Antimalarial herbal drugs: a review of their interactions with conventional antimalarial drugs

AbstractDevelopment of resistance by malaria parasites to conventional antimalarial drugs has rejuvenated the exploration of herbal medicine as alternatives. Also, the increasing rate of the use of herbal antimalarial remedies in combination with conventional antimalarial drugs (both synthetic and semi-synthetic) has inspired researchers to validate their herb-drug interaction effects. This review evaluated the interaction outcomes between herbal antimalarial drugs in combination with conventional antimalarial drugs. With the aid of electronic databases, Pubmed and Google scholar, articles related to this subject were sourced from English peer reviewed scientific journals published from 2003 to 2020. Search terms used include “antimalarial-herbal drugs interaction”, “antimalarial medicinal plant interactions with conventional antimalarial drugs”, “drug-herbal interactions, “antimalarial drugs and medicinal plants”. Synergistic, antagonistic and none effects were reported among 30 studies reviewed. Among 18 in vivo studies on P. berghei and P. yoelii nigerense infected mice model, 14 showed synergism, 3 showed antagonism and 1 involving three plants showed both effects. Among 9 in-vivo studies involving normal animal (non-infected), 2 showed antagonism, 2 showed synergism and 5 showed none-effects. Two (2) studies on human volunteers and one (1) in vitro quantitative study showed that Garcinia kola reduced plasma concentrations of quinine and halofantrine. Generally, majority of herbal antimalarial drugs showed synergistic effects with CAMDs. Vernonia amygdalina was the most studied plant compared to others. Consequently, herbal remedies that produced synergistic effects with conventional antimalarial drugs may be prospects for standardization and development of antimalarial-medicinal plant combination therapy that could curtail malaria resistance to conventional antimalarial therapies.

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Design, Synthesis, Anticonvulsant Activity, Preclinical Study and Pharmacokinetic Performance of N-{[3-(4-chlorophenyl)-4-oxo-3, 4-dihydroquinazolin- 2-yl] methyl}, 2-[(2-isopropyl-5-methyl) 1-cyclo Hexylidene] Hydrazinecarboxamide

Central Nervous System Agents in Medicinal Chemistry ◽

10.2174/1871524919666181122124012 ◽

2019 ◽

Vol 19 (1) ◽

pp. 31-45

Author(s):

Meena K. Yadav ◽

Laxmi Tripathi

Keyword(s):

Anticonvulsant Activity ◽

Computational Study ◽

Plasma Concentrations ◽

Elimination Rate ◽

Area Under The Curve ◽

Preclinical Study ◽

In Vivo Studies ◽

Maximum Plasma ◽

Seizure Models

Background: N-{[3-(4-chlorophenyl)-4-oxo-3, 4-dihydroquinazolin-2-yl] methyl}, 2-[(2- isopropyl-5-methyl) 1-cyclohexylidene] hydrazinecarboxamide QS11 was designed by computational study. It possessed essential pharmacophoric features for anticonvulsant activity and showed good docking with iGluRs (Kainate) glutamate receptor. Methods: QSAR and ADMET screening results suggested that QS11 would possess good potency for anticonvulsant activity. QS11 was synthesised and evaluated for its anticonvulsant activity and neurotoxicity. QS11 showed protection in strychnine, thiosemicarbazide, 4-aminopyridine and scPTZ induced seizure models and MES seizure model. QS11 showed higher ED50, TD50 and PI values as compared to the standard drugs in both MES and scPTZ screen. A high safety profile (HD50/ED50 values) was noted and hypnosis, analgesia, and anaesthesia were only observed at higher doses. No considerable increase or decrease in the concentration of liver enzymes was observed. Optimized QS11 was subjected to preclinical (in-vivo) studies and the pharmacokinetic performance of the sample was investigated. The result revealed that the pharmacokinetic performance of QS11 achieved maximum plasma concentrations (Cmax) of 0.315 ± 0.011 µg/mL at Tmax of 2.0 ± 0.13 h, area under the curve (AUC0-∞) value 4.591 ± 0.163 µg/ml x h, elimination half-life (T1/2) 6.28 ± 0.71 h and elimination rate constant was found 0.110 ± 0.013 h-1. Results and Conclusion: Above evidences indicate that QS11 could serve as a lead for development of new antiepileptic drugs.

