21 results on '"Islam, Arshad"'
Search Results
2. Novel coumarin-isatin hybrids as potent antileishmanial agents: Synthesis, in silico and in vitro evaluations
- Author
-
Khatoon, Saira, Aroosh, Aiman, Islam, Arshad, Kalsoom, Saima, Ahmad, Faisal, Hameed, Shahid, Abbasi, Sumra Wajid, Yasinzai, Masoom, and Naseer, Muhammad Moazzam
- Published
- 2021
- Full Text
- View/download PDF
3. Comprehensive investigation on the synergistic antibacterial activities of Jatropha curcas pressed cake and seed oil in combination with antibiotics
- Author
-
Haq, Abdul, Siddiqi, Maleeha, Batool, Syeda Zakia, Islam, Arshad, Khan, Alam, Khan, Dildar, Khan, Samiullah, Khan, Haji, Shah, Aamer Ali, Hasan, Fariha, Ahmed, Safia, and Badshah, Malik
- Published
- 2019
- Full Text
- View/download PDF
4. NORMS OF RISE AND FALL OF CIVILIZATIONS IN THE QUR'AN: Beneficial Knowledge and Justice as a Model.
- Author
-
Islam, Arshad and Al-Alwani, Ruqaia Taha
- Subjects
CIVILIZATION ,MODERN society ,STORYTELLING ,JIHAD - Abstract
This paper deals with some of the norms of the establishment and emergence of civilizations according to the Qur'an and analyses the components of such norms. The Qur'an gives explicit attention to the laws and norms on which human societies and civilizations are based, directly and indirectly, by telling the stories of peoples in past eras. The Qur'an also emphasizes that giving priority to the pursuit of material aspects and elements of societies while neglecting their religious and moral aspects is a reason for the decline and collapse of civilizations, as was the case with the people of Sheba. This paper clarifies that the most important norms of the establishment of civilizations include focusing attention on beneficial knowledge and instilling the value of justice in society. The study explores some conditions of previous nations that vanished owing to the absence of these two basic elements, as mentioned in the Qur'an. In conclusion, this article argues for further studies of the Quranic approach to the issue of the rise and fall of human civilizations. Contemporary societies need to be enlightened by the Quranic perspectives on the issue in the light of the present human condition. [ABSTRACT FROM AUTHOR]
- Published
- 2023
5. New Paradigm in Addressing Islamophobia: An Analytical Study Based on the Life of the Prophet Muhammad (PBUH).
- Author
-
Alalwani, Ruqaia Taha and Islam, Arshad
- Subjects
- *
ISLAMOPHOBIA , *RACISM , *STEREOTYPES , *HUMANITY - Abstract
A vast number of studies have acknowledged the existence of Islamophobia, but few have attempted to deconstruct the concept. This study deconstructs Islamophobia into its constituent elements: hatred, hostility, and racism against Islam and Muslims. The study seeks to shed light on some methods applied by Prophet Muhammad (PBUH) in dealing with the roots of hatred, racism, and stereotypes. This can lead members of society to practice different forms of animosity between people based on religion, race, color, etc. In this context, the study confirms the depth of the prophetic biography and its ability to provide the modern world with systematic methods in dealing with its growing problems and challenges. Based on this biography, the study proposes solutions to the matter of Islamophobia, including the need for Muslims to interact with the regional and international societies from a standpoint of collaboration and engagement. This would be for the universal benefit of all societies and humanity in general. [ABSTRACT FROM AUTHOR]
