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The present study explored the changes in phytochemical profiles (proximate, amino acids, fatty acids, and lignans) and antioxidant activity of Schisandra sphenathera fruit with three maturity stages (un-ripen, semi-ripen and fully-ripen). The results showed that the whole fruit contained high levels of essential amino acids and unsaturated fatty acids (linoleic and oleic acids), whose content slightly reduced with maturity. Meanwhile, the contents of total phenolics, total flavonoids, and total tannins were generally decreased in the extractable, free, conjugated, and bound phenolic fractions, while the total anthocyanin content in these phenolic fractions were increased during ripening. Furthermore, the lignan profiling of these fractions indicated an increased content of schisandrol A and gomisin J, but a decreased content of schisandrin B and schisandrin C in the extractable phenolic fractions during fruit maturation. It was noted that schisantherin B and schisandrin A were recorded in all phenolic fractions, alongside schisandrin B and schisandrin C detected only in extractable form. Additionally, the extractable phenolic fractions exerted considerable antioxidant activity with little or low significance at three maturity stages. Therefore, the whole fruit of S. sphenathera abound with unsaturated fatty acids and antioxidant lignans, boosting its chances of being fully utilized as a versatile and economical crop in pharmaceutical and food industries for different purposes. • S. sphenathera fruit contained high levels of essential amino acids and unsaturated fatty acids. • Both extractable and non-extractable phenolics changed with ripening stages. • Lignan profiles of different phenolics fractions were also varied. • Schisantherin B and schisandrin A presented in free, conjugated and bound forms. [ABSTRACT FROM AUTHOR]