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Characterization of Weissella viridescens UCO-SMC3 as a Potential Probiotic for the Skin: Its Beneficial Role in the Pathogenesis of Acne Vulgaris

Microorganisms ◽

10.3390/microorganisms9071486 ◽

2021 ◽

Vol 9 (7) ◽

pp. 1486

Author(s):

Marcela Espinoza-Monje ◽

Jorge Campos ◽

Eduardo Alvarez Villamil ◽

Alonso Jerez ◽

Stefania Dentice Maidana ◽

...

Keyword(s):

Immune Response ◽

Oral Treatment ◽

Acne Vulgaris ◽

Topical Administration ◽

In Vivo Studies ◽

Mice Model ◽

Cutibacterium Acnes ◽

Snail Helix Aspersa

Previously, we isolated lactic acid bacteria from the slime of the garden snail Helix aspersa Müller and selected Weissella viridescens UCO-SMC3 because of its ability to inhibit in vitro the growth of the skin-associated pathogen Cutibacterium acnes. The present study aimed to characterize the antimicrobial and immunomodulatory properties of W. viridescens UCO-SMC3 and to demonstrate its beneficial effect in the treatment of acne vulgaris. Our in vitro studies showed that the UCO-SMC3 strain resists adverse gastrointestinal conditions, inhibits the growth of clinical isolates of C. acnes, and reduces the adhesion of the pathogen to keratinocytes. Furthermore, in vivo studies in a mice model of C. acnes infection demonstrated that W. viridescens UCO-SMC3 beneficially modulates the immune response against the skin pathogen. Both the oral and topical administration of the UCO-SCM3 strain was capable of reducing the replication of C. acnes in skin lesions and beneficially modulating the inflammatory response. Of note, orally administered W. viridescens UCO-SMC3 induced more remarkable changes in the immune response to C. acnes than the topical treatment. However, the topical administration of W. viridescens UCO-SMC3 was more efficient than the oral treatment to reduce pathogen bacterial loads in the skin, and effects probably related to its ability to inhibit and antagonize the adhesion of C. acnes. Furthermore, a pilot study in acne volunteers demonstrated the capacity of a facial cream containing the UCO-SMC3 strain to reduce acne lesions. The results presented here encourage further mechanistic and clinical investigations to characterize W. viridescens UCO-SMC3 as a probiotic for acne vulgaris treatment.

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Plasmodium vivax and Drug Resistance

10.5772/intechopen.97320 ◽

2021 ◽

Author(s):

Puji Budi Setia Asih ◽

Din Syafruddin

Keyword(s):

Drug Resistance ◽

Molecular Basis ◽

Indirect Evidence ◽

Antimalarial Drugs ◽

In Vivo Studies ◽

In Vitro Cultivation ◽

Radical Cure ◽

The Status

Resistance to antimalarial drugs is a threat to global efforts to eliminate malaria by 2030. Currently, treatment for vivax malaria uses chloroquine or ACT for uncomplicated P. vivax whereas primaquine is given to eliminate latent liver stage infections (a method known as radical cure). Studies on P. vivax resistance to antimalarials and the molecular basis of resistance lags far behind the P. falciparum as in vitro cultivation of the P. vivax has not yet been established. Therefore, data on the P. vivax resistance to any antimalarial drugs are generated through in vivo studies or through monitoring of antimalarial treatments in mixed species infection. Indirect evidence through drug selective pressure on the parasites genome, as evidenced by the presence of the molecular marker(s) for drug resistance in areas where P. falciparum and P. vivax are distributed in sympatry may reflect, although require validation, the status of P. vivax resistance. This review focuses on the currently available data that may represent the state-of-the art of the P. vivax resistance status to antimalarial to anticipate the challenge for malaria elimination by 2030.