- Published
- 2021
6. The Effects of Japanese Occupation in Sabah: During and After World War II (1941-1963).
- Author
-
Yacho, Rosdianah Binti and Islam, Arshad
- Subjects
- *
HEGEMONY , *DECOLONIZATION - Abstract
The Japanese were the only colonial power that challenged British hegemony in Sabah, then known as “North Borneo”. In 1941 they attacked and defeated the British North Borneo Company (BNBC) and assumed governance of the land for the remainder of the war. Although their presence was temporary, it was enough to fundamentally alter the course of the history of Sabah. This paper explores the effects of the Japanese occupation during the years 1942 to 1963, concentrating on economic, political, and social progress. This includes two distinctive periods: the invasion and occupation (1942-1945) and over the longer term, including both positive and negative effects for local peoples. This study is important to understand the reasons for the transition of Sabah from a British Protectorate to a Crown Colony, set against its role in the framework of the Japanese “Greater East Asia Co-Prosperity Sphere”. Studies of the history of Sabah in general are lacking, particularly concerning the important years of British colonialism, the Japanese occupation, and the decolonization period. This study draws on archival and library resources to find that the Japanese occupation brought problems to certain parties and fields, alongside some tangible benefits for some groups. It is hoped that this study will open up historical understanding and investigation of the significance of Japanese influence in Sabah. [ABSTRACT FROM AUTHOR]
- Published
- 2020
7. Charismatic Political Leadership and Tun Dr Mahathir Mohamad's Malaysia: Power, Control, Stability and Defence.
- Author
-
Temiz, Suleyman and Islam, Arshad
- Subjects
- *
DEMOCRACY , *LEADERSHIP , *PRIME ministers - Abstract
Prior to his renewed incumbency, as the fourth Prime Minister of Malaysia, Mahathir Mohamad (b. 1925) was able to remain in power for a more prolonged period compared to his predecessors. He was actively involved in galvanizing political action immediately after the independence of Malaysia and did not abandon active politics until his 2003 resignation. Under Mahathir's leadership and guidance, Malaysia made remarkable economic and political progress. He oversaw many innovations in the fledgling democracy and was able to develop the country due to his exceptional leadership qualities. His style and attitude towards engaging with problems, particularly his stance during the Asian Monetary Crisis in 1997, was highly criticized by some, and labelled as dictatorial. This stigma did not detract him from the path he considered right for Malaysia, and under his leadership he garnered worldwide appreciation for his national efforts and success in overcoming the economic crisis. Mahathir is undeniably an excellent case study as a prime minister, as well as a highly productive person. He contributed to a better understanding of modern Malaysia and his own tenure as PM in a series of books and articles. One of the significant aspects of his political heritage is his influential charisma and leadership. In all of his undertakings he has attracted both passionate support and hatred from friends and foes, but his political footsteps have always been certain and directed toward Malaysia's national wellbeing. Mahathir is a politician with sharp views on many issues and he was profoundly brave in verbalising them in the public arena, within Malaysia and internationally. His clear posture and speeches without fear made him a world-embracing political personality. This descriptive research study adopts a qualitative approach to analyse historical information, documents, memoirs and articles, and books to better understand the leadership of Mahathir. [ABSTRACT FROM AUTHOR]
- Published
- 2019
8. Indian Muslims' Support for Ottoman Pan-Islamism: The Case of Shibli Nu'mani.
- Author
-
Islam, Arshad
- Subjects
- *
PANISLAMISM , *OTTOMAN Empire , *JIHAD , *POLITICAL participation of Muslims , *IMPERIALISM - Abstract
Following their violent suppression of the Indian Revolution of 1857, the British founded and consolidated their secular empire in the Indian Subcontinent, which marginalized and bypassed religion as far as possible, particularly Islam, which had been the official religion of the Mughal ancien régime. Contemporaneous Ottoman efforts to counter European imperialism led to Sultan Abdul Hamid II's (r. 1876-1909) policy of pan-Islamism, particularly the call for Islamic unity against the Russian aggression against Turkey in 1877. It was at this critical juncture that some Indian Muslim scholars gallantly volunteered to counter this threat, and to preserve the Islamic faith and heritage worldwide, despite the severe problems faced by the Muslims in India itself. This study highlights the role of an eminent scholar in this movement, namely Allama Shibli Nu'mani (1857-1914), who in 1914 conceived the idea of founding the world-famous Islamic research institute Darul Musannefin Shibli Academy in his home town of Azamgarh, Uttar Pradesh, India. Shibli was very active and instrumental in collecting donations from the wealthy landowners (zamindars) among the Muslim elite in his hometown of Azamgarh for the Ottoman cause, raising 3,000 rupees, which was handed to Husain Hasib Afendi, the Ottoman Consul in Bombay in 1877. Furthermore, his eloquent poetry rallied Muslims across India to support the valour and heroism displayed in the jihad by Ghazi Usman Pasha against the Russians. Shibli travelled to Istanbul in 1892 and met with the Pasha, on whose efforts Tamgha-i Majidi (gold medal) was granted to Shibli on 13th Muharram, 1310/7th August, 1892. This article is based on Shibli's major works in Urdu, particularly his arousing eulogies (qasaid), Turkish archival reports, newspapers and magazines, and secondary sources in Urdu and English. [ABSTRACT FROM AUTHOR]
- Published
- 2019
9. Injection Modeling and Shear Failure Predictions in Tight Gas Sands — A Coupled Geomechanical Simulation Approach
- Author
-
Islam, Arshad
- Subjects
Technology & Engineering / Hydraulics - Abstract
Injection Modeling and Shear Failure Predictions in Tight Gas Sands — A Coupled Geomechanical Simulation Approach
