Moringa oleifera Lam. (M. oleifera), which belongs to the Moringaceae family, is a perennial deciduous tropical tree, and native to the south of the Himalayan Mountains in northern India. M. oleifera is rich in proteins, vitamin A, minerals, essential amino acids, antioxidants, and flavonoids, as well as isothiocyanates. The extracts from M. oleifera exhibit multiple nutraceutical or pharmacological functions including anti-inflammatory, antioxidant, anti-cancer, hepatoprotective, neuroprotective, hypoglycemic, and blood lipid-reducing functions. The beneficial functions of M. oleifera are strongly associated with its phytochemicals such as flavonoids or isothiocyanates with bioactivity. In this review, we summarize the research progress related to the bioactivity and pharmacological mechanisms of M. oleifera in the prevention and treatment of a series of chronic diseases—including inflammatory diseases, neuro-dysfunctional diseases, diabetes, and cancers—which will provide a reference for its potential application in the prevention and treatment of chronic diseases or health promotion.

Isothiocyanates are biologically active products resulting from the hydrolysis of glucosinolates predominantly present in cruciferous vegetables belonging to the Brassicaceae family. Numerous studies have demonstrated the diverse bioactivities of various isothiocyanates, encompassing anticarcinogenic, anti-inflammatory, and antioxidative properties. Nature harbors distinct isothiocyanate precursors, glucosinolates such as glucoraphanin and gluconastrin, each characterized by unique structures, physical properties, and pharmacological potentials. This comprehensive review aims to consolidate the current understanding of Moringa isothiocyanates, mainly 4-[(α-L-rhamnosyloxy) benzyl] isothiocyanate), comparing this compound with other well-studied isothiocyanates such as sulforaphane and phenyl ethyl isothiocyanates. The focus is directed toward elucidating differences and similarities in the efficacy of these compounds as agents with anticancer, anti-inflammatory, and antioxidative properties.

Natural flavonoids display diverse therapeutic capabilities, including potent antioxidant, anti-inflammatory, neuroprotective, and anticancer properties. However, poor aqueous solubility, rapid metabolic clearance, and low oral bioavailability severely constrain their translational success. This review critically evaluates recent synthetic strategies designed to overcome these pharmacokinetic bottlenecks through targeted chemical derivatization of flavonoid scaffolds. We focus on regioselective modifications—specifically acetamidation, phosphorylation, amidation, sulfonation/sulfamylation and systematically evaluate their impacts on structure–activity relationships (SAR), physicochemical stability, and biological performance. Acetamide functionalization strengthens target affinity within kinase ATP-binding pockets and prolongs metabolic half-life by shielding vulnerable phenolic sites. Phosphorylated derivatives serve as highly soluble (>100-fold increase in water solubility), bioreversible prodrugs that undergo targeted enzymatic cleavage in tissues, while sulfonated and sulfamate analogs preserve core radical-scavenging capabilities while resisting autoxidation in physiological media. Furthermore, amino acid modification of flavonoids via semi-synthetic conjugates, such as quercetin para-aminobenzoic acid (Q-PABA), demonstrates synergistic dual-action photoprotection and enhanced pro-apoptotic anticancer activity. By integrating chemical, structural, and pharmacological perspectives, this review establishes a mechanistic framework for rational flavonoid design, paving the way for next-generation natural product-derived therapeutics with optimized bioavailability and clinical efficacy.