scholarly journals Phytochemical and safety evaluations of Diospyros mespiliformis, and in silico evaluations of drug-likeness, pharmacokinetics and acute toxicity of its bioactive compound (Diospyrin)

2021 ◽  
Vol 1 (2) ◽  
pp. 11-19
Author(s):  
Chizoba P. Agbadoronye ◽  
Simon O. Abolarinwa ◽  
Khadeejah O. Nasir-Naeem ◽  
Victor E. Oigbochie ◽  
Adonis E. Irhue ◽  
...  

Diospyros mespiliformis is among the popular multipurpose tropical fruit trees, commonly used as herbal medicines. However, due to the lack of adequate scientific data on the safety of this plant, the present study was conducted to determine the phytochemical compositions and acute toxicity profile of the crude methanol extract of D. mespiliformis. In addition, diospyrin, a bioactive compound from the plant was evaluated for in silico drug-likeness, pharmacokinetics (PKs) and acute toxicity. The phytochemical contents of the plant were quantified using standardized protocols while the 50% lethal dose (LD50) was evaluated using Lorke’s methods. Results revealed that flavonoids (265.46±0.32 mg/g) are the most abundant phytochemical in methanol leaf extract of D. mespiliformis, followed by alkaloids (224.56±0.19 mg/g) and phenols (191.82±0.04 mg/g) while saponins (7.90±0.32 mg/g) was the least abundant phytochemical. The plant extract has LD50 of > 5000 mg/kg in rats. No death was recorded throughout the study period. Similarly, no behavioural changes were observed in animals dosed with the crude extract at 10 -2900 mg/kg BW. Animals administered 5000 mg/kg BW were hyperactive, restless, and displayed profused breathing which lasted only for 30 minutes after administrations. Diospyrin a bioactive compound from D. mespiliformis demonstrated good druglike candidates and exhibited a high safety profile as revealed by in silico study. In conclusion, the crude methanol extract of D. mespiliformis and its bioactive compound is well-tolerated and non-toxic to rats, and thus could be considered a safe medicinal plant for acute oral remedies

2021 ◽  
Vol 14 (1) ◽  
pp. 018-026
Author(s):  
Charles Akhadelor Unuigbe ◽  
Chinem Fumi Unula ◽  
Anthony Aiwonegbe ◽  
Jeremiah Ogboma Uadia ◽  
Isaac Akhigbe ◽  
...  

Polyalthia longifolia (masquerade tree) is a plant which is believed to possess varied pharmacological and therapeutic values among different populations. The present report investigated the phytochemical composition, proximate, acute toxicity and antioxidant potential of P. longfolia root. All analyses were carried out using established methods; the antioxidant activity of the crude methanol extract and its fractions (n-hexane and ethyl acetate) were examined using 1,1-diphenyl-2-picrylhydrazyl (DPPH) radical scavenging assay while the total phenolic and flavonoid contents were assessed using the Folin-Ciocalteu and the aluminum chloride calibration methods respectively. The phytochemical analysis revealed the presence of alkaloids, carbohydrate, reducing sugars, tannins, saponins, flavonoids, phenolic compounds and protein in aqueous extract. The proximate analysis showed moisture content, total ash, alcohol extractive value, water extractive value, acid insoluble ash and water soluble ash at 8.80, 9.35, 3.28, 3.29, 2.27 and 7.29% respectively. The ethyl acetate fraction showed the highest antioxidant property compared to the n-hexane fraction and crude methanol extract in all assays conducted. Also, the methanol fraction was found to have the highest flavonoids and phenolic content among the extract and fractions. Oral administration of crude methanol extract of P. longifolia to Swiss mice was relatively non-toxic at a maximum dose of 5000 mg/kg. The root extract and fractions of P. longifolia indicated moderately high level of some phytochemicals with outstanding radical scavenging activity, and therefore substantiate its use as a conventional and comparatively non-toxic plant antioxidant.


