scholarly journals Recent Advances in the Anti-Inflammatory Activity of Plant-Derived Alkaloid Rhynchophylline in Neurological and Cardiovascular Diseases

Pharmaceutics ◽  
2021 ◽  
Vol 13 (8) ◽  
pp. 1170
Author(s):  
Rajeswari Gopal Geetha ◽  
Surya Ramachandran

Rhynchophylline (Rhy) is a plant-derived indole alkaloid isolated from Uncaria species. Both the plant and the alkaloid possess numerous protective properties such as anti-inflammatory, neuroprotective, anti-hypertensive, anti-rhythmic, and sedative effects. Several studies support the significance of the anti-inflammatory activity of the plant as an underlying mechanism for most of the pharmacological activities of the alkaloid. Rhy is effective in protecting both the central nervous system and cardiovascular system. Cerebro-cardiovascular disease primarily occurs due to changes in lifestyle habits. Many previous studies have highlighted the significance of Rhy in modulating calcium channels and potassium channels, thereby protecting the brain from neurodegenerative diseases and related effects. Rhy also has anticoagulation and anti-platelet aggregation activity. Although Rhy has displayed its role in protecting the cardiovascular system, very little is explored about its intervention in early atherosclerosis. Extensive studies are required to understand the cardioprotective effects of Rhye. This review summarized and discussed the various pharmacological effects of Rhy in neuro- and cardioprotection and in particular the relevance of Rhy in preventing early atherosclerosis using Rhy-loaded nanoparticles.

Molecules ◽  
2018 ◽  
Vol 23 (11) ◽  
pp. 2912 ◽  
Author(s):  
Ping Zhou ◽  
Weijie Xie ◽  
Yun Luo ◽  
Shan Lu ◽  
Ziru Dai ◽  
...  

Inflammation is a major contributing factor to the progression of atherosclerosis. Ginsenoside Rb1 (Rb1), an active saponin of Panax notoginseng, has been found to exert beneficial effects on inflammation and oxidative stress. This study investigated the ability of Rb1 to inhibit the formation of atherosclerotic plaques and the potential mechanisms. In this study, the effects of Rb1 on the development of atherosclerosis were investigated in ApoE-/- deficient mice fed with a western diet. Mice were intragastrically administrated with Rb1 (10 mg/kg) for 8 weeks. This study is that ginsenoside Rb1 exerted an inhibitory effect on early atherosclerosis in ApoE-/- mice via decreasing body weight and food intake daily, upregulating the lipid levels of serum plasma, including those of TC, TG and LDL-C and HDL-C and reducing the atherosclerotic plaque area, suppressing inflammatory cytokines (levels of IL-1β, IL-6 and TNF-α) in the serum of ApoE-/- mice, changing the expression levels of BCL-2, BAX, cleaved caspase-3 and cleaved caspase-9 and weakening apoptosis associated with anti-inflammatory activity. Hence, all these effects against atherosclerosis were tightly associated with regulation of necrosis or apoptosis associated with anti-inflammatory activity. Additionally, the results found that ginsenoside Rb1 increased autophagy flux to inhibit apoptosis via acceleration of autophagy by promoting transformation of LC3 from type I to type II in high-fat diet-induced atherosclerosis in ApoE-/- mice. This finding, along with those of the previous study, provides evidence that Rb1 promotes the process of autophagy to protect against atherosclerosis via regulating BCL-2 family-related apoptosis. These results indicate that Rb1 exhibits therapeutic effects in atherosclerosis by reversing the imbalance between apoptosis and autophagy.