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Renal localization and actions of adrenomedullin: a natriuretic peptide

AJP Renal Physiology ◽

10.1152/ajprenal.1995.268.4.f657 ◽

1995 ◽

Vol 268 (4) ◽

pp. F657-F663 ◽

Cited By ~ 22

Author(s):

M. Jougasaki ◽

C. M. Wei ◽

L. L. Aarhus ◽

D. M. Heublein ◽

S. M. Sandberg ◽

...

Keyword(s):

Natriuretic Peptide ◽

Sodium Excretion ◽

Collecting Duct ◽

Plasma Concentrations ◽

In Vivo Studies ◽

Sodium Reabsorption ◽

Contralateral Kidney ◽

Arterial Blood ◽

Group I

Adrenomedullin (ADM) is a newly described 52-amino acid peptide originally isolated from extracts of human pheochromocytoma and, more recently, detected in human plasma. Based on the report that ADM mRNA and immunoreactivity are present in the kidney, the current study was designed to determine the renal distribution of ADM by immunohistochemistry and the renal biological actions of ADM. In the immunohistochemical studies, the present investigation demonstrated the localization of ADM in glomeruli, cortical distal tubules, and medullary collecting duct cells of the normal canine kidney. In the in vivo studies, ADM was administered (0.25 ng.kg-1.min-1 in group I and 1, 5, and 25 ng.kg-1.min-1 in group II) intrarenally in normal mongrel dogs with the contralateral kidney receiving only saline vehicle. Intrarenal infusion of ADM resulted in a marked diuretic and natriuretic response, whereas the contralateral kidney showed no renal effects. These significant natriuresis and diuresis in the ADM kidney were associated with increases in glomerular filtration rate and fractional sodium excretion and with a decrease in distal tubular sodium reabsorption. Intrarenal infusion of ADM also caused an increase in mean arterial blood pressure and a decrease in heart rate. Plasma concentrations of atrial natriuretic peptide, renin activity, aldosterone, and guanosine 3',5'-cyclic monophosphate were not changed during the infusion of ADM. The current study demonstrates that ADM is present in renal glomerular and tubular cells and is a potent natriuretic peptide that may play an important role in the regulation of sodium excretion.

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Nutraceutical Activity in Osteoarthritis Biology: A Focus on the Nutrigenomic Role

Cells ◽

10.3390/cells9051232 ◽

2020 ◽

Vol 9 (5) ◽

pp. 1232

Author(s):

Stefania D’Adamo ◽

Silvia Cetrullo ◽

Veronica Panichi ◽

Erminia Mariani ◽

Flavio Flamigni ◽

...

Keyword(s):

Signaling Pathways ◽

Antioxidant Activities ◽

Synergistic Effects ◽

National Health System ◽

Bioactive Molecules ◽

Joint Disease ◽

In Vivo Studies ◽

Wide Range

Osteoarthritis (OA) is a disease associated to age or conditions that precipitate aging of articular cartilage, a post-mitotic tissue that remains functional until the failure of major homeostatic mechanisms. OA severely impacts the national health system costs and patients’ quality of life because of pain and disability. It is a whole-joint disease sustained by inflammatory and oxidative signaling pathways and marked epigenetic changes responsible for catabolism of the cartilage extracellular matrix. OA usually progresses until its severity requires joint arthroplasty. To delay this progression and to improve symptoms, a wide range of naturally derived compounds have been proposed and are summarized in this review. Preclinical in vitro and in vivo studies have provided proof of principle that many of these nutraceuticals are able to exert pleiotropic and synergistic effects and effectively counteract OA pathogenesis by exerting both anti-inflammatory and antioxidant activities and by tuning major OA-related signaling pathways. The latter are the basis for the nutrigenomic role played by some of these compounds, given the marked changes in the transcriptome, miRNome, and methylome. Ongoing and future clinical trials will hopefully confirm the disease-modifying ability of these bioactive molecules in OA patients.