2021 ◽  
Vol 3 (1) ◽  
pp. 41-48
Author(s):  
Joseph Fomnya Hyellavala

The methanol extract of Securidaca longepedunculata root bark was screened phytochemically and its intraperitoneal acute toxicity evaluated in mice. The phytochemical screening was carried out based on standard methods. The Median Lethal Dose (LD50 ) was determined using Lorke’s method while the Maximum Tolerated Dose (LD0 ) was determined by the method described by Mosser and Padilla. The root bark extract revealed the presence of carbohydrates, terpenoids, cardiac glycosides, saponins and flavonoids. The extract produced intraperitoneal LD0 and LD50 values of 6.92 mg/kg and 6.0 mg/kg, respectively. Based on the research findings, the methanol extract of S. longepedunculata root bark was found to contain important phytochemicals which may be attributed to its enormous use in traditional medicine, but it was a highly toxic extract in mice with intraperitoneal LD50 and LD0 values of 6.92 mg/kg and 6.0 mg/kg, respectively.


2012 ◽  
Vol 2012 ◽  
pp. 1-6 ◽  
Author(s):  
Prapassorn Bussaman ◽  
Piyarat Namsena ◽  
Paweena Rattanasena ◽  
Angsuman Chandrapatya

Colletotrichum gloeosporioides(Penz.) Sacc. is a fungus that causes anthracnose disease in tropical fruit plants, resulting in damages of the fruit plants and low yield and quality of fruits. The use of chemical fungicides is common for management of this disease, but it also results in the development of fungal resistance to the chemicals. Therefore, this study aims toin vitroevaluate the efficacy of 14 crude leaf extracts againstC. gloeosporioides. The results showed thatPiper sarmentosumleaf extracts, using 80% of ethanol, methanol, and chloroform as solvents, were found to have very high antifungal activities. Crude methanol extract ofP. sarmentosumleaves could effectively inhibit the growth of fungal mycelium (100%), followed by crude chloroform extract (81.85%) and 80% ethanol extract (45.50%). Maximum inhibition ofC. gloeosporioidesspore germination could be obtained after application with crude methanol extract ofP. sarmentosumleaves and crude chloroform extract ofMentha cordifolialeaves at 1.25 and 2.5%, respectively. In conclusion, crude extracts ofP. sarmentosumleaves were found to be highly effective for inhibiting bothC. gloeosporioidesmycelium growth and spore germination, and they have a potential as the new natural fungicides for management of anthracnose disease.


Author(s):  
AKM Shahidur Rahman ◽  
Oqna; Arslan ◽  
Rama Saha ◽  
Nirupama Talukder ◽  
SMA Khaleque ◽  
...  

The crude methanol extract of leaves, seeds and stem-bark of Clitoria ternatea demonstrated a significant cytotoxic activity in a brine shrimp lethality bioassay test. The LC50 values of the crude methanol extract of leaves, seeds and stem-bark were found to be 25.82, 110.92, 179.89 μgm/ml respectively Among them crude methanol extract of leaves (25.82 μgm/ml) and methanol fraction of leaves (22.28 μgm/ml) showed a very promising cytotoxic activity. Further studies have been suggested to discover a novel bioactive compound from methanol fraction of leaves of Clitoria ternatea.   DOI: 10.3329/bjpp.v22i1.3564Bangladesh J Physiol Pharmacol 2006; 22(1/2) : 18-21


2012 ◽  
Vol 7 (9) ◽  
pp. 1934578X1200700 ◽  
Author(s):  
Tomoko Takemura ◽  
Tsunashi Kamo ◽  
Raihan Ismil ◽  
Baki Bakar ◽  
Naoya Wasano ◽  
...  

A crude methanol extract of Goniothalamus andersonii J. Sinclair strongly inhibited elongation of lettuce ( Lactuca sativa L.) radicles. We conducted bioassay-guided purification of G. andersonii bark extract and obtained goniothalamin as the major bioactive compound. Its EC50 values against elongation of lettuce radicles and hypocotyls were 50 and 125 μmol L−1, respectively. Among the six species tested, timothy was the most sensitive to goniothalamin. Quantification of this compound in other Goniothalamus species suggested that the plant inhibitory activity of this genus is explainable by goniothalamin, with G. calcareus as an exception.


