Febrifugine and Its Analogs: Studies for Their Antimalarial and Other Therapeutic Properties

Ningthoujam, Sanjoy Singh; Talukdar, Anupam Das; Nath, Deepa; Basar, Norazah; Potsangbam, Kumar Singh; Choudhury, Manabendra Dutta

doi:10.1016/b978-0-444-63460-3.00003-1

Cited by 9 publications

(4 citation statements)

References 74 publications

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“…In addition, it has a similar docking score to those found in Febrifuginequinazoline alkaloids, which were tested experimentally with successful anti-Trypanosoma cruzi activity but high toxicity to human cells, thus limiting its use. [40] Future studies will focus on the isolation of a,10ba-dihydroxy-9-Odemethylhomolycorine in tropical regions where it can be found [26] to validate our results and also to determine its selectivity towards Trypanosoma cruzi.…”

Section: Resultsmentioning

confidence: 74%

Finding for New Drugs in Nature for Neglected Tropical Diseases: In Silico Study of Homolycorine Alkaloids against Chagas Disease

Mora,

Schosinsky,

Castellón

et al. 2023

Preprint

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Chagas disease or American trypanosomiasis is a neglected tropical disease (NTD). It is mainly caused by infection with the Trypanosoma cruzi parasite. In this study, part of an Ibero-American project of a CYTED network devoted to the use of Amaryllidaceae alkaloids as templates for the synthesis of new pharmaceuticals, we have performed a virtual screening of homolycorine-type alkaloids where two alkaloids, 10-Norneronine and 2,10b-dihydroxy-9-O-demethylhomolycorine, can be the basis for the design of new drugs due to their interaction with both Trypanothione reductase (TR), and Cruzain (CZ) showing scores close to -7 kcal/mol in molecular docking studies.

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Section: Resultsmentioning

confidence: 74%

Finding for New Drugs in Nature for Neglected Tropical Diseases: In Silico Study of Homolycorine Alkaloids against Chagas Disease

Mora,

Schosinsky,

Castellón

et al. 2023

Preprint

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“…At present, chemoprophylaxis and anticoccidial feed additives are used to control the spread of coccidiosis, in addition to the chemical synthesis of drugs with excellent efficiency to prevent and treat chicken coccidiosis, including diclazuril, toltrazuril, and halofuginone. Many studies have been conducted on the anticoccidial effects and mechanism of the above-mentioned drugs [25]. However, these methods have become complicated by the emergence of drug resistance and the toxic effects of such additives on animal health [10][11][12].…”

Section: Discussionmentioning

confidence: 99%

Efficacy of an Oral Solution Prepared from the Ultrasonic Extract of Radix dichroae roots against Eimeria tenella in Broiler Chickens

Wang¹,

Guo²,

Gong

et al. 2020

Evidence-Based Complementary and Alternative Medicine

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This study was conducted to determine the optimal dose of the oral solution of the ultrasonic extract of Radix dichroae (UERD) and to provide experimental support for a safe clinical dose for anticoccidial treatment of broiler chickens. Radix dichroae root extracts were prepared using the ultrasonic extraction method. The anticoccidial activity of the oral solution prepared from the ultrasonic extract of Radix dichroae roots was tested in broiler chickens following oral infection with a field isolate of E. tenella. Ninety Lingnan yellow broiler chickens (14 days old) were randomly divided into nine groups (n = 10), including six UERD oral solution treatments (0.25, 0.50, 1.50, 2.50, 3.50, and 5.00%), a toltrazuril group (0.10%), an E. tenella-infected control group, and a healthy control group. All groups were inoculated orally with 7 × 104 sporulated E. tenella oocysts (Guangdong strain) except for the healthy control group. The chickens in the seven drug-treated groups were administered a UERD oral solution or toltrazuril in drinking water for 7 days. The anticoccidial efficacy of the UERD oral solution was evaluated by the bloody diarrhoea severity level, relative body weight gain (rBWG), lesion score, oocyst per gram (OPG), and anticoccidial index (ACI). Compared with the infected control group, there were no significant differences in the groups treated with UERD oral solution or toltrazuril with regard to the lesion changes in the caecal regions (P>0.05); however, the blood contents, OPG, and oocyst score in three UERD oral solution treatment groups (0.50, 1.50, and 2.50%) were significantly reduced, and the bloody diarrhoea was also alleviated. The ACI in three UERD oral solution treatment groups (0.50%, ACI = 143.7; 1.50%, ACI = 151.0; and 2.50%, ACI = 144.3) was higher than that in the toltrazuril group (ACI = 127.0), and the rBWG in the 1.50% UERD oral solution treatment group (95.0%) was similar to that in the healthy control group (100%), which was also 12.5% higher than that in the toltrazuril group (82.5%). The findings of this study demonstrated that the UERD oral solution (0.50% ～ 2.50% dose range) showed better prevention, anticoccidial efficacy, and growth promotion effects than toltrazuril (0.10%), and the 1.50% dose level of UERD oral solution in water is the clinically recommended dose according to the present study conditions.

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“…is the dry root of Saxiaceae Changshan which contains mainly alkaloids, coumarins, steroids, polyphenols and other chemical constituents. Isofebrifugine (IFE) which is one of its main alkaloids, has a variety of biological effects, including anti-malaria, anti-tumor, anti-inflammation, and wound-healing properties (8)(9)(10)(11). Studies have shown that IFE is used to antagonize bladder, prostate, breast, skin and lung tumors through inhibition of tumor angiogenesis, proliferation and migration (11)(12)(13)(14).…”

Section: Introductionmentioning

confidence: 99%

Effect of isofebrifugine on the proliferation and invasion of human gastric cancer cells via MMP

Tang

2020

Cell Mol Biol (Noisy-le-grand)

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Gastric cancer (GC) is one of the most common fatal cancers among gastrointestinal malignancies. At present, the treatment of gastric cancer involves a combination of surgery and chemotherapy. Isofebrifugine (IFE) is an alkaloid with many biological properties. In this study, results from MTT, scratch and invasion assays showed that IFE significantly inhibited the proliferation, migration and invasion of SGC7901 gastric cancer cells. Through RT-PCR and Western blot experiments, it was revealed that IFE significantly inhibited the mRNA and protein expressions of MMP-2, MMP-9 and SDF-1 which are closely related to cancer invasion and metastasis. Thus, IFE possesses anti-gastric cancer properties.

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Febrifugine and Its Analogs: Studies for Their Antimalarial and Other Therapeutic Properties

Cited by 9 publications

References 74 publications

Finding for New Drugs in Nature for Neglected Tropical Diseases: In Silico Study of Homolycorine Alkaloids against Chagas Disease

Finding for New Drugs in Nature for Neglected Tropical Diseases: In Silico Study of Homolycorine Alkaloids against Chagas Disease

Efficacy of an Oral Solution Prepared from the Ultrasonic Extract of Radix dichroae roots against Eimeria tenella in Broiler Chickens

Effect of isofebrifugine on the proliferation and invasion of human gastric cancer cells via MMP

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