2009 ◽  
Vol 64 (5-6) ◽  
pp. 335-338 ◽  
Author(s):  
Irene M. Villaseñor ◽  
Arlyn C. Sanchez

Cassiaindoline is a new dimeric indole alkaloid isolated from Cassia alata L. leaves whose structure was elucidated through spectroscopic analyses. It exhibited analgesic activity at a dosage of 125.0 mg/kg mouse and decreased the number of writhings induced by acetic acid by 49.4%. It also showed a 57.1% anti-inflammatory activity at a dosage of 75 mg/kg mouse


1927 ◽  
Vol 23 (4) ◽  
pp. 464-464
Author(s):  
V. I. Znamensky

According to V. I. Znamensky indicated for treatment in Matsesta: 1) diseases of the peripheral nervous system, -neuralgia, neuritis; 2) diseases of the central nervous system connected with disorders of the cardiovascular system, - hemiplegia and hemiparesis due to thrombosis and embolism; (treatment of acute forms of the mentioned diseases, it goes without saying, is contraindicated); 3) Luetic diseases,-vascular syphilis of the brain, lues cerebrospinalis, meningo-myelitis, tabes dorsalis incipiens and Luetic radiculitis (here; baths, giving increase of metabolism and excretions, make possible mercury treatment with impunity); 4) remnants of lethargic encephalitis.


Planta Medica ◽  
2017 ◽  
Vol 84 (01) ◽  
pp. 20-25 ◽  
Author(s):  
Xinyao Yang ◽  
Xiaoli Gao ◽  
Yuan Cao ◽  
Qiang Guo ◽  
Shanshan Li ◽  
...  

AbstractThe anti-inflammatory effects of boldine and reticuline isolated from Litsea cubeba were evaluated by using xylene-induced ear edema and carrageenan-induced paw edema in mice and rats. Our results demonstrated that intragastric administration with boldine and reticuline significantly mitigated ear weight in mice and decreased paw volume in rats. A combination administration of boldine (0.5 mg/kg) + reticuline (0.25 mg/kg) resulted in a potentiated inhibition in these two models. In parallel, boldine or reticuline reduce the infiltration of neutrophil leukocytes in rat paw tissue, respectively, and the combination of the two groups performed a better anti-inflammatory activity as shown in histopathologies. Boldine, reticuline, and their combination notably inhibited mRNA expressions of TNF-α, and IL-6 and reduced the phosphorylation levels of Janus kinase 2 (JAK2) and signal transducer and activator of transcription 3 (STAT3). Beyond that, their combination also can reduce the phosphorylation levels of p65 and IκBα in the pathological tissues of animals, as observed by real-time PCR and western blot analyses, respectively. These findings indicate for the first time that boldine and reticuline have not only anti-inflammatory activity but also potential synergistic effects in vivo. The underlying mechanism may relate to the inhibition on the expression of pro-inflammatory cytokines, such as TNF-α and IL-6, which may be a consequence of JAK2/STAT3 and NF-κB pathway involvements. This study provides useful data for further exploration and application of boldine and reticuline as potential anti-inflammatory medicines.


2021 ◽  
Vol 66 (2) ◽  
pp. 29-35
Author(s):  
F. Torubarov ◽  
Z Zvereva ◽  
S. Luk'yanova

Purpose: The aim is to study the bioelectric activity of the brain in the operational workers of the Novovoronezh and Beloyarsk nuclear power plants with a low level of psychophysiological adaptation. Material and methods: An EEG study of 101 operational employees of the NPP was conducted, visual and spectral analyses were used. EEG indicators of individuals with a low level of psychophysiological adaptation and low functional activity of structural and functional formations of the central nervous system were compared with those of individuals with a high level of adaptation, high functional activity of structural and functional formations of the central nervous system. Results: Visual analysis of individuals with a low level of psychophysiological adaptation revealed abnormal EEG indicators, indicating functional disorders of the central nervous system. The greatest violations were revealed in the structural and functional formation responsible for the central regulation of the cardiovascular system. A comparative assessment of the spectral power of the EEG at different levels of psychophysiological adaptation revealed a state of tension (tense adaptation) observed in individuals with both low and high levels of adaptation. The similarity between the structural and functional formation "central regulation of the cardiovascular system" with low functional activity and a low level of psychophysiological adaptation in terms of the number of abnormal EEG indicators can be considered as evidence of its greatest contribution to the formation of a low level of adaptation.The evaluation of interhemispheric interactions in structural and functional formations at their low and high activity, as well as at low and high levels of adaptation, suggested that the formation of a high level of psychophysiological adaptation as an integral characteristic of the main role played by the formation of the "Cortex" and "central regulation of the cardiovascular system". In the formation of a low level of psychophysiological adaptation as an integral characteristic, the main role is played by the formations "cortex" and "cortical-subcortical interaction". Conclusion: A violation of the bioelectric activity of the brain may be one of the pathogenetic mechanisms of reduced adaptation. The presence of statistically significant differences in EEG indicators in individuals with low and high levels of adaptation, revealed by visual and spectral analysis, allows us to consider these indicators as informative not only in terms of identifying deviations in the diagnosis of functional disorders, but also in assessing the effectiveness of rehabilitation and health measures.