- Published
- 2013
10. Turkish Waqf After the 2004Aceh Tsunami.
- Author
-
Tekin, Alaeddin and Islam, Arshad
- Subjects
- *
WAQF , *TSUNAMIS , *MOSQUES , *INTERNATIONAL relief , *RELIGION - Abstract
This paper studies waqf projects including schools, mosques, orphanages and housing built by Turkish aid agencies in Aceh province of Indonesia after the 2004 Aceh Tsunami following the Indian Ocean Earthquake. Such projects continue to be actively supported and to serve the Acehnese community, playing an important role with local organizations. Besides the Turkish Government, NGOs such as Turkish Foundation Institutions including the Turkish Red Crescent (Kızılay), Deniz Feneri and Humanitarian Relief Foundation (IHH) are the main groups considered in this study. The paper situates Turkish waqf in the long-term history of relations between Turkey and Aceh, dating from the mid-16th century, which was reinvigorated by Turkish solidarity following the 2004 tsunami. Essentially, the fact that there is a serious lack of literature on studies of these institutions and activities and their deeper cultural significance is the main rationale for presenting this work. The main purpose of this study is to examine the foundation and relief works from Turkey to Aceh after the shocking earthquake of 9.1 magnitude, which resulted in 126,741 deaths, 93,285 missing and massive destruction of property and infrastructure on 26th December 2004 in Aceh. [ABSTRACT FROM AUTHOR]
- Published
- 2018
11. Origin and Development of Unani Medicine: An Analytical Study.
- Author
-
Islam, Arshad
- Subjects
- *
AYURVEDIC medicine , *ARAB medicine , *EGYPTIAN medicine , *MEDICAL care , *ISLAMIC civilization - Abstract
This study traces the history of the origin and development of Unani medicine in the Islamic world and its later blossoming in Persia. Based mainly on Arabic, Persian, Urdu and English sources, the study focuses on the intellectual legacy of the Muslims in the development of Unani medicine and their interest in the progress of medical sciences, when a number of classical works were produced by great Muslim scholars during this period that provide evidence of organized medical care that provided the basis for modern medicine as it emerged from the 17th century onwards in Europe. The early Muslim scholars' works were focused on the integration or Islamicisation of human knowledge in the areas of medical and health-care sciences as well as those who seek to understand the role of moral values and Maqaṣid al-Sharīʿah ('objectives of Sharīʿah) in medical and healthcare practices in a more comprehensive framework, exposing the dynamic contribution of Islamic civilization to medical progress that was later obscured in modernity by Western ideologies. [ABSTRACT FROM AUTHOR]
