Wen Hou

Extracting natural active ingredients from plants is an effective way to develop and screen modern drugs. Psoralea corylifolia (PC) is a leguminous plant whose seeds have long been used as a Traditional Chinese Medicine to treat psoriasis, rheumatism, dermatitis, and other diseases. To date, several main compounds, including coumarins, flavonoids, monoterpene phenols, and benzofurans, have been identified from the seeds of PC. Among them, bavachinin is a type of flavonoid with various biological activities. In this article, the biological activities and mechanisms of action of bavachinin and its derivatives are reviewed. It includes the pharmacokinetic characteristics of bavachinin and its derivatives, as well as its prominent anti‐inflammatory, antitumor, antibacterial, and antiviral pharmacological activities and related metabolic studies. Bavachinin displayed these activities through different receptors, such as peroxisome proliferator‐activated receptors (PPARs), as well as multiple signaling pathways and enzyme systems. In summary, bavachinin and its derivatives have potential drug development value in many fields, such as anti‐inflammatory, antitumor, nervous system disease, and diabetes. We believe that this review will lay a foundation for bavachinin‐based drug development throughout the world.

Pigeon pea (Cajanus cajan (L.) Millsp.) is a traditional Chinese medicinal plant widely utilized in folk medicine due to its significant pharmacological and nutritional properties. Cajaninstilbene acid (CSA), a stilbene compound derived from pigeon pea leaves, has been extensively investigated since the 1980s. A thorough understanding of CSA’s mechanisms of action and its therapeutic effects on various diseases is crucial for developing novel therapeutic approaches. This paper presents an overview of recent research advancements concerning the biological activities and mechanisms of CSA and its derivatives up to February 2024. The review encompasses discussions on the in vivo metabolism of CSA and its derivatives, including antipathogenic micro-organisms activity, anti-tumor activity, systematic and organ protection activity (such as bone protection, cardiovascular protection, neuroprotection), anti-inflammatory activity, antioxidant activity, immune regulation as well as action mechanism of CSA and its derivatives. The most studied activities are antipathogenic micro-organisms activities. Additionally, the structure–activity relationships of CSA and its derivatives as well as the total synthesis of CSA are explored, highlighting the potential for developing new pharmaceutical agents. This review aims to provide a foundation for future clinical applications of CSA and its derivatives.

Sinomenine, an isoquinoline alkaloid extracted from the roots and stems of Sinomenium acutum, has been extensively studied for its derivatives as bioactive agents. This review concentrates on the research advancements in the biological activities and action mechanisms of sinomenine-related compounds until November 2023. The findings indicate a broad spectrum of pharmacological effects, including antitumor, anti-inflammation, neuroprotection, and immunosuppressive properties. These compounds are notably effective against breast, lung, liver, and prostate cancers, exhibiting IC₅₀ values of approximately 121.4 nM against PC-3 and DU-145 cells, primarily through the PI3K/Akt/mTOR, NF-κB, MAPK, and JAK/STAT signaling pathways. Additionally, they manifest anti-inflammatory and analgesic effects predominantly via the NF-κB, MAPK, and Nrf2 signaling pathways. Utilized in treating rheumatic arthritis, these alkaloids also play a significant role in cardiovascular and cerebrovascular protection, as well as organ protection through the NF-κB, Nrf2, MAPK, and PI3K/Akt/mTOR signaling pathways. This review concludes with perspectives and insights on this topic, highlighting the potential of sinomenine-related compounds in clinical applications and the development of medications derived from natural products.

Cancer with low survival rates is the second main cause of death among all diseases in the world and consequently, effective antineoplastic agents are urgently needed. Allosecurinine is a plant-derived indolicidine securinega alkaloid shown bioactivity. The object of this study is to investigate synthetic allosecurinine derivatives with considerable anticancer capacity against nine human cancer cell lines as well as mechanism of action. We synthesized twenty-three novel allosecurinine derivatives and evaluated their antitumor activity against nine cancer cell lines for 72 h by MTT and CCK8 assay. FCM were applied to analyze the apoptosis, mitochondrial membrane potential, DNA content, CD11b expression. Western blot was selected to analyze the protein expression. Structure-activity relationships were established and potential anticancer lead BA-3 which induces differentiation of leukemia cells towards granulocytosis at low concentration and apoptosis at high concentration were identified. Mechanism studies showed that mitochondrial pathway mediated apoptosis within cancer cells with cell cycle blocking is induced by BA-3. In addition, western blot assays revealed that BA-3 induces expression of the proapoptotic factor Bax, p21 and reduces the levels of antiapoptotic protein such as Bcl-2, XIAP, YAP1, PARP, STAT3, p-STAT3, and c-Myc. Collectively, BA-3 is a lead compound for oncotherapy at least in part, through the STAT3 pathway. These results are an important step in further studies on allosecurinine-based antitumor agent development.