2020 ◽  
Vol 20 (9) ◽  
pp. 1391-1411 ◽  
Author(s):  
Thea Magrone ◽  
Manrico Magrone ◽  
Matteo A. Russo ◽  
Emilio Jirillo

Background & Objectives: In old people, both innate and adaptive immune responses are impaired, thus leading to a condition of systemic inflamm-ageing, even including the involvement of the central nervous system (CNS). Aims: Here, main mechanisms of the immune ageing and neuro-inflammation will be discussed along with the dietary approaches for the modulation of age related diseases. Discussion: Neuroinflammation is caused by the passage of inflammatory mediators through the brain blood barrier to CNS. Then, in the brain, antigenic stimulation of microglia and/or its activation by peripheral cytokines lead to a robust production of free radicals with another wave of proinflammatory cytokines which, in turn, causes massive neuronal damage. Also, infiltrating T cells [T helper (h) and T cytotoxic cells] contribute to neuronal damage. Additionally, a peripheral imbalance between inflammatory Th17 cells and anti-inflammatory T regulatory cells seems to be prevalent in the aged brain, thus leading to a proinflammatory profile. Alzheimer’s disease, Parkinson’s disease and multiple sclerosis will be described as typical neurodegenerative diseases. Finally, modulation of the immune response thanks to the anti-oxidant and anti-inflammatory effects exerted by dietary products and nutraceuticals in ageing will be discussed. Special emphasis will be placed on polyunsaturated fatty acids, polyphenols, micronutrients and pre-probiotics and synbiotics. Conclusion: Ageing is characterized by an imbalance subversion of the immune system with a condition of inflamm-ageing. Neuroinflammation and neurodegenerative diseases seem to be a central manifestation of a peripheral perturbation of the immune machinery. Dietary products and nutraceuticals may lead to a down-regulation of the oxidative and pro-inflammatory profile in ageing.


2003 ◽  
pp. 377-392 ◽  
Author(s):  
HJ Schneider ◽  
U Pagotto ◽  
GK Stalla

The somatotropic axis interacts with the central nervous system (CNS) on several levels. Growth hormone (GH) and insulin-like growth factor-I (IGF-I) receptors are expressed in many brain areas including the hippocampus, pituitary and hypothalamus. GH and IGF-I can pass the blood-brain barrier by an as yet not completely understood mechanism. They can also be produced in the brain and thus act via paracrine/autocrine mechanisms. GH and IGF-I are important factors in the development and differentiation of the CNS and have protective properties in dementia, and in traumatic and ischemic injury of the CNS. An improvement in cognitive functioning in GH-deficient patients by GH substitution has been shown. Significant results could, however, only be achieved with supraphysiological doses. In some studies, a correlation between IGF-I and cognitive function in the elderly has been found. GH has an important impact on mood and well-being with GH secretory capacity being reduced in depression. Pulsatile GH secretion is closely related to slow wave sleep (SWS) with SWS being stimulated by GH releasing hormone and rapid eye movement (REM) sleep by GH.


2021 ◽  
Vol 22 (12) ◽  
pp. 6238
Author(s):  
Anna Kiełbasa ◽  
Renata Gadzała-Kopciuch ◽  
Bogusław Buszewski

Cytokines play a huge role in many biological processes. Their production, release and interactions are subject to a very complex mechanism. Cytokines are produced by all types of cells, they function very differently and they are characterized by synergism in action, antagonism, and aggregation activity, opposing action of one cytokine, overlapping activity, induction of another cytokine, inhibition of cytokine synthesis at the mRNA level as well as autoregulation-stimulation or inhibition of own production. The predominance of pro-inflammatory cytokines leads to a systemic inflammatory response, and anti-inflammatory-to an anti-inflammatory response. They regulate the organism’s immune response and protect it against sudden disturbances in homeostasis. The synthesis and activity of cytokines are influenced by the central nervous system through the endocrine system (pituitary gland, adrenal glands).