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The Comparative Analysis of Antiviral Activity of Native and Modified Fucoidans from Brown Algae Fucus evanescens In Vitro and In Vivo

Marine Drugs ◽

10.3390/md18040224 ◽

2020 ◽

Vol 18 (4) ◽

pp. 224 ◽

Cited By ~ 8

Author(s):

Natalya V. Krylova ◽

Svetlana P. Ermakova ◽

Vyacheslav F. Lavrov ◽

Irina A. Leneva ◽

Galina G. Kompanets ◽

...

Keyword(s):

Antiviral Activity ◽

Brown Algae ◽

Biological Activities ◽

Intraperitoneal Administration ◽

In Vivo Studies ◽

Mice Model ◽

Dna And Rna ◽

Antiviral Activities

The enzymatic depolymerization of fucoidans from brown algae allowed the production of their standardized derivatives with different biological activities. This work aimed to compare the antiviral activities of native (FeF) and modified with enzyme (FeHMP) fucoidans from F. evanescens. The cytotoxicity and antiviral activities of the FeF and FeHMP against herpes viruses (HSV-1, HSV-2), enterovirus (ECHO-1), and human immunodeficiency virus (HIV-1) in Vero and human MT-4 cell lines were examined by methylthiazolyltetrazolium bromide (MTT) and cytopathic effect (CPE) reduction assays, respectively. The efficacy of fucoidans in vivo was evaluated in the outbred mice model of vaginitis caused by HSV-2. We have shown that both FeF and FeHMP significantly inhibited virus-induced CPE in vitro and were more effective against HSV. FeF exhibited antiviral activity against HSV-2 with a selective index (SI) > 40, and FeHMP with SI ˃ 20, when they were added before virus infection or at the early stages of the HSV-2 lifecycle. Furthermore, in vivo studies showed that after intraperitoneal administration (10 mg/kg), both FeF and FeHMP protected mice from lethal intravaginal HSV-2 infection to approximately the same degree (44–56%). Thus, FeF and FeHMP have comparable potency against several DNA and RNA viruses, allowing us to consider the studied fucoidans as promising broad-spectrum antivirals.

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Comparison of the synergistic effects of tamsulosin versus phentolamine on penile erection: in vitro and in vivo studies

Urological Research ◽

10.1007/s002400050133 ◽

1999 ◽

Vol 27 (6) ◽

pp. 437-444 ◽

Cited By ~ 1

Author(s):

S. C. Kim ◽

K. K. Seo ◽

S. K. Lee ◽

E. S. Song ◽

M. Y. Lee

Keyword(s):

Penile Erection ◽

Synergistic Effects ◽

In Vivo Studies

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Low Intensity Pulsed Ultrasound for Bone Tissue Engineering

Micromachines ◽

10.3390/mi12121488 ◽

2021 ◽

Vol 12 (12) ◽

pp. 1488

Author(s):

Colleen McCarthy ◽

Gulden Camci-Unal

Keyword(s):

Bone Formation ◽

Bone Tissue ◽

Mechanical Stimulation ◽

Synergistic Effects ◽

In Vivo Studies ◽

Pulsed Ultrasound ◽

Low Intensity Pulsed Ultrasound ◽

Low Intensity

As explained by Wolff’s law and the mechanostat hypothesis, mechanical stimulation can be used to promote bone formation. Low intensity pulsed ultrasound (LIPUS) is a source of mechanical stimulation that can activate the integrin/phosphatidylinositol 3-OH kinase/Akt pathway and upregulate osteogenic proteins through the production of cyclooxygenase-2 (COX-2) and prostaglandin E2 (PGE2). This paper analyzes the results of in vitro and in vivo studies that have evaluated the effects of LIPUS on cell behavior within three-dimensional (3D) titanium, ceramic, and hydrogel scaffolds. We focus specifically on cell morphology and attachment, cell proliferation and viability, osteogenic differentiation, mineralization, bone volume, and osseointegration. As shown by upregulated levels of alkaline phosphatase and osteocalcin, increased mineral deposition, improved cell ingrowth, greater scaffold pore occupancy by bone tissue, and superior vascularization, LIPUS generally has a positive effect and promotes bone formation within engineered scaffolds. Additionally, LIPUS can have synergistic effects by producing the piezoelectric effect and enhancing the benefits of 3D hydrogel encapsulation, growth factor delivery, and scaffold modification. Additional research should be conducted to optimize the ultrasound parameters and evaluate the effects of LIPUS with other types of scaffold materials and cell types.

