Recent patents on anti-infective drug discovery最新文献

Background: The global outbreak of COVID-19 incepted in Wuhan, China in the late 2019. It is still unclear about the origin of the infection. Over time, it has migrated geographically to 150 countries in the world and World Health Organization (WHO) has declared the infectious disease to be pandemic.

Objective: Recently, COVID-19 has stepped into India by the travellers from other countries. The transmissibility and epidemicity of COVID-19 in India is exponential. So, in-order to understand the above characteristics, specifically COVID-19 status in India is analyzed. To analyze this into deeper, the state of Kerala is selected. The epidemiological characteristics of patients in Kerala, South India and the possible transmission of COVID-19 from asymptomatic members to other peers are shown using certain cases.

Methods: The COVID-19 dataset is taken from Kaggle dataset. This dataset contains the details of the infected patients from different states of India. Statistical analysis techniques where used to analyze the distribution of the affected cases in a particular state.

Results: The analysis shows that there is possibility of transmission of the infection even during incubation period. The recent trend in the number of infected cases in India is discussed.

Conclusion: The transmissibility of COVID-19 and its epidemicity in India is discussed. In specific, a case study on COVID -19 cases in the state of Kerala relating the transmissibility is also summarized. Further, data related to patents on corona virus is also discussed. From the analysis, it can be concluded that there is a possibility of COVID-19 transmission even during incubation period. The preventive measures to overcome COVID-19 and methods to increase the immunity are discussed.

Background: Malaria is a deadly disease. It is mostly treated using 4- aminoquinoline derivatives such as chloroquine etc. because it is well-tolerated, displays low toxicity, and after administration, it is rapidly absorbed. The combination of 4-aminoquinoline with other classes of antimalarial drugs has been reported to be an effective approach for the treatment of malaria. Furthermore, some patents reported hybrids 4-aminoquinolines containing ferrocene moiety with potent antimalarial activity.

Objective: The objective of the current study is to prepare 4-aminoquinoline-ferrocene hybrids via esterification and amidation reactions. The compounds were characterized via FTIR, LC-MS and NMR spectroscopy. In vitro screening against chloroquine-sensitive P. falciparum parasite (NF54) at concentrations (1 μM and 5 μM) and an inhibitory concentration (full dose-response) was studied.

Methods: The compounds were prepared via known reactions and monitored by Thin Layer Chromatography. The compounds were purified by column chromatography and characterized using FTIR, NMR and MS. In vitro antiplasmodial evaluation was performed against asexual parasite and chloroquine was used as a reference drug.

Results: The percentage inhibition effects of the hybrid compounds were in a range of 97.9-102% at 5 μM and 36-96% at 1 μM. Furthermore, the IC50 values of the compounds were in the range of 0.7-1.6 μM when compared to the parent drug, 4-ferrocenylketobutanoic acid.

Conclusion: The hybrid compounds displayed significant antimalarial activity when compared to the parent drug. However, they were not as effective as chloroquine on the drug-sensitive parasite. The findings revealed that 4-aminoquinolines and ferrocene are potential scaffolds for developing potent antimalarials.

Aim: To design controlled release topical delivery of mupirocin for the treatment of skin infection.

Background: Mupirocin is an antibacterial drug. Mupirocin works to kill the bacteria, which include strains of Staphylococcus aureus and Streptococcus pyogenes. It is also used for the treatment of inflammation of a hair follicle. The half-life of mupirocin is only 20-40 min. It has very slight solubility in water. Patent literature had shown work on ointment, antibiotic composition, nasal and topical composition. Emulgel is a duel control release system for the topical delivery of hydrophobic drugs.

Objective: The objective was to formulate emulgel with controlled delivery of mupirocin using Sepineo P 600.

Methods: Soya oil, tween 80 and polyethylene glycol 400 (Oil:Surfactant:Cosurfactant) were used for emulsion formulation. Emulgel was optimized by 32 factorial design. Sepineo P 600 and hydroxy propyl methyl cellulose K4M were used as independent variables. Drug excipient compatibility analysis was carried out by FTIR, UV and DSC spectra. Emulgel was evaluated for its physical characterization, in vitro release, ex vivo release, antimicrobial and anti-inflammatory study.

Results: DSC, UV and FTIR analysis confirmed drug excipient compatibility. FE SEM showed a size range between 228-255 nm. Zeta potential was found to be -25.1 mV, which showed good stability of the emulsion. Design expert software showed F2 as an optimized batch. Release studies indicated that the controlled release of drugs forms Sepineo P 600 gel due to its higher gelling capacity. Batch F2 showed comparable results with marketed formulation against Staphylococcus aureus. For batch F2, 40 μg/ml was the minimal inhibitory concentration.

Conclusion: Antimicrobial and anti-inflammatory study proved successful development of stably controlled release mupirocin emulgel.