- Published
- 2018
12. A SCATTERED LIFE: THE LIVED EXPERIENCES OF ROHINGYA REFUGEE MOTHERS IN MALAYSIA.
- Author
-
Arshad, Munira and Islam, Arshad
- Subjects
ROHINGYA (Burmese people) ,REFUGEES - Abstract
This phenomenological study explores the lived experience of refugee mothers in Malaysia, specifically Rohingya asylum seekers (the most persecuted Muslim minority from Myanmar), using a qualitative research design. Semi-structured, face-to-face, in-depth interviews were held with 20 Rohingya refugee mothers with the aim of providing rich description of the lived experiences related to mothering among refugee and asylum seeking women in Malaysia, thereby filling a significant gap in the research literature. The mothers shared a range of lived experiences that affected their experiences as mothers, including negotiating an opaque and hostile asylum system, and unemployment leading to poor living conditions. Children's education, well-being, and religion were found to be coping mechanisms that enabled them to feel comforted. As the experiences of these mothers were threatening, they were inhibited from giving the best to their children, yet some of the mothers developed a sense of resilience in dealing with their situation. The implications of the findings are discussed in light of the roles that government agencies and professional bodies share when working with refugee mothers. [ABSTRACT FROM AUTHOR]
- Published
- 2018
13. The civilizational role of Islam in the Indian subcontinent: The Delhi sultanate.
- Author
-
Islam, Arshad
- Subjects
- *
ISLAM , *ART & architecture , *SULTANATE , *CULTURAL history , *HISTORY , *HISTORY of Islam ,HISTORY of India - Abstract
Muslim presence was manifest in the coastal regions of Southern India from the earliest days of Islam, as evidenced by the establishment of Arab trading settlements, with minor political impact prior to the conquests in Northern India from the beginning of the 8th century, which solidified the influence of Islam leading to tangible political and socio-cultural impacts in the region. The history of India furnishes an amazing picture of the syntheses of many divergent cultural trends which were gradually transformed by a process of mutual adjustment and assimilation. Islam played a significant role in this by contributing to India's multi-cultural and multi-religious ethos, embedding the subcontinent in the Arab-Islamic maritime civilization, stretching from southern Africa to China, particularly in connecting Africa as well as the great Turkic empires of Central Asia. It offers a pertinent example of the interaction of human minds and the effects of cultural and civilizational contacts on indigenous customs, religion, literature and arts. This paper examines the impact of Islam in the Indian Peninsula from three different angles: its political predominance, its intellectual and cultural impact, and finally, its influence on art and architecture. Based mainly on Arabic and Persian sources, the article focuses on the intellectual legacy, achievements and the role that the Indian Muslims played in the Indian subcontinent during the Delhi Sultanate, the first major Islamic political authority to govern large parts of South Asia. [ABSTRACT FROM AUTHOR]
- Published
- 2017
14. The Genesis of Persian and Urdu Languages and Literatures in India.
- Author
-
Islam, Arshad
- Subjects
CIVILIZATION of India ,PERSIAN language ,URDU language - Abstract
The Indian subcontinent has contained a vast array of ethnicities, cultures, traditions and languages since the beginning of civilisation. While classical Indian civilisation was based on Sanskrit, the sacerdotal language of the Brahmins, this sacred language did not affect the general mass of people, nor literature beyond a privileged elite. The first true lingua franca that transcended caste barriers to a certain extent was Persian, which was adopted by the ruling dynasties of Muslim India (who themselves were generally Turks or indigenous Indians rather than Persians), their Hindu peers, as well as the civil servants. However, from the beginning of the seventeenth century Urdu began to form around the lower echelons of society as a pidgin common tongue to enable communication between the myriad ethnicities of the Mughal Empire, ultimately restricting Persian to a refined language of culture and courtly life in the Mughal court and becoming a vibrant and dynamic language in its own right, thus becoming the first literary language with a substantial original contribution from Indians since ancient Sanskrit. This article charts the adoption of Persian and later the emergence of Urdu as spoken and literary languages in the Indian subcontinent using original sources in those languages. [ABSTRACT FROM AUTHOR]
- Published
- 2015
15. Proteome scale comparative modeling for conserved drug and vaccine targets identification in Corynebacterium pseudotuberculosis.
