antidiabetic activity was determined by evaluating the inhibition of α-amylase, with acarbose as a positive reference. The combined effect of aethiopinone with standards was also studied to reduce the minimum effective dose and minimize side effects.

The hexane extract of Salvia argentea is mainly composed of aethiopinone (53.3%) and ferruginol (20.5%). aethiopinone was isolated and identified using spectroscopic methods, including ¹H NMR, ¹³C NMR, and IR. The biological activity assessment showed that hexane extract and aethiopinone had promising antioxidant, anti-inflammatory, and antidiabetic properties. In addition, synergistic effects were observed when aethiopinone was combined with positive references, resulting in a significant reduction of the required minimum inhibitory concentrations. The human erythrocyte toxicity assessment showed that hexane extract and aethiopinone induced very low hemolysis levels, reaching 24.18% and 31.13%, respectively, at high concentrations of 2000 μg/mL.

Further research is needed to confirm their therapeutic effects and assess their potential for use in the pharmaceutical industry.

The use of plant extracts in the biosynthesis of nanoparticles has garnered attention in recent years due to the rapid, ecological, and economical production protocol. The current study aimed to biosynthesize silver nanoparticles (AgNPs) of Hypochaeris radicata L. extract.

These nanoparticles were characterized by UV-Vis, Fourier Transform Infrared Spectroscopy (FTIR), and X-Ray Diffraction (XRD) to determine their size and composition. The bioactivity was assessed by the determination of their antimicrobial effect using the well diffusion method and their cytotoxicity by hemolysis method.

The results showed that AgNPs have been successfully synthesized and exhibit a surface plasmon resonance spectrum with an absorption maximum at 420 nm. FTIR affirmed the role of H. radicata L. as a reducing and capping agent of silver ions and XRD revealed their crystalline nature. Interestingly, the synthesized AgNPs exhibited significant antimicrobial effects particularly against Escherichia coli and Aspergillus niger with inhibition zones of 20.5 and 19 mm, respectively. The cytotoxicity test confirmed the non-toxic characteristics of the synthesized AgNPs.

The bio-ingredients present in the plant extract were effective for the synthesis of Ag nanoparticles with significant biological efficacy.

Ochna integerrima (Lour.) Merr., commonly known as “Mai Vàng,” is a flowering plant native to Southeast Asia. The plant contains various flavonoids, contributing to its medicinal properties, including antioxidant and anti-inflammatory effects. However, the understanding of its chemical components is limited. This study aimed to isolate compounds from ethyl acetate (EtOAc) extract and evaluated their NO inhibitory activities.

The structures of isolates were clarified using nuclear magnetic resonance (NMR) and high-resolution electrospray ionization mass spectrometry (HR-ESI-MS) analyses, and they were compared with previously published spectral data. The Griess assay was performed to evaluate the anti-inflammatory activity of isolated compounds in LPS-stimulated RAW 264.7 cells.

Six compounds (1-6) were obtained from the EtOAc extract, including 2,4-dihydroxyphenylacetate (1), (+)-catechin (2), luteolin (3), apigenin (4), vitexin (5), and cynaroside (6). Among them, compounds 1 and 2 exhibited significant NO inhibitory activity against LPS-stimulated RAW 264.7 cells without any cytotoxicity. Compounds 1, 4, and 6 were first reported from this species.

This species holds promise as a potential candidate for its anti-inflammatory effects.