The anti-diarrheal and anti-inflammatory effects of hydroethanol extracts of ripe Annona muricata fruit pulp in Wistar rats using curative method.

Objective: The study aimed to determine the anti-diarrheal and anti-inflammatory activities of hydroethanolic extract of ripe Annona muricata fruit pulp (HEAMP) on Wistar rats. Methods: Fifty male Wistar rats were divided into five groups, each for the diarrhea and inflammatory phases. Groups A and B 10 mL/kg of distilled water and 2 mL of castor oil, Groups C, D, and E received 2 mL of castor oil + extract (150, 300, and 600 mg/kg). Groups A and B received 10 mL/kg of distilled water and 0.1 mL of egg white. Groups C, D, and E received the (0.1 mL) egg white and extract (150, 300, and 600 mg/kg). Data were analyzed using SPSS (25) using ANOVA followed by post hoc least significant difference, presented as mean ± standard error of the mean, and values considered significant at P < 0.05. Results: The acute toxicity test of HEAMP is above 5000 mg/kg and rich in flavonoids, saponins, and proteins, with carbohydrates and tannins, and glycosides at moderate levels. Steroids, alkaloids, amino acids, and triterpenoids were absent. Furthermore, 30 min after diarrhea induction, the treated groups significantly increased (P = 0.012) in fecal count compared to Group A. Compared to Group B, the treated groups had a significant decrease in the fecal count at 60, 90, 120, and 150 min. At 30-min, there was a significant increase (P = 0.000) in paw-size in the treated groups compared to Group A. The treated groups had significantly lower edematous paw-size levels from 60 to 150 min compared to Group B. Conclusion: The HEAMP had anti-diarrheal and anti-inflammatory properties and is safe for consumption.

Efflux Pump-Mediated resistance in Chemotherapy

Efflux pump mechanisms perform important physiological functions such as prevention of toxin absorption from the gastrointestinal tract; elimination of bile from the hepatocytes; effective functioning of the blood-brain barrier and placental barrier; and renal excretion of drugs. They exist in all living cells; but those in the bacterial and mammalian cells are more important to the clinician and pharmacologist; as they constitute an important cause of antimicrobial drug resistance; which contributes to treatment failure; high medical bills; and increased mortality / morbidity. This review was aimed at highlighting the role of efflux pump mechanisms in microbial resistance to chemotherapeutic agents. It was also aimed to elucidate their structure and mechanisms of action so as to integrate the efflux pump mechanisms in the design and development of novel antimicrobial agents.Findings from previous studies and research on this subject assessed through Google search; Pubmed; Hinari websites; as well as standard textbooks on chemotherapy; provided the needed information in the process of this review. Efflux pump inhibitors are promising strategies for preventing and reverting efflux-mediated resistance to chemotherapeutic agents. They are usually employed as adjuncts in antimicrobial and cancer chemotherapy. Toxicity; more common with the older-generation inhibitors such as verapamil and reserpine; constitutes the greatest impediment to their clinical applications. No efflux pump inhibitor has been approved for routine clinical use; as a result of doubtful clinical efficacy and unacceptably high incidence of adverse effects; particularly inhibition of the P-450 drug metabolizing enzyme. At present; their applications are mainly restricted to epidemiological studies. Nonetheless; the search for efficacious and tolerable efflux pump inhibitors continues because of the potential benefits. There is a need to consider efflux pump substrate selectivity in the design and development of novel chemotherapeutic agents

Evaluation of Antiulcer Properties of Ethanolic and Hot Aqueous Stem Extracts of Synclisia Scabrida on Experimentally Induced Ulcer Models in Albino Mice

Background : The treatment of peptic ulcer disease poses therapeutic challenges to both patients and physicians alike because of the tendency of ulcers to relapse. Drugs used in the treatment of this disease are either costly or are associated with high incidence of adverse effects. Synclisia scabrida is a plant used in ethnomedicine for the treatment of various forms of stomach disorders and menstrual pains. The medicinal properties of the plants are claimed to reside in the roots; stems; and the leaves. Aim : This study; therefore; is to verify this claim and elucidate the probable mechanism of action by using crude stem extracts of this plant on drug- and stress-induced ulcer models in albino mice. Materials and Methods : Crude ethanol and hot water extracts; EE and HWE respectively; of the stem were prepared. These extracts were fractionated and separated by chromatographic methods and the fractions pooled together as fractions (PF-1; PF-2; PF-3 respectively) based on their chromatographic mobility and color reactions. Phytochemical analysis was done on the extracts. Ulcer models were induced in albino mice by means of indomethacin; histamine; and stress after prior cytoprotection with orally administered crude extracts and control (cimetidine). Results : Phytochemical analysis of the crude extracts and their fractions revealed the presence of cardiac glycosides (+++); tannins (+++); saponins (+); flavonoids (++); carbohydrates (++) and alkaloids (+++). Acute toxicity study on the crude extracts and their fractions revealed relative safety at the dose of 5000 mg/kg. The crude extracts (EE and HWE) and their fractions (PF-1; PF-2; PF-3) significantly (P = 0.001) protected against indomethacin-; histamine- and stress-induced ulcers. The decrease in GIT motility produced by these extracts was comparable to that produced by atropine sulfate. Conclusion : The findings suggest that these extracts of Synclisia scabrida possess antiulcer and antispasmodic properties; which justify the claims for its use in the treatment of various forms of stomach disorders