- Author
-
Hassan, Syed Shah, Tiwari, Sandeep, Guimarães, Luís Carlos, Jamal, Syed Babar, Folador, Edson, Sharma, Neha Barve, de Castro Soares, Siomar, Almeida, Síntia, Ali, Amjad, Islam, Arshad, Dias, Fabiana, de Abreu, Vinicius Augusto Carvalho, Jain, Neha, Bhattacharya, Antaripa, Juneja, Lucky, Miyoshi, Anderson, Silva, Artur, Barh, Debmalya, Turjanski, Adrian Gustavo, and Azevedo, Vasco
- Abstract
Corynebacterium pseudotuberculosis (Cp) is a pathogenic bacterium that causes caseous lymphadenitis (CLA), ulcerative lymphangitis, mastitis, and edematous to a broad spectrum of hosts, including ruminants, thereby threatening economic and dairy industries worldwide. Currently there is no effective drug or vaccine available against Cp. To identify new targets, we adopted a novel integrative strategy, which began with the prediction of the modelome (tridimensional protein structures for the proteome of an organism, generated through comparative modeling) for 15 previously sequenced C. pseudotuberculosis strains. This pan-modelomics approach identified a set of 331 conserved proteins having 95-100% intra-species sequence similarity. Next, we combined subtractive proteomics and modelomics to reveal a set of 10 Cp proteins, which may be essential for the bacteria. Of these, 4 proteins (tcsR, mtrA, nrdI, and ispH) were essential and non-host homologs (considering man, horse, cow and sheep as hosts) and satisfied all criteria of being putative targets. Additionally, we subjected these 4 proteins to virtual screening of a drug-like compound library. In all cases, molecules predicted to form favorable interactions and which showed high complementarity to the target were found among the top ranking compounds. The remaining 6 essential proteins (adk, gapA, glyA, fumC, gnd, and aspA) have homologs in the host proteomes. Their active site cavities were compared to the respective cavities in host proteins. We propose that some of these proteins can be selectively targeted using structure-based drug design approaches (SBDD). Our results facilitate the selection of C. pseudotuberculosis putative proteins for developing broad-spectrum novel drugs and vaccines. A few of the targets identified here have been validated in other microorganisms, suggesting that our modelome strategy is effective and can also be applicable to other pathogens. [ABSTRACT FROM AUTHOR]
- Published
- 2014
- Full Text
- View/download PDF
16. Novel Triphenylantimony(V) and Triphenylbismuth(V) Complexes with Benzoic Acid Derivatives: Structural Characterization, in Vitro Antileishmanial and Antibacterial Activities and Cytotoxicity against Macrophages.
- Author
-
Islam, Arshad, Da Silva, Jeferson Gomes, Moan Berbet, Filipe, da Silva, Sydnei Magno, Lages Rodrigues, Bernardo, Beraldo, Heloisa, Melo, Maria Norma, Frézard, Frédéric, and Demicheli, Cynthia
- Subjects
- *
ANTI-infective agents , *CELL-mediated cytotoxicity , *ANTIBACTERIAL agents , *CRYSTAL structure , *CARBOXYLATES , *ORGANOBISMUTH compounds , *ORGANOANTIMONY compounds - Abstract
Two novel organoantimony(V) and two organobismuth(V) complexes of the type ML2 were synthesized, with L = acetylsalicylic acid (HL1) or 3-acetoxybenzoic acid (HL2) and M = triphenylantimony(V) (M1) or triphenylbismuth(V) (M2). Complexes, [M1(L1)2] (1), [M1(L2)2]·CHCl3 (2), [M2(L1)2], (3) and [M2(L2)2] (4), were characterized by elemental analysis, IR and NMR. Crystal structures of triphenylantimony(V) dicarboxylate complexes 1 and 2 were determined by single crystal X-ray diffraction. Structural analyses revealed that 1 and 2 adopt five-coordinated extremely distorted trigonal bipyramidal geometries, binding with three phenyl groups in the equatorial position and two deprotonated organic ligands (L) in the axial sites. The metal complexes, their metal salts and ligands were evaluated in vitro for their activities against Leishmania infantum and amazonensis promastigotes and Staphylococcus aureus and Pseudomonas aeruginosa bacteria. Both the metal complexes showed antileishmanial and antibacterial activities but the bismuth complexes were the most active. Intriguingly, complexation of organobismuth(V) salt reduced its activity against Leishmania, but increased it against bacteria. In vitro cytotoxic test of these complexes against murine macrophages showed that antimony(V) complexes were the least toxic. Considering the selectivity indexes, organoantimony(V) complexes emerge as the most promising antileishmanial agents and organobismuth(V) complex 3 as the best antibacterial agent. [ABSTRACT FROM AUTHOR]
- Published
- 2014
- Full Text
- View/download PDF
17. Mixed Antimony(V) Complexes with Different Sugars to Modulate the Oral Bioavailability of Pentavalent Antimonial Drugs.