Planta Medica ◽  
2009 ◽  
Vol 75 (09) ◽  
Author(s):  
WM Shaik Mossadeq ◽  
K Syamimi ◽  
MP Azyyati ◽  
ZA Zakaria ◽  
AK Arifah ◽  
...  

2020 ◽  
pp. 31-32
Author(s):  
Mikhail A. Levchenko ◽  
◽  
Natalia A. Sennikova ◽  

Toxicological assessment is a mandatory research step in the development of new insecticidal drugs. At the All-Russian Research Institute of Veterinary Entomology and Arachnology, a prototype of the insecticidal bait Mukhnet IF was obtained with an active ingredient content of 0.06% ivermectin and 0.015% fipronil, which showed a highly effective effect against houseflies. This work presents the results of the study of acute oral toxicity of the above agent. For this, male white mice with a live weight of 16-26 g were selected. They were kept on a starvation diet for one day in individual houses with water. The drug was given in mg/kg body weight the next day. A total of 33 doses have been tested, ranging from 100 mg/kg to 40,000 mg/kg. The animals were observed for 14 days. According to the research results, it was revealed that at doses up to 20,000 mg/kg there were no signs of intoxication, but when tested at 25,000 mg/kg in some mice, these signs were noted, and at 30,000, 35,000 and 40,000 mg/kg deaths were recorded 20±10, 45±30 and 60±20%, respectively. It was not possible to test the drug over the last above dose due to incomplete eaten by mice. According to the degree of danger for warm-blooded animals, the drug belongs to the 4th class of low-hazard drugs (average lethal dose of 5000 mg/kg or more) in accordance with the classification of GOST 12.1.007-76. When analyzing the literature data on the toxicological characteristics of preparations containing ivermectin and chlorfenapyr, it was revealed that the insecticidal agent in its acute toxicity for warm-blooded animals is comparable to known analogues.


Author(s):  
Kyoung- Sun Seo ◽  
Seong Woo Jin ◽  
Seongkyu Choi ◽  
Kyeong Won Yun

The antibacterial activity of three Cupressaceae plants (Thujaoccidentalis,ThujaorientalisandChamaecyparisobtusa) was tested against three bacteria using the agar diffusion method. The ether and ethylacetate fraction of crude methanol extract from the three plants showed potent antibacterial activity against the tested microorganisms. The result showed that Staphylococcus aureus revealed the most sensitivity among the tested bacteria. Thujaoccidentalisether fraction and Thujaorientalis hexane fraction exhibited the highest antibacterial activity against Staphylococcus aureus. E. coli was shown the highest MIC values compared to the other two tested bacteria, which indicates the lowest antibacterial activity against the bacterium. This study promises an interesting future for designing a potentially active antibacterial agent from the three Cupressaceae plants.


2020 ◽  
Vol 15 (3) ◽  
pp. 194-208
Author(s):  
Pravin Kumar ◽  
Dinesh Kumar Sharma ◽  
Mahendra Singh Ashawat

Atopic Dermatitis (AD) is a prolonged reverting skin ailment with characteristically distributed skin lesions. In the previous decades, researchers had shown a marked interest in AD due to its increased prevalence in developed countries. Although different strategies including biological and immune modulators are available for the treatment of AD, each has certain limitations. The researchers had shown considerable interest in the management of AD with herbal medicines. The establishment of herbal drugs for AD might eliminate local as well as systemic adverse effects associated with long term use of corticosteroids and also higher cost of therapy with biological drugs. The present review discusses the traditional East Asian herbal medicines and scientific data related to newer herbal extracts or compositions for the treatment of AD. In vivo animal models and in vitro cell cultures, investigated with herbal medicines to establish a possible role in AD treatment, have also been discussed in the paper. The paper also highlights the role of certain new approaches, i.e. pharmacopuncture, a combination of allopathic and herbal medicines; and novel carriers (liposomes, cubosomes) for herbal drugs on atopic skin. In conclusion, herbal medicines can be a better and safe, complementary and alternative treatment option for AD.


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