Anti-Cancer Agents from Natural Sources
Rohit Dutt, Anil K. Sharma, Raj K. Keservani, Vandana Garg in Promising Drug Molecules of Natural Origin, 2020
In rhubarb, the main anticancer anthraquinones were emodin, aloe-emodin, rhein, and chrysophanol (Figure 5.7). Early studies conducted on emodin showed that it could prevent cell proliferation in breast, cervical, colon, and prostate cancers (Chang et al., 1999; Pecere et al., 2000; Ren et al., 2018). Also, emodin has little or no cytotoxic effect in normal cells, suggesting that normal cells are comparatively safe than cancer cells when it comes to emodin-induced cytotoxicity. Aloe-emodin could inhibit the cell growth in many malignant tumors like hepatoma (liver) (Cha et al., 2005), human lung carcinoma (Chan et al., 1993; Jeon et al., 2012) and leukemia (Yeh et al., 2003). Jeon et al. (2012) treated hepatoma (HUH-7) cells with a dose-dependent concentration of aloe-emodin. He concluded that aloe-emodin could decrease CAPN2 and UBE3A, two essential proteins, which reduces cell growth and speeds up apoptosis. Since the mechanistic routes of aloe-emodin is unknown in H640 (lung cancer) cells, Yeh et al. (2003) conducted a study to evaluate the cytotoxicity of aloe-emodin in H640 cells. When introduced, the initial observation was apoptosis due to the modification of cAMP-dependent protein kinase. Other important protein expressions that were modified were BCL-3, protein kinase C, caspase-3, and p38.
Bone Regeneration Effect of Cassia occidentalis Linn. Extract and Its Isolated Compounds
Brijesh Kumar, Vikas Bajpai, Vikaskumar Gond, Subhashis Pal, Naibedya Chattopadhyay in Phytochemistry of Plants of Genus Cassia, 2021
Induction of osteoblast differentiation by emodin is associated with the upregulation of BMP-9, osterix, activin receptor-like kinase 1 (ALK1), smad 1, smad 9 and Msh homeobox 2 (Msx2) mRNA levels in osteoblasts. Emodin-induced osteogenic differentiation could be blocked by noggin, thus suggesting the role of BMP-9 as the mediator of this process as BMP-2 expression was unchanged by emodin. In OVX rats, emodin (100 mg/kg, route of administration unspecified) given for 12 weeks although inhibited tartrate-resistant acid phosphatase 5b (TRACP5b, the surrogate of osteoclast number) had no effect on preventing loss of bone volume and strength. A “low dose” E2 (50 μg/kg) also had no effect however, when combined with emodin, complete protection against OVX-induced trabecular osteopenia and loss of strength was observed. As 50 μg/kg E2 had no uterotrophic effect, a combination of low-dose E2 and emodin has been suggested for the treatment of postmenopausal osteoporosis (Chen et al., 2017).
Nano Delivery of Antiviral Plant Bioactives as Cancer Therapeutics
Devarajan Thangadurai, Saher Islam, Charles Oluwaseun Adetunji in Viral and Antiviral Nanomaterials, 2022
Emodin, an anthraquinone extracted from aloe vera is used to treat liver injuries, necrosis, inflammation, and kidney diseases and to treat carcinoma. Studies report that aloe-emodin exhibits antiviral properties against enveloped viruses like influenza A virus and herpes simplex virus. It is also shown to obstruct attachment, entry, and replication of the influenza virus (Gansukh et al. 2018). The anticancer properties of aloe-emodin have been found to inhibit cancer cells like hepatoma cells, glioma, and carcinoma cells. It also possesses strong anti-proliferative and antineoplastic reaction on cancer cells due to its apoptotic nature (Chou and Liang 2009).