- Author
-
Ferreira, Weverson A., Islam, Arshad, Andrade, Aretha Priscilla S., Fernandes, Flaviana R., Frézard, Frédéric, and Demicheli, Cynthia
- Subjects
- *
ANTIMONY compounds , *CHEMICAL synthesis , *MALTOSE , *SUGAR derivatives , *CIRCULAR dichroism , *RIBONUCLEOSIDES - Abstract
Previous studies have shown that the association of the drug meglumine antimoniate (MA) with β-cyclodextrin can improve its bioavailability by the oral route. In this work, ribose and maltose were investigated for their ability to form mixed or association complexes with MA, release MA and modulate the serum levels of Sb after oral administration in mice. Analysis of the MA/ribose composition by high performance liquid chromatography coupled to mass spectrometry (LCMS-IT-TOF) revealed the presence of mixed meglumine-Sb-ribose and Sb-ribose complexes. Analysis of the MA/maltose composition suggested the formation of MA-maltose association compounds. Circular dichroism characterization of these compositions following dilution in water at 37 °C suggested a partial and slow dissociation of the association compounds. When the MA/ribose composition was administered orally and compared to MA, the serum concentration of Sb was significantly lower after 1 h and greater after 3 h. On the other hand, the MA/maltose composition showed similar serum Sb concentration after 1 h and higher level of Sb after 3 h, when compared to MA. In conclusion, the present study has demonstrated the formation of mixed or association complexes of MA with sugars, such as maltose and ribose, which promoted sustained serum level of Sb after oral administration. [ABSTRACT FROM AUTHOR]
- Published
- 2014
- Full Text
- View/download PDF
18. Allama Shibli and the early Muslim League: A dissenting voice.
- Author
-
Islam, Arshad
- Subjects
- *
INDIAN Muslims , *ORGANIZATIONAL structure ,POLITICS & government of India ,SOCIAL conditions in India - Abstract
The All-India Muslim League (AIML) was formed in 1906, with the primary aim to improve the educational and socioeconomic status of Muslims. Allama Shibli Nu'mani (1857-1914) put forward an argument in support of Muslims recovering from the political stupor into which they had fallen after the British suppression of the 1857 uprising. He encouraged Muslims to participate in democratic politics in India, departing from the educational focus of his mentor, Sir Saiyid Ahmad Khan (1817-1898). Shibli advanced a strong critique of the Muslim League's limited ambitions in comparison with the Indian National Congress (INC). His critique, notably in ironic and emotive poetry, signiicantly contributed to the national discussion pertaining to the Muslim League's reform and restructure. Based on Shibli's original writings, this paper analyses his critique of the Muslim League and his efforts to overhaul its structure and policies. It examines the response of the Muslim League to these critiques and studies the extent to which its structure and policies changed. [ABSTRACT FROM AUTHOR]
- Published
- 2013
19. Complete genome sequence of Corynebacterium pseudotuberculosis biovar ovis strain P54B96 isolated from antelope in South Africa obtained by rapid next generation sequencing technology.
