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Inflammatory Biomarkers: An Important Tool for Herbal Drug Discovery
Published in Mahfoozur Rahman, Sarwar Beg, Mazin A. Zamzami, Hani Choudhry, Aftab Ahmad, Khalid S. Alharbi, Biomarkers as Targeted Herbal Drug Discovery, 2022
Mahfoozur Rahman, Ankit Sahoo, Mohammad Atif, Sarwar Beg
Celastrol is pentacyclic triterpene obtained and used in Chinese traditional medicine. It has anti-tumor and anti-inflammatory properties. During the daily administration to AIA rats of celastrol I.P administration, shows anti-inflammatory action possibly through the inhibition of caspase-1 and inhibits the activation of NF-JB, and downregulation of the IL-lb and TNF secretion in an AIA rat model.
Phytosomes as Novel Carriers of Herbal Extracts
Published in Madhu Gupta, Durgesh Nandini Chauhan, Vikas Sharma, Nagendra Singh Chauhan, Novel Drug Delivery Systems for Phytoconstituents, 2020
Sevgi Güngör, Özlem Akbal-Dağıstan, Evren Algın Yapar, Murat Kartal, Yıldız Özsoy
Diosmin is classified as a phlebotonic flavonoid with a great potential for treatment of colon and hepatocellular carcinoma and also possesses good safety profile with a high tolerability. Freag and his colleagues (2013) demonstrated an extensive study that covered formulation, optimization, characterization, and ex vivo permeation of diosmin from its phytosome formulation and suggested that lyophilized formulation of diosmin could significantly increase the dissolution rate of diosmin compared to its marketed available options. Phytosome formulation can also enhance intestinal permeation of diosmin in rats. A second study performed by the same research group investigated the laminated chitosan: hydroxyproply methylcellulose composite sponges loaded with tripterine liposomes and functionalized with protamine. The results from the in vivo pharmacokinetic data and ex vivo permeation data confirmed an increased rate of buccal delivery of the chitosan-based phytosome (Freag et al., 2018a). A third study from Freag and his co-workers (2018b) highlighted for the first time formulation of self-assembled phytosome nanocarriers to increase solubility and oral bioavailability of celastrol. As a conclusion of in vitro release and in vivo pharmacokinetic data, it was shown that there is a great potential usage of phytosome nanocarriers systems of celastrol for oral cancer treatment.
Plant-Based Natural Products Against Huntington’s Disease: Preclinical and Clinical Studies
Published in Megh R. Goyal, Hafiz Ansar Rasul Suleria, Ademola Olabode Ayeleso, T. Jesse Joel, Sujogya Kumar Panda, The Therapeutic Properties of Medicinal Plants, 2019
Banadipa Nanda, Samapika Nandy, Anuradha Mukherjee, Abhijit Dey
The absolute bioavailability of α-mangostin, another reported anti-HD phytochemical, was also increased in animals when administered orally as a soft capsule [135]. Similarly, unmatched biochemical properties of celastrol were nullified by nanoencapsulation, which also contributed to its enhanced bioactive efficacy [102]. It has also been reported that the self-micro emulsifying drug delivery system (SMEDDS) dispersible tablet can be the mode of oral administration for celastrol [90].
Dextran sulfate-based MMP-2 enzyme-sensitive SR-A receptor targeting nanomicelles for the treatment of rheumatoid arthritis
Published in Drug Delivery, 2022
Caiwei Yu, Hui Liu, Chunjing Guo, Qiang Chen, Yanguo Su, Huimin Guo, Xiaoya Hou, Feng Zhao, Huaying Fan, Hui Xu, Yan Zhao, Xiaofeng Mu, Guohua Wang, Haiyu Xu, Daquan Chen
Celastrol was a pentacyclic triterpene compound extracted from Tripterygium wilfordii, belonging to the quinone methide family (Bao and Dai 2011; Chen et al. 2018；Luo et al. 2019). Celastrol has shown the ability to inhibit the development of rheumatoid arthritis, obesity and metabolic dysfunction and the proliferation of different cancer cells (Kashyap et al. 2018; Tang et al. 2018; Zeng et al. 2018). Celastrol’s shortcomings were poor water solubility and low bioavailability, which greatly limited its effect. To resolve this drawback, amphiphilic polymer had been adopted. Macrophages played a very central pathogenic role in the development of RA (Sun et al. 2017; Keewan and Naser 2020). Fibroblast-like synovial cells contributed to the pathological changes in the rheumatoid synovium and the propagation of inflammation. Accumulating evidence had implicated celastrol inhibits RA-FLS proliferation by inducing apoptosis in vitro, DNA damage and cell cycle arrest (Tice et al. 2000; Xu et al. 2013).
Celastrol-conjugated chitosan oligosaccharide for the treatment of pancreatic cancer
Published in Drug Delivery, 2022
Xiaohu Zeng, Xin Zhu, Qikang Tian, Xiaoke Tan, Ning Sun, Min Yan, Junwei Zhao, Xiangxiang Wu, Ruiqin Li, Zhenqiang Zhang, Huahui Zeng
Celastrol group after administered at a dose of 6 mg/kg displayed obvious elevation of both ALT and AST in comparison with control group, indicating the occurrence of liver injury (p < .01, Figure 7(A,B). However, Cel-CSO groups all showed no significant increase of both ALT and AST. After administered at a dose of 6 mg/kg, Cel-CSO group showed an obvious reduction of both ALT and AST compared with Celastrol group (p < .01), which was still normal for hepatic metabolic function. Significant increase of BUN and Crea indicated the kidney dysfunction including dilation of kidney proximal tubules (Figure 7(C,D)). Celastrol at a dose of 6 mg/kg caused higher BUN and Crea level in mouse serum than the Cel-CSO conjugate at the same dose (p < .05), while the Cel-CSO conjugates of 2, 4 and 6 mg/kg all had only slight effects on BUN and Crea. The results suggested that the Celastrol treatment was associated with nephrotoxicity and hepatotoxicity. Furthermore, the toxicity of Celastrol increased in dose-dependence manner. The Cel-CSO group demonstrated a slight increase in AST, ALT, BUN and Crea levels, indicating that the incidence of Cel-CSO induced kidney and liver toxicity is very low.
In vitro immunomodulatory activity of celastrol against influenza A virus infection
Published in Immunopharmacology and Immunotoxicology, 2018
Niloofar Khalili, Ali Karimi, Mohammad-Taghi Moradi, Hedayatollah Shirzad
Celastrol, which is a quinone methide also called tripterine, is an active compound derived from the root bark of the traditional Chinese medicine27Tripterygium wilfordii Hook27,28, a perennial creeping plant indigenous to a large area in southern China, known as Thunder of God vine, which belongs to the family Celastraceae. In several animal models, it has been reported to exert anti-inflammatory properties without toxicity. Thus, celastrol can serve as an interesting modulator of the inflammatory and immune responses29. Celastrol has been effectively used to treat chronic inflammation, autoimmune diseases such as arthritis, lupus erythematosus, lateral sclerosis and neurodegenerative diseases because of its anti-inflammatory activity27. It has been shown that the NF-kB pathway comprises the direct targets and molecular mechanisms of celastrol. Recent investigations have shown that celastrol can reduce production of TNFα and IL6 in Crohn’s disease and production of IL6 in prostate cancer by affecting the NF-kB pathway, which leads to decreased inflammation in Crohn’s disease and inhibiting cancer cell differentiation in the prostate29,30.