Evaluation of Antiulcer Properties of Ethanolic and hot Aqueous Stem Extracts of Synclisia Scabrida on Experimentally Induced Ulcer Models in Albino Mice

The treatment of peptic ulcer disease poses therapeutic challenges to both patients and physicians alike because of the tendency of ulcers to relapse. Drugs used in the treatment of this disease are either costly or are associated with high incidence of adverse effects. Synclisia scabrida is a plant used in ethnomedicine for the treatment of various forms of stomach disorders and menstrual pains. The medicinal properties of the plants are claimed to reside in the roots; stems; and the leaves. Aim : This study; therefore; is to verify this claim and elucidate the probable mechanism of action by using crude stem extracts of this plant on drug- and stress-induced ulcer models in albino mice. Materials and Methods : Crude ethanol and hot water extracts; EE and HWE respectively; of the stem were prepared. These extracts were fractionated and separated by chromatographic methods and the fractions pooled together as fractions (PF-1; PF-2; PF-3 respectively) based on their chromatographic mobility and color reactions. Phytochemical analysis was done on the extracts. Ulcer models were induced in albino mice by means of indomethacin; histamine; and stress after prior cytoprotection with orally administered crude extracts and control (cimetidine). Results : Phytochemical analysis of the crude extracts and their fractions revealed the presence of cardiac glycosides (+++); tannins (+++); saponins (+); flavonoids (++); carbohydrates (++) and alkaloids (+++). Acute toxicity study on the crude extracts and their fractions revealed relative safety at the dose of 5000 mg/kg. The crude extracts (EE and HWE) and their fractions (PF-1; PF-2; PF-3) significantly (P = 0.001) protected against indomethacin-; histamine- and stress-induced ulcers. The decrease in GIT motility produced by these extracts was comparable to that produced by atropine sulfate. Conclusion : The findings suggest that these extracts of Synclisia scabrida possess antiulcer and antispasmodic properties; which justify the claims for its use in the treatment of various forms of stomach disorders

Effect of mefloquine on the mechanical activity of the mouse isolated rectal smooth muscle.

The effects of mefloquine on the mechanical activity of the mouse isolated rectal smooth muscle was studied. Mefloquine (4.1 x 10(-5) - 5.2 x 10(-3)M) when applied alone and separately exerted variable effects on the rectum. In some preparations, it caused slight phasic contractions while in others no response was elicited. When the external Ca(2+) was increased from 1.8 mM to 300 mM mefloquine produced phasic contractile activity which was abolished on return to normal 1.8mM suggesting that the contractile activity was due to extracellular Ca(2+) influx. Mefloquine [4.1 x 10(-6)M - 4.1 x 10(-4)M] caused contraction-dependent inhibition of KCL, Carbachol and CaCl2 [in depolarizing Tyrode solution]. Mefloquine [2.1 x 10(-4)M] blocked KCL, but not carbachol contractions which were largely reversed by increasing [Ca2+]. The results show that mefloquine possesses anticholinergic and appreciable calcium channel blocking activity.

Management of anemic effects of chloramphenicol using amino acids on albino rats infected with Salmonella typhi.

Chloramphenicol is an antibiotic originally extracted from the fungus Streptomyces venezuelae, but it is now synthesized. It is a drug of choice for many of its toxicity in the blood-forming organs. The main objective of this study is to find out how to reduce the anemic effects of chloramphenicol and to increase its therapeutic efficacy using amino acid. In albino-rats infected with Salmonella typhi the results indicate that the rats became anemic after treatment with chloramphenicol. They also show that the combined treatment of chloramphenicol with amino acid yielded positive results in the management of anemia caused by chloramphenicol.

The effects of electrical stimulation, adenosine and adenosine-5'-triphosphate (ATP) on mouse rectal muscle.

The effects of electrical field stimulation and of purine compounds, adenosine and adenosine-5'-triphosphate (ATP) were examined on the mouse isolated rectum. Electrical field stimulation induced frequency-dependent contractions of mouse rectal muscles which were potentiated by physostigmine and inhibited by atropine or tetrodotoxin. Contractile amplitude at 37 degrees C was significantly (P less than 0.05) greater than at 25 degrees C, but the degree of potentiation by physostigmine was significantly (P less than 0.05) greater at 25 degrees C. ATP (1.6 x 10(-4)-1.28 x 10(-3) M) and adenosine (1.8 x 10(-4)-1.48 x 10(-3) M) inhibited in concentration-related fashion contractile responses induced by KCl (1.34 x 10(-2) M-1.07 x 10(-1) M) by acetylcholine (2.2 x 10(-7) M-1.4 x 10(-5) M) and by CaCl2 in high KCl (120 mM)-CaCl2-free Tyrode solution. Theophylline and quinidine ('purinoceptor' antagonists) antagonized ACH contractile effects and so could not be satisfactorily employed in the characterization of the purine receptors in the mouse rectum. It may be concluded from this study that in the mouse rectum, acetylcholine is an excitatory neurotransmitter and that there is a non-adrenergic, non-cholinergic inhibitory neuromuscular transmission in this tissue. Further, ATP and adenosine have been demonstrated to cause relaxation in this tissue by possibly a post-synaptic mechanism involving inhibition of Ca2+ influx into the depolarized muscle.