- Author
-
Hassan, Syed Shah, Guimarães, Luis Carlos, Pereira, Ulisses de Pádua, Islam, Arshad, Ali, Amjad, Bakhtiar, Syeda Marriam, Ribeiro, Dayana, Dos Santos, Anderson Rodrigues, Soares, Siomar de Castro, Dorella, Fernanda, Pinto, Anne Cybelle, Cruz Schneider, Maria Paula, Barbosa, Maria Silvanira, Almeida, Síntia, Abreu, Vinícius, Aburjaile, Flávia, Carneiro, Adriana Ribeiro, Cerdeira, Louise Teixeira, Fiaux, Karina, and Barbosa, Eudes
- Subjects
CORYNEBACTERIUM pseudotuberculosis ,ACTINOBACTERIA ,LYMPHADENITIS ,GENOMES - Abstract
The Actinobacteria, Corynebacterium pseudotuberculosis strain P54B96, a nonmotile, non-sporulating and a mesophile bacterium, was isolated from liver, lung and mediastinal lymph node lesions in an antelope from South Africa. This strain is interesting in the sense that it has been found together with non-tuberculous mycobacteria (NTMs) which could nevertheless play a role in the lesion formation. In this work, we describe a set of features of C. pseudotuberculosis P54B96, together with the details of the complete genome sequence and annotation. The genome comprises of 2.34 Mbp long, single circular genome with 2,084 protein-coding genes, 12 rRNA, 49 tRNA and 62 pseudogenes and a G+C content of 52.19%. The analysis of the genome sequence provides means to better understanding the molecular and genetic basis of virulence of this bacterium, enabling a detailed investigation of its pathogenesis. [ABSTRACT FROM AUTHOR]
- Published
- 2012
- Full Text
- View/download PDF
20. Combination oral therapy against Leishmania amazonensis infection in BALB/c mice using nanoassemblies made from amphiphilic antimony(V) complex incorporating miltefosine
- Author
-
Ricardo Toshio Fujiwara, Daniel Menezes Souza, Luis Rivas, Arshad Islam, Cynthia Demicheli, Frédéric Frézard, Juliane Sousa Lanza, Virgínia Mendes Carregal, Conselho Nacional de Desenvolvimento Científico e Tecnológico (Brasil), Coordenação de Aperfeiçoamento de Pessoal de Nível Superior (Brasil), Fundação de Amparo à Pesquisa do Estado de São Paulo Minas Gerais, Redes Temáticas de Investigación Cooperativa en Salud (España), Carregal, Virginia, Islam, Arshad, Fujiwara, R. T., Rivas, Luis, Frézard, Frédéric, Carregal, Virginia [0000-0003-3505-9494], Islam, Arshad [0000-0002-9953-4816], Fujiwara, R. T. [0000-0002-4713-575X], Rivas, Luis, [0000-0002-2958-3233], and Frézard, Frédéric [0000-0003-3783-5717]
- Subjects
Drug ,Antimony ,Combination therapy ,media_common.quotation_subject ,Phosphorylcholine ,Leishmania mexicana ,Antiprotozoal Agents ,Oral route ,Administration, Oral ,Leishmaniasis, Cutaneous ,Drug resistance ,Pharmacology ,BALB/c ,Oral administration ,medicine ,Animals ,Drug combination ,Leishmaniasis ,media_common ,Miltefosine ,Mice, Inbred BALB C ,General Veterinary ,biology ,General Medicine ,biology.organism_classification ,Leishmania ,medicine.disease ,Disease Models, Animal ,Infectious Diseases ,Insect Science ,Nanoparticles ,Parasitology ,Female ,medicine.drug - Abstract
8p.-3 fig.-1 tab., Clinically available drugs for mucocutaneous and cutaneous leishmaniases (CL) include mainly pentavalent antimony (Sb(V)) complexes, liposomal amphotericin B, and miltefosine (HePC). However, they present at least one of the following limitations: long-term parenteral administration through repeated doses, severe side effects, drug resistance, and high cost. HePC is the only oral drug available, but the appearance of resistance has resulted in changes of its use from monotherapy to combination therapy. Amphiphilic Sb(V) complexes, such as SbL8 obtained from reaction of Sb(V) with N-octanoyl-N-methylglucamide, were recently found to be orally active against experimental CL. The property of SbL8 to self-assemble in aqueous solution, forming nanostructures, led us to investigate the incorporation of HePC into SbL8 nanoassemblies and the therapeutic efficacy of SbL8/HePC nanoformulation by