To date, severe acute respiratory syndrome coronavirus 2 (SARSCoV- 2) has infected millions of individuals worldwide. This virus causes coronavirus disease 2019 (COVID-19) and has led to numerous deaths worldwide. A large percentage of infected patients present asymptomatically, augmenting the spread of the virus. Symptomatic COVID-19 commonly causes mild to severe respiratory disease and fever, but some individuals experience serious complications resulting in death. Immune compromised, high risk, and elderly individuals are at an increased risk of more severe consequences of the illness such as respiratory failure, organ dysfunction, and shock. Cytokine storm (also known as cytokine release syndrome (CRS)), a systemic inflammatory response that can be triggered by an infection, has been associated with the symptom progression of COVID-19. This review evaluates several published studies that have implemented tocilizumab (TCZ), an IL-6 receptor antibody (US20120253016A1), in COVID-19 treatment. Outcomes and biomarkers of patients treated with TCZ are compared to patients treated with standard of care regimens. Interleukin-6 (IL-6), a prominent inflammatory cytokine involved in CRS in various inflammatory conditions, may have a vital role in the underlying mechanism involved in debilitating SARS-CoV-2 infections and could serve as a viable treatment target. Studies suggest that TCZ may aid in the recovery of patients with COVID-19 and reduce mortality.

Background: Acne is an infection of the skin that occurs in both men and women during their lifespan. There are various natural or synthetic products available in the market to prevent and cure this disease.

Introduction: The majority of the world population depends on the herbs or natural resources for the relief of acne disease. These are used to lessen the cost of treatment and the side effects of synthetic analogs.

Methods: We have explored the various authentic web resources to compile information regarding different patented and marketed herbal formulations for acne treatment.

Results: It has been found that most of the herbal formulation for acne include the plant actives/extracts having the potential activity against the Propionibacterium acne. The occurrence of this skin disease is also associated with the presence of free radicals in the body, which also causes the inflammation and redness of the skin. Further, the study of various patents also revealed that herbs with anti-oxidant properties have been used in most of the herbal anti-acne formulations. Moreover, the various patents also give the idea that herbal formulations also prevent the appearance of pimples on the skin.

Conclusion: It has been concluded that the herbal anti-acne formulation is not only used to treat acne but also prevents this disease safely and economically.

Background: Studies showed that biogenic selenium nanoparticles (SeNPs) have a number of pharmacological properties, such as antimicrobial ones.

Objective: The present investigation assesses the efficacy of biogenic selenium nanoparticles (SeNPs) as a new patent against latent toxoplasmosis in a mice model.

Methods: Male BALB/c mice were orally treated with SeNPs at the doses of 2.5, 5, 10 mg/kg once a day for 14 days. On the 15th day, the mice were infected with the intraperitoneal inoculation of 20-25 tissue cysts from the Tehran strain of Toxoplasma gondii. The mean numbers of brain tissue cysts and the mRNA levels of TNF-α, IL-12, IL-10, IFN-γ, and inducible nitric oxide synthase (iNOS) in mice of each tested group were measured. Moreover, serum clinical chemistry factors in treated mice were examined to determine the safety of SeNPs.

Results: The mean number of the brain tissue cysts was significantly (P<0.001) decreased in mice treated with SeNPs at doses 2.5 (n=37), 5 (n=11), and 10 mg/kg (n=3) based on a dose dependent manner compared with the control group (n=587). The mRNA levels of IFN-γ, TNF-α, IL-12, and iNO were significantly increased in mice treated with SeNPs at the doses 10 mg/kg compared with control subgroups (p<0.05). No significant variation (p>0.05) was observed in the clinical chemistry parameters among the mice in the control subgroups compared with groups treated with SeNPs.

Conclusion: The results of the present study showed a new patent in the treatment of toxoplasmosis; so that taking the biogenic selenium nanoparticles in concentrations of 2.5-10 mg/kg for 2 weeks was able to prevent severe symptoms of the toxoplasmosis in a mice model. This indicated the prophylactic effects of SeNPs with no considerable toxicity against latent toxoplasmosis. However, more studies are required to elucidate the correct anti-Toxoplasma mechanisms of SeNPs.

Coronavirus disease is a potentially deadly disease and of significant apprehension for global communal health because of its lethality. Vaccines and antiviral medications are still under trial to prevent or treat human coronavirus (HCoV) till date. The virus HCoV originated in 2003, SARS-CoV, which causes respiratory syndrome having distinctive pathogenesis and infections of the respiratory tract. A mechanism was projected for the evolution of SARS virus, and a handy association with bats was found. When this virus reaches the respective host system, the infection starts with spike protein binding to its complementary receptor of the host cell. The coronavirus spike protein's association with its host cell receptor complement is crucial in deciding the virus infectivity, tissue tropism and species variety. Recent studies show that SARS Coronavirus 2 or COVID-19 requires protease to get into cells, offering a new therapeutic target. Distinctive attention and exertions should be given to defending or reducing transmission in vulnerable populaces, including those directly associated with caregiving and treatment and also aged one. Researchers are planning to develop a vaccine for COVID-19, and in this approach are also considered developing a vaccine that sensitizes our immune system preventing from this pandemic. The present review focuses on the role of S-spike protein in COVID-19, which helps the virus intruding the enzyme ACE2 (Angiotensin-Converting Enzyme 2). Passive antibody therapy is an additional alternative to use blood donors from hale and hearty people who have already recovered from COVID-19 and therapeutic advancement in handling the COVID-19 pandemic.