Experimental anti-tumor effect of emodin in suspension – in situ hydrogels formed with self-assembling peptide
Published in Drug Delivery, 2021
Weipeng Wei, Jianhua Tang, Lei Hu, Yujie Feng, Hongfang Li, Chengchen Yin, Fushan Tang
Emodin (EM) is a natural anthraquinone derivative extracted from the rhizome of rhubarb, polygonum cuspidatum, polygonum multiflorum, and other traditional Chinese medicines (shown in Figure 1(A)). Many studies have shown that EM has anti-inflammatory, bacteriostatic, and immunomodulatory effects (Lee et al., 2010; Lu et al., 2011; Alisi et al., 2012). With the further study of the anticancer activity of EM, the researchers also found that EM can treat lung cancer, breast cancer and other cancers by inhibiting cancer cell proliferation, migration, and promoting its apoptosis (Fu et al., 2007; Li et al., 2013). As EM is practically insoluble in water, easily precipitating to form crystals in water solution, and its characteristic of sudden release in a short time, together with its large side effects, EM has limited clinical use. Even in in vivo and in vitro experiments, it is inevitable to use some organic solvents such as dimethyl sulfoxide (DMSO), ethanol, or methanol before they can be used. The use of solvents, such as DMSO, which is toxic to the body, limited the administration concentration of EM (Park et al., 2019; Tu et al., 2019). Therefore, EM’s water solubility is crucial to treat cancer, it is necessary to develop a suitable drug delivery system to improve the delivery of EM and other hydrophobic drugs, to improve the efficacy while reducing the side effects of these drugs.
Macrophage polarization: an effective approach to targeted therapy of inflammatory bowel disease
Published in Expert Opinion on Therapeutic Targets, 2021
Yaoyao Du, Lan Rong, Yuanhua Cong, Lan Shen, Ning Zhang, Bing Wang
Emodin (1,3,8-trihydroxy-6-methylanthraquinone) is an anthraquinone derivative found in Chinese herbs such as Rheum palmatum, Polygonum cuspidatum, P. multiflorum, and Aloe vera [194].Several reports showed that emodin has a therapeutic efficacy on viruses, bacteria, and osteoporosis and also has relatively good inhibitory effect on inflammation and tumors [194]. Luo et al. studied the protective effect of emodin on DSS-induced UC in mice and found that emodin mitigates inflammation by significantly downregulating the expression of TLR5 and NF-κB p65 in the colon [195]. Furthermore, emodin has been shown to inhibit M1-associated signals including NF-κB, IRF5, MAPK, and STAT1 [22]. Importantly, it can also promote the expression of M2-associated molecules such as TGF-β and PPARγ [196]. However, under certain circumstances, emodin can inhibit the activation of STAT6 and IRF4 signals while suppressing the polarization of M1 macrophages, thereby reducing the response of macrophages to M1 and M2 stimuli [197].
Qingyi granules ameliorate severe acute pancreatitis in rats by modulating the gut microbiota and serum metabolic aberrations
Published in Pharmaceutical Biology, 2023
Juying Jiao, Jianjun Liu, Fei Luo, Mengxue Shang, Chen Pan, Bing Qi, Liang Zhao, Peiyuan Yin, Dong Shang
Emodin is the main effective ingredient of Rheum officinale, the primary drug in Qingyi granules. Studies have shown that emodin can induce circulating neutrophil apoptosis through the Ca2+-calpain1-caspase12-caspase-3 signaling pathway to protect SAP rats from excessive inflammation (Wang et al. 2016), In addition, emodin suppresses the P2X7/NLRP3 signaling pathway and reactive oxygen species generation to reduce the production of proinflammatory factors (Xia et al. 2019; Zhang et al. 2019). Moreover, sodium taurocholate-induced pancreatic acinar cell damage could be attenuated by emodin via miR-30a-5p/HTRA1 (Xiang et al. 2017). Considering that the crude drug emodin is poorly absorbed, intestinal interplay was predicted to contribute to its distal effects. Here, emodin was tested in a parallel group to study whether there were similarities between the compound formula in Qingyi granules and monomeric emodin in SAP treatment. We integrated microbiome research and metabolomics to investigate SAP-associated gut dysbiosis and serum metabolite alterations, aiming to reveal the potential enterogenic repair mechanism of Qingyi granules and emodin.
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