Search Results (6)

Background: Higenamine, a bioactive alkaloid derived from plants such as Aconitum and Annona squamosa, has been traditionally used in Chinese medicine for treating heart diseases like bradycardia, arrhythmia, and heart failure. It exhibits multiple pharmacological effects, including anti-oxidative stress, improved cellular energy metabolism, anti-apoptosis, and enhanced erectile dysfunction. Aim and Methods: To investigate the reasons for these functions of higenamine and its application in the clinic, the literature of the database was searched and read in this study. Results: As a non-selective β-agonist, higenamine activates both β₁- and β₂-adrenergic receptors, leading to cardiovascular benefits such as increased heart rate and myocardial contractility, as well as bronchodilation. It has also been studied for its potential in weight loss, anti-inflammatory properties, and antioxidant properties, with applications in treating asthma, cardiovascular diseases, and ischemia-reperfusion injuries. However, its clinical use is limited by the need for further research on its long-term safety, pharmacokinetics, and interactions with other drugs. Despite its promising therapeutic potential, higenamine’s inclusion in the World Anti-Doping Agency’s banned list highlights concerns over its stimulant effects and safety in athletic contexts. Conclusions: Future studies should focus on optimizing its clinical applications while ensuring safety and efficacy. In terms of clinical applications, future research will also be able to explore more possibilities to use higenamine more in the treatment of diseases. Full article

Background and objectives: Higenamine is an alkaloid found in different plant species like Aconitum japonica, Nandina domestica, Gnetum parvifolium, and Asarum heterotropoides. According to the available data in the literature, its dietary intake leads to an enhancement of lipolysis. The objective of this study was to explore whether the ingestion of a one-component higenamine supplement (75 mg/day) for three weeks would introduce some changes in the fatty acid (FA) profiles of serum phospholipids of female recreational athletes. Methods: A total of 12 female recreational athletes were included in a double-blind study, with six participants in both groups—a higenamine treatment group and placebo group. Serum phospholipids were isolated via one-dimensional thin-layer chromatography. Fatty acid methyl ester samples from the phospholipids were analyzed by a gas–liquid chromatography method. Desaturase and elongase activities were calculated from product/precursor FA ratios. Results: In the group that was undergoing higenamine treatment, a statistically significant increase in the levels of linolenic acid, a total n − 6 polyunsaturated FAs (PUFAs), and an n − 6/n − 3 FA ratio were observed. But saturated palmitic acid and monounsaturated palmitoleic and oleic acid, as well as consequent total saturated FAs and monounsaturated FA acids decreased in serum phospholipids. Also, after 3 weeks of higenamine supplementation, arachidonic n − 6 acid and docosapentaenoic n − 3 acids levels were significantly decreased, and estimated delta-5 desaturase activity (arachidonic/dihomo-gamma-linolenic acid ratio) was decreased too. In the placebo group, a significant change was increased levels of oleic acid compared to baseline levels. Conclusion: According to the results obtained for the FA status of serum phospholipids, treatment with higenamine was followed by a modulation of serum phospholipid FA profiles. Furthermore, this could influence the desaturation/elongation metabolic pathway of endogenous FA metabolisms, leading to a decrease in delta-5 desaturase activity and consequently lower levels of long-chain PUFAs. For further discussion, it is necessary to assess the dietary intake of study participants. Full article

Environmental pollutants such as fine dust are increasingly linked to premature skin aging. In this study, we investigated the protective effects of higenamine, a natural plant alkaloid, against fine-dust-induced skin aging in human keratinocytes (HaCaT cells). We found that higenamine significantly attenuated fine-dust-induced expression of matrix metalloproteinase-1 (MMP-1), a key enzyme involved in collagen degradation. Furthermore, higenamine was found to modulate fine-dust-induced AP-1 and NF-κB transactivation, which are crucial factors for MMP-1 transcription. Higenamine also impeded fine-dust-induced phosphorylation in specific pathways related to AP-1 and NF-κB activation, and effectively alleviated reactive oxygen species (ROS) production, a key factor in oxidative stress caused by fine dust exposure. These results suggest that higenamine exerts protective effects against fine-dust-induced skin aging, primarily through its MMP-1 inhibitory properties and ability to mitigate ROS-induced oxidative damage. Our data highlight the potential of higenamine as an effective ingredient in skincare products designed to combat environmental skin damage. Full article

Current anti-doping policy seeks to protect honest athletes from biochemically overeducated colleagues. However, there is a question of whether the present policy has gone too far. This article illustrates the ambiguity of the anti-doping policy in the context of a particular plant-based substance (i.e., higenamine) by providing certain case studies. In such cases, the process of proof requires the continuous checking of suppositions since an athlete must establish how the prohibited substance could have entered his or her body. This obligation implies that an athlete and the defending team must have legal, medical, dietary, and biochemical knowledge. However, even with all precautions, it is still possible to fail an anti-doping test and be severely punished because it is almost impossible to trace all the sources that caused the prohibited substance to enter the athlete’s body. Full article

Background: Higenamine is a β₂ agonist of plant origin. The compound has been included in WADA’s prohibited list since 2017. Higenamine may be detected in different plants and many food supplements of natural origin. Methods: Our literature search was conducted through PubMed, Science Direct, Google Scholar, and Web of Science studies investigating the presence of higenamine in plants that are used in traditional folk medicine or included in food supplements. Our study aimed to assess the risk of adverse analytical findings caused by higenamine-containing plants. Results: Based on our literature search, Nelumbo nucifera, Tinospora crispa, Nandina domestica, Gnetum parvifolium, Asarum siebodii,Asarum heterotropoides, Aconitum carmichaelii, and Aristolochia brasiliensis are higenamine-containing plants. Based on data from Eastern folk medicine, these plants can provide numerous health benefits. Professional athletes likely ingest these plants without knowing that they contain higenamine; these herbs are used in treatments for different conditions and various foods/food supplements in addition to folk medicine. Conclusion: Athletes and their teams must be aware of the issues associated with the use of plant-based products. They should avoid consuming higenamine-containing plants during and outside of competition periods. Full article

Higenamine is a tetrahydroisoquinoline present in several plants that has β-adrenergic receptor agonist activity. Study of the biosynthesis of higenamine has shown the participation of norcoclaurine synthase, which controls the stereochemistry to construct the (S)-isomer. However, when isolated from nature, higenamine is found as the racemate, or even the (R)-isomer. We recently reported the isolation of higenamine 4′-O-β-d-glucoside. Herein, its (R)- and (S)-isomers were synthesized and compared to precisely determine the stereochemistry of the isolate. Owing to their similar spectral properties, determination of the stereochemistry based on NMR data was considered inappropriate. Therefore, a high-performance liquid chromatography method was established to separate the isomers, and natural higenamine 4′-O-β-d-glucoside was determined to be a mixture of isomers. Full article