Molecules ◽  
2021 ◽  
Vol 26 (21) ◽  
pp. 6630
Author(s):  
Daria D. Vaulina ◽  
Kira I. Stosman ◽  
Konstantin V. Sivak ◽  
Andrey G. Aleksandrov ◽  
Nikolai B. Viktorov ◽  
...  

Neolignans honokiol and 4′-O-methylhonokiol (MH) and their derivatives have pronounced anti-inflammatory activity, as evidenced by numerous pharmacological studies. Literature data suggested that cyclooxygenase type 2 (COX-2) may be a target for these compounds in vitro and in vivo. Recent studies of [11C]MPbP (4′-[11С]methoxy-5-propyl-1,1′-biphenyl-2-ol) biodistribution in LPS (lipopolysaccharide)-treated rats have confirmed the high potential of MH derivatives for imaging neuroinflammation. Here, we report the synthesis of four structural analogs of honokiol, of which 4′-(2-fluoroethoxy)-2-hydroxy-5-propyl-1, 1′-biphenyl (F-IV) was selected for labeling with fluorine-18 (T1/2 = 109.8 min) due to its high anti-inflammatory activity confirmed by enzyme immunoassays (EIA) and neuromorphological studies. The high inhibitory potency of F-IV to COX-2 and its moderate lipophilicity and chemical stability are favorable factors for the preliminary evaluation of the radioligand [18F]F-IV in a rodent model of neuroinflammation. [18F]F-IV was prepared with good radiochemical yield and high molar activity and radiochemical purity by 18F-fluoroethylation of the precursor with Boc-protecting group (15) with [18F]2-fluoro-1-bromoethane ([18F]FEB). Ex vivo biodistribution studies revealed a small to moderate increase in radioligand uptake in the brain and peripheral organs of LPS-induced rats compared to control animals. Pretreatment with celecoxib resulted in significant blocking of radioactivity uptake in the brain (pons and medulla), heart, lungs, and kidneys, indicating that [18F]F-IV is likely to specifically bind to COX-2 in a rat model of neuroinflammation. However, in comparison with [11C]MPbP, the new radioligand showed decreased brain uptake in LPS rats and high retention in the blood pool, which apparently could be explained by its high plasma protein binding. We believe that the structure of [18F]F-IV can be optimized by replacing the substituents in the biphenyl core to eliminate these disadvantages and develop new radioligands for imaging activated microglia.


Neuroglia ◽  
2021 ◽  
Vol 2 (1) ◽  
pp. 89-97
Author(s):  
Satoshi Okuyama ◽  
Masafumi Matsuda ◽  
Yuna Okusako ◽  
Sanae Miyauchi ◽  
Toshiki Omasa ◽  
...  

Inflammation is the cause and/or result of many diseases in peripheral tissues and the central nervous system. Recent findings suggested that inflammation in peripheral tissue induces an inflammatory response in the brain that activates glial cells, which, in turn, induce neuronal cell dysfunction. Therefore, anti-inflammatory compounds are important for the suppression of chronic inflammation and prevention of disease. The present study revealed microglial activation in the hippocampus of the brain two days after the peripheral administration of lipopolysaccharide (LPS). Furthermore, the expression of the synaptic vesicle membrane protein, synaptophysin, in the CA3 stratum lucidum of the hippocampus was down-regulated 7 days after the LPS injection. The administration of tocotrienols, a type of vitamin E, significantly attenuated these changes in the hippocampus. Collectively, the present results demonstrated the spread of peripheral inflammatory responses to the brain, in which glial activation and neuronal dysfunction were induced, while tocotrienols exerted anti-inflammatory effects and protected neurons from damage.


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