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In vivo antimalarial activity of crude fruit extract of Capsicum frutescens var. minima (Solanaceae) against Plasmodium berghei infected mice

10.21203/rs.3.rs-33601/v1 ◽

2020 ◽

Cited By ~ 1

Author(s):

Getu Habte ◽

Solomon Assefa

Keyword(s):

Survival Time ◽

Antimalarial Activity ◽

Antimalarial Drugs ◽

Negative Control ◽

Antiplasmodial Activity ◽

Capsicum Frutescens ◽

Mice Model ◽

Fruit Extract ◽

Dose Levels

Abstract Background: The alarming spread of drug resistance to current antimalarial agents is threatening malaria controlling efforts. This, consequently, urged the scientific community to discover novel antimalarial drugs. Successful and most potent antimalarial drugs were obtained from medicinal plants. Capsicum frutescens is claimed to possess an antiplasmodial activity in Ethiopian and Ugandan folkloric medicine. However, there is lack of pharmacological evidence for its antiplasmodial activity. This study, hence, was aimed at evaluating the in vivo antiplasmodial activity of C. frutescens in mice model. Methods: The 4-day suppressive test was employed to ascertain the claimed antiplasmodial effect of the plant. Following inoculation with P. berghei , mice in treatment groups were provided with three dose levels (100, 200 and 400 mg/kg) of the extract. Whereas, 2% Tween80 and chloroquine served as negative and positive control, respectively. Weight, temperature, packed cell volume, parasitemia and survival time were then monitored.Results: The oral acute toxicity study revealed that the crude extract caused no mortality and revealed no overt sign of toxicity. In 4-day suppressive test, all dose levels of the extract was found to exhibit a significant (p<0.05) inhibition of parasitemia compared to negative control. Maximum parasite suppression (93.28%) was exerted by the highest dose (400mg/kg/day) of extract. In addition, the extract significantly (p<0.05) prolonged survival time and prevented body weight loss, reduction in temperature and anemia compared to vehicle treated group.Conclusion: This investigation found a strong evidence that fruit extract of C. frutescens is endowed with a promising antiplasmodial activity. Hence, the plant could serve as a potential source of newer antimalarial agent.

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NATURAL PRODUCTS WITH ANTI-HERPES ACTIVITIES: IN VIVO STUDIES

International Journal of Advanced Research ◽

10.21474/ijar01/13879 ◽

2021 ◽

Vol 9 (12) ◽

pp. 79-90

Author(s):

Hala Sabry Al-Atbi ◽

◽

Asmaa B. Sabti ◽

Sahar A. Ali ◽

◽

...

Keyword(s):

Natural Products ◽

Herpes Simplex ◽

Marine Species ◽

Herbal Remedies ◽

In Vivo Studies ◽

Term Basis ◽

Simplex Virus ◽

Antiviral Medications

Herpes are a group of similar viruses that are responsible for a number of infecting diseases, the most important of which are herpes simplex, herpes zoster and pseudopox. Resistance to traditional antiviral medications is becoming increasingly common, making treatment of such infections even more difficult. For example, the usage of nucleoside analogues like acyclovir to target the DNA-polymerase of the virus on a regular and long-term basis promotes the generation of resistant viruses. As a result, a different treatment is required. Natural products, such as herbal remedies, have been shown to have in vitro and in vivo activity against herpes viruses, and have shown to be a valuable source for new antivirals development and separation. The goal of this review is to highlight the most promising extracts and pure chemicals obtained from plants and marine species that have in vivo anti-herpes simplex virus (HSV-1 and HSV-2) action. Natural products as new anti-HSV medications offer a number of benefits, including fewer side effects, minimal toxicity, and lowered resistance, and a variety ways of deed.

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