oral route in a murine model of CL. HePC incorporation into the SbL8 nanosystem was evidenced by using a fluorescent analog of HePC. The antileishmanial activity of SbL8/HePC nanoassemblies was evaluated after daily oral administration for 30 days in Leishmania amazonensis-infected BALB/c mice, in comparison with monotherapies (SbL8 or HePC) and saline control. All the treatments resulted in significant reduction in the lesion size growth, when compared with control. Strikingly, only SbL8/HePC nanoassemblies promoted a significant decrease of the parasite burden in the lesion. This work establishes the therapeutic benefit of SbL8/HePC association by oral route in a CL model and constitutes an important step towards the development of new orally active drug combination., This work was supported by the Brazilian agencies Conselho Nacional de Desenvolvimento Científico e Tecnológico (CNPq, grant number: 425332/2018–7), Coordenação de Aperfeicoamento de Pessoal de Nível Superior (CAPES, grant number: PNPD20131163), and Fundação de Amparo a Pesquisa do Estado de Minas Gerais (FAPEMIG, grant number: APQ-03129-16) for financial support. F.F. was recipient of fellowship from CNPq (grant number: 305659/2017-0) and Chaire Jean d’Alembert, Université Paris-Saclay, France (ANR-11-IDEX-0003-02). L.R was supported by Program of Redes Temáticas de Investigación Cooperativa RETICS-FEDER (grant number: RD16/0027/0010).
- Published
- 2019
21. Efficacy of Meglumine Antimoniate in a Low Polymerization State Orally Administered in a Murine Model of Visceral Leishmaniasis.
- Author
-
Kato KC, de Morais-Teixeira E, Islam A, Leite MF, Demicheli C, de Castro WV, Corrêa-Junior JD, Rabello A, and Frézard F
- Subjects
- Administration, Oral, Animals, Caco-2 Cells, Disease Models, Animal, Female, Humans, Meglumine Antimoniate administration & dosage, Meglumine Antimoniate chemistry, Mice, Mice, Inbred BALB C, Polymerization, Leishmaniasis, Visceral drug therapy, Meglumine Antimoniate therapeutic use
- Abstract
Progress toward the improvement of meglumine antimoniate (MA), commercially known as Glucantime, a highly effective but also toxic antileishmanial drug, has been hindered by the lack of knowledge and control of its chemical composition. Here, MA was manipulated chemically with the aim of achieving an orally effective drug. MA compounds were synthesized from either antimony pentachloride (MA-SbCl
5 ) or potassium hexahydroxyantimonate [MA-KSb(OH)6 ] and prepared under a low polymerization state. These compounds were compared to Glucantime regarding chemical composition, permeation properties across a cellulose membrane and Caco-2 cell monolayer, and uptake by peritoneal macrophages. MA-SbCl5 and MA-KSb(OH)6 were characterized as less polymerized and more permeative 2:2 Sb-meglumine complexes than Glucantime, which consisted of a mixture of 2:3 and 3:3 Sb-meglumine complexes. The antileishmanial activities and hepatic uptake of all compounds were evaluated after oral administration in BALB/c mice infected with Leishmania infantum chagasi , as a model of visceral leishmaniasis (VL). The synthetic MA compounds given at 300 mg Sb/kg of body weight/12 h for 30 days significantly reduced spleen and liver parasite burdens, in contrast to those for Glucantime at the same dose. The greater activity of synthetic compounds could be attributed to their higher intestinal absorption and accumulation efficiency in the liver. MA-SbCl5 given orally was as efficacious as Glucantime by the parenteral route (80 mg Sb/kg/24 h intraperitoneally). These data taken together suggest that treatment with a less-polymerized form of MA by the oral route may be effective for the treatment of VL., (Copyright © 2018 American Society for Microbiology.)- Published
- 2018
- Full Text
- View/download PDF
Catalog
Discovery Service for Jio Institute Digital Library
For full access to our library's resources, please sign in.