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Rhubarb
Published in Mahendra Rai, Shandesh Bhattarai, Chistiane M. Feitosa, Ethnopharmacology of Wild Plants, 2021
Gan B. Bajracharya, Richa K. Gupta
Rhubarb is well known for its cathartic and diuretic effects, which are closely correlated with water adjustment of colon and kidney by the theory of traditional Chinese medicine (Li et al. 2008). Researches have indicated that the anthraquinone glycosides can bring about fairly obvious effects of ‘watery diarrhea’. Rhubarb regulates aquaporins in the colon that lead to less absorption of water and more secretion of intestinal juice. It is likely that aquaporin 2 is regulated through protein kinase A signal pathway (Zhang et al. 2008).
Anti-Cancer Agents from Natural Sources
Published in Rohit Dutt, Anil K. Sharma, Raj K. Keservani, Vandana Garg, Promising Drug Molecules of Natural Origin, 2020
Debasish Bandyopadhyay, Felipe Gonzalez
Anthraquinones are naturally occurring aromatic compounds, found in certain plant families viz. Fabaceae, Liliaceae, Polygonaceae, and Rhamnaceae. Their presence are seen in marine-derived fungi, for example, Microsporum sp. The major use of anthraquinones is as color pigment and they are used commercially to prepare natural dyes. Anthraquinones affect the cell cycle of malignant cells by disrupting it. Cancer cells may follow diverse pathways to avoid the influence of antineoplastic medicines which eventually may result in DNA damage. To make sure that DNA is not damaged, checkpoint proteins are able to control pathways by manipulating cell cycle. Tumorigenesis occurs when the tumor is formed because the cells lose checkpoint controls, this is the main reason why chemotherapy is required to regulate the cell cycle. Aside from being used commercially, anthraquinones are used extensively in pharma industries. For instance, Rheum palmatum or Rhubarb, a good source of anthraquinones, is still being used today. Traditionally, Rhubarb is used as a phytomedicine to treat constipation, jaundice, and some ulcers. But studies conducted on Rhubarb determined that its anthraquinones are able to prevent the proliferation of numerous cancer cells.
Chronic Idiopathic Constipation
Published in Kevin W. Olden, Handbook of Functional Gastrointestinal Disorders, 2020
Stimulant laxatives include castor oil, anthraquinones (cascara sagrada, senna, and casanthranol), and diphenylmethanes (phenolphthalein and bisacodyl). Castor oil is hydrolyzed by intestinal lipases to ricinoleic acid, which stimulates intestinal secretion and intestinal motility. Anthraquinone laxatives increase fluid and electrolyte accumulation in the distal ileum and colon and are pharmacologically activated when they come in contact with intestinal microorganisms. Pathological changes in the colon produced by chronic anthraquinone use include melanosis coli, a benign and reversible condition, and possible damage to the myenteric plexus (45). Bisacodyl and phenolphthalein act directly to stimulate colonic motor activity and inhibit glucose and sodium absorption to increase intraluminal fluid content.
Evaluation of WO2017098421: GSK’s benzothiazine compounds as CD73 inhibitor filings
Published in Expert Opinion on Therapeutic Patents, 2018
Ya-Ping Gong, Ren-Zhong Wan, Zhao-Peng Liu
The discovery of small molecular CD73 inhibitors is more challenging. The ADP analogs, AMPCP (Figure 2), is the first studied CD73 inhibitor [39–41]. Structural modifications of AMPCP at the adenine core, the sugar moiety, and the phosphate portion were appeared in two patent filings [42,43]. In addition, several flavonoid-based compounds and anthraquinone derivatives were found to inhibit CD73 [44,45]. However, the anthraquinones are not suitable for therapeutic use, since they are charged under physiological conditions. A structure-based virtual screening has identified more druglike sulfonamide inhibitors represented by compound 1 [46]. Benzothiadiazine derivatives are first disclosed as CD73 inhibitors in the patent filings that form the subject of this evaluation [47].
Phytochemical composition, toxicity, and repellent effects of medicinal plants Peganum harmala, Pterocarya fraxinifolia, and Tanacetum parthenium extracts against Sitophilus oryzae L.
Published in Toxin Reviews, 2023
Mahmoud Fazeli-Dinan, Seyed Hanif Osia-Laghab, Mina Amini, Ali Davoodi, Seyed Hassan Nikookar, Jamshid Yazdani Charati, Mohammad Azadbakht, Ahmadali Enayati
The phytochemical compounds present in different extracts under study on qualitative basis are shown in Table 1. Peganum harmala showed the presence of most phytochemicals including steroid, terpenoid, alkaloids, tannin, and flavonoid. Steroid, terpenoid, and flavonoid were detected in T. parthenium; and P. fraxinifolia contained flavonoid and tannin. It should be noted that anthraquinone was absent in all plant extracts.
Pharmacokinetics, tissue distribution and excretion of five rhubarb anthraquinones in rats after oral administration of effective fraction of anthraquinones from rheum officinale
Published in Xenobiotica, 2021
Di Zhao, Su-Xiang Feng, Hao-Jie Zhang, Na Zhang, Xue-Fang Liu, Yan Wan, Yu-Xiao Zhou, Jian-Sheng Li
Concentrations of aloe-emodin, rhein, emodin, chrysophanol, physcion were determined at different time points after i.g. administration of rhubarb extract (300 mg/kg) in various tissues of rats, which were shown in Figure 3(a–e). And the AUC of the five anthraquinones in different internal organs were displayed in Figure 4. The results suggested that different levels of five anthraquinones were observed in most tissues at 10 min after i.g. administration of rhubarb extract to rats. Even at 24 h, five anthraquinones were still detectable in all collected tissues, but obvious downward trend. It indicated that five anthraquinones could be distributed rapidly and widely, while eliminated slowly with time. The tissue contents of each anthraquinone were ranked as follows: stomach > liver > intestines > kidney > lung > spleen > heart > brain > plasma for aloe-emodin, stomach > kidney > liver > intestines > lung > plasma > spleen > heart > brain for rhein, stomach > intestines > liver > kidney > lung > spleen > heart > brain > plasma for emodin, stomach > intestines > kidney > liver > lung > brain > heart > spleen > plasma for chrysophanol, and stomach > intestines > liver > kidney > lung > brain > heart > spleen > plasma for physcion. The results demonstrated that the highest concentration of five anthraquinones was observed in stomach followed by the intestine. The high affinity in the intestine of five anthraquinones confirmed that it had a good curative effect on constipation and gastrointestinal disease. The high level in liver, lung and kidney demonstrated that they might be the primary metabolic organs of five anthraquinones, which might lead to the first-pass effect to reduce the absorption of the drug in plasma. Meanwhile, the low level of five anthraquinones found in spleen, heart, brain. Five anthraquinones could be detected in brain, suggesting that they were able to cross the blood-brain barrier (BBB). These results were in accordance with the findings of our study that the main pharmacological effect of five anthraquinones was resisting the cerebral ischaemia-reperfusion. In addition to rhein, the concentrations of the other four anthraquinones in most tissues were higher than plasma, which could account for much more lipophilic and thus less soluble than rhein.