Background: On 11th March 2020, WHO announced novel coronavirus infectious (COVID-19) as a pandemic. New Coronavirus Pneumonia (NCP) that emerge on 31st December 2019 from China and quickly became a Public Health Emergency of International Concern (PHEIC). In the absence of evidence-based proven prophylactic or therapeutic options, chloroquine/hydroxychloroquine (CQ/HCQ) patented as first line choice in COVID- 19 treatment, which raised concerns about drug poisoning, especially ocular toxicity.

Objective: This study aims to investigate the possibility of ocular toxicity and the need for ophthalmic counseling to prescribing this therapeutic protocol.

Methods: All the articles that were most relevant to the COVID-19 therapeutic or prophylactic options and CQ derivative ocular toxicity, were founded by a literature search and were thoroughly reviewed.

Results: Anecdotal recent reports introduce CQ/HCQ as an effective therapeutic or prophylactic choice for COVID-19. Because of the short time prescribe and the insignificant cumulative dose of the drug on the one hand and a higher risk of cross-infection during an ophthalmic examination, on the other hand, an ophthalmologic consult is not recommended except in highrisk patients for retinal toxicity.

Conclusion: This study recommended ophthalmic evaluation before CQ/HCQ prescription for treatment or prophylaxis of COVID-19 only in preexisting maculopathy.

Background: Acne vulgaris a chronic disease which is caused by blockage of the sebaceous gland is commonly seen in almost every human being at some point in their lives. There are 20-25% chances of progression of acne to severe cases, which leads to permanent scarring that results in psychological problems like depression, social isolation, lowered self-esteem, and lowered self-confidence.

Objective: Though several conventional treatments are available in the market but still there are various adverse effects associated with topical anti-acne agents due to which it lacks patient compatibility. The present study is undertaken to find out the major shortcoming; why the current therapies do not give the desired therapeutic results.

Conclusion: Novel drug delivery strategies can play a crucial role in the enhancement of topical delivery of anti-acne agents by escalating their dermal localization and reducing their adverse effects. Consumption of medicinal plants like Aloe vera, Withania somniferia etc. have clinical evidence regarding the effective management of acne. The current inclination towards nanotechnology is considerable due to several changes in the pharmaceutical research area. To secure the research work in different pharmaceutical fields, patents are filed against various agents like Galderma Research & Development have filed patents for adapalene and benzoyl peroxide for the management of acne vulgaris. The current review highlights the potential of various novel drug delivery approaches like liposomes, niosomes, ethosomes, transfersomes etc. in enhancing the topical delivery of anti-acne agents.

Introduction: Antibiotic resistance and extensive use of antibiotics are amongst the major causes of failure in antibiotic treatment. The purpose of this study was to investigate antibiotic resistance patterns and to identify resistance genes of quinolones and colistin in Escherichia coli. There are a very few patents on E. coli isolated from colorectal cancer. So, this study demonstrates that some bacteria resistant to ciprofloxacin have not resistance genes.Moreover, new patterns for E. coli are presented for isolates of patients with colorectal cancer.

Materials and methods: Of the three healthy people, inflammatory bowel diseases (IBD) patients and colorectal cancer patients, 40 E. coli strains isolated after confirmation by biochemical and molecular methods. The susceptibility of isolates to antibiotics was investigated using disk diffusion test. After deoxyribonucleic acid (DNA) extraction, polymerase chain reaction (PCR) was used to identify genes encoding resistance to ciprofloxacin (qnr A, qnr B) and colistin (mcr-1).

Results: The results showed that E. coli isolates from colorectal cancer patients had the highest resistance to piperacillin (67.5%), ceftazidime (47.5%), and cefepime (42.5%). Also, E. coli strains isolated from IBD patients showed resistance to antibiotic ceftazidime 13%. More than 95% of E. coli strains isolated from healthy people were susceptible to antibiotics. Based on the results, 18 (15%) E. coli strains showed resistance to ciprofloxacin. The qnr A gene was detected in 61.11% isolates; however, qnr B was detected in 9 (50%) isolates. Isolates resistant to colistin were not observed.

Conclusion: These findings indicate increased resistance of E. coli to ciprofloxacin in comparison with prior studies. Further research in this field will increase our knowledge and more effective exposure to the antibiotic resistance of the pathogenic microorganisms.