Cresorol

Graptophyllum grandulosum (G. grandulosum) is a plant of the Acanthaceae family found in the Littoral region of Cameroon. This plant is traditionally used by the local population for its various medicinal properties. G. grandulosum contains multiple bioactive compounds such as chrysoeriol and luteolin. This study aimed to evaluate the preventive effect of the aqueous extract of G. grandulosum on nicotine-induced addiction. 42 Wistar pubescent adolescent male rats were used during this experiment. Nicotine addiction was induced following a 5 days injections of nicotine tartrate (0.4 mg/kg, sc). The behavioural assessment was done using the Conditioned Place Preference (CPP) test and the Elevated plus maze (EPM) test. 24 h following the last nicotine administration, animals were evaluated for preference change in the CPP and 1 h following this test, animals were submitted to the EMP. The animals were sacrificed; the hippocampus and striatum were collected for biochemicals assays (dopamine, acetylcholine, Brain-Derived Neurotrophic Factor (BDNF) and proinflammatory cytokines). The acute toxicity of G. grandulosum was also performed. G. grandulosum prevented CPP preference change (p < 0.001) induced by nicotine injection and reduced hyperactivity and risk taking (p < 0.001) in the EPM test. G. grandulosum reduced dopamine levels (p < 0.001) and increased acetylcholine levels (p < 0.01). Additionally, G. grandulosum modulated BDNF levels (p < 0.001) and reduced proinflammatory cytokines (Interleukine-1β (IL-1β) and Tumor necrosis factor (TNFα)) (p < 0.01). G. grandulosum did not present any sign of toxicity. These results suggest that G. grandulosum prevents addictive behavior via the modulation of dopaminergic, cholinergic, BDNF and neuroinflammatory pathways.

Traditionally, Callicarpa species have been utilized their anti‐inflammatory and hemostatic properties. Prominently featured species in the 2020 Edition of the Chinese Pharmacopoeia were Callicarpa nudiflora (CN), Callicarpa macrophylla (CM), Callicarpa formosana (CF), and Callicarpa kwangtungensis (CK), which were formulated into several medicinal preparations. Extensive applications led to the significant depletion of CN's wild resources. The management of germplasm resources was significantly disordered. Adulteration issues were also prevalent.

It is imperative that the study aims to identify alternative sources for CN and other pharmacopeial varieties and develop methods to distinguish different Callicarpa species.

Data were acquired using three mass spectrometry modes: Data Dependent Analysis (DDA), Data‐Independent Analysis (DIA), and full mass spectrometry (MS). The DDA mode identified or inferred information on 54 compounds. The Full MS mode identified or inferred 74 compounds, including 20 that were previously unreported in Callicarpa. These compounds were confirmed using standards. The DIA mode did not facilitate identification due to missing precursor ion data. With metabolomics, 19 differential compounds were identified or inferred. Luteolin, chrysoeriol, and quercetin were selected as potential markers, integrating the 10 active compounds from network pharmacology.

Based on the relative abundance of these markers, it was proposed that Callicarpa giraldii Hesse ex Rehd. var. (CGHRV) and CM could serve as alternative resource species to CN, while CGHRV and Callicarpa giraldii Hesse ex Rehd. (CGHR) could substitute the pharmacopeial CM. Callicarpa longissimi (CLG) was suggested as an alternative to CK, while Callicarpa cathayana (CC) and Callicarpa rubella (CRL) could replace CF. Furthermore, the absence of certain compounds in CK presented a novel opportunity for the differentiation of various Callicarpa species.