Search or add a thesis

Advanced Search (Beta)
Home > Synthesis, Structure Elucidation & Biological Evaluation of Molecules from Piperine Alkaloid

Synthesis, Structure Elucidation & Biological Evaluation of Molecules from Piperine Alkaloid

Thesis Info

Access Option

External Link

Author

Yasir, Ammar

Program

PhD

Institute

Government College University

City

Lahore

Province

Punjab

Country

Pakistan

Thesis Completing Year

2018

Thesis Completion Status

Completed

Subject

Chemistry

Language

English

Link

http://prr.hec.gov.pk/jspui/bitstream/123456789/11008/1/AMMAR%20YASIR.pdf

Added

2021-02-17 19:49:13

Modified

2024-03-24 20:25:49

ARI ID

1676727529532

Asian Research Index Whatsapp Chanel
Asian Research Index Whatsapp Chanel

Join our Whatsapp Channel to get regular updates.

Similar


Piper nigrum is a medicinal plant and commonly used as household spice, having piperine alkaloid as major and active ingredient. Piperine is an antibacterial compound and its multiple uses have already been established in literature, therefore it is widely used in folk. There are many other potent antibiotics available in the market that contain substituited-1,3,4-oxadiazole heterocyclic ring structures. The high resistivity of microorganisms towards the prevailing drugs motivated us to synthesize new bioactive molecules by combining the piperine backbone to biological active oxadiazole system. It was assumed that 2,5 – disubstituited-1,3,4- oxadiazole heterocyclic ring may act as potent biological active molecules that boost the pharmacological activities to the new limits. The presented research work comprises the synthesis of some novel multifunctional derivatives followed by structural characterization & biological evaluation. Piperine alkaloid is extracted in lab using soxhlet apparatus, purified, further derivatized and characterized. Piperine, by basic hydrolysis, is converted to piperic acid, which on esterification changed into ethyl piperate and upon reaction with hydrazine lead to piperine hydrazide molecule, which acts as backbone for further derivatization. Piperine hydrazide in three different routes changed to 1-oxadaizole moiety by reacting with CS2 in aprotic solvents, 2- Imine functionality bearing molecules by reacting with various aldehydes, 3-sulphonamide functionalities by reacting with various aryl sulphonyl chlorides. Oxadiazoles further converted to oxatriazole by reacting with hydrazine. Overall we have synthesized 83 derivatives of piperine, with oxadiazole, oxatriazole, amide, imine and sulphonamide functionalities. The compounds presented in this work were synthesized according to available protocols in the literature and has been mentioned in seven schemes in detail (at the end of Chapter 1: Introduction). These synthesized compounds were purified through chromatographic techniques including column chromatography and preparative chromatography. Structures of all these were elucidated through IR, EIMS, 1H and 13C NMR spectroscopic techniques. As literature showed that various molecules containing these type of functionalities are biologically active and used for the treatment of various diseases. This encouraged us to evaluate piperine derivatives to search for more biological active or potent molecules. We have evaluated antibacterial, antifungal, hemolytic and thrombolytic xxvi activities. Some selected molecules from these series were also evaluated for analgesic and anti-inflammatory potential. The antibacterial activity was studied against both gram positive (Bacillus subtilus) and gram negative (Escherichia coli) bacterial strains and also evaluated as antifungal activity against Aspergilus niger strain. We have also investigated their toxicity through hemolytic and thrombolytic activities using blood as a substrate. Analgesic and anti-inflammatory activities for selected compounds were performed using swiss albino mice, which showed very encouraging results. Out of seven prepared series, the series (6a-s) in wihich piperidine ring is replaced with oxadiazole moiety shows most significant results. Two of the derivatives (6b & 6h) from this series (6a-s) found more potent antibacterial activity when compared with diclophenac sodium standard. From same series 6l & 6p showed improved hemolytic activity while 6e & 6f exhibited better thrombolytic activity as compared to piperine.7a-p series have aryl derivatives of oxadiazole-amide functionalities and in this series 7b showed the maximum antimicrobial activity while 7l and 7e of this series exhibited better hemolytic and thrombolytic activities respectively. A minor change in carbon chain for the series 8a-p as compared to 7a-p display overall decrease in activities, however prominent antibacterial and antifungal activities were shown by 8a and 8d. Schiff base containing derivative, 10l showed prominent hemolytic activity among the other members of this series. Sulphonamide bearing derivatives 11a-e showed moderate thrombolytic and hemolytic activity but 11e exhibited maximum antibacterial & antifungal activities. Oxatraizole containing derivative 12b and 12f found to have better thrombolytic activity as well as good antimicrobial agents.Selective derivatives were analyzed against analgesic and anti-inflammatory activities. Addition to Schiff Base moiety to piperine (10h) showed maximum analgesic activity (tail + hot plate method) even higher than Diclofenac sodium standard, while simple oxadiazole (5) and alkyl substituted oxadiazole (6o) showed maximum anti-inflammatory activities.Overall it is concluded that introduction of new functionality to piperine alkaloid made the molecules potent than the parent in most of the cases.
Loading...
Loading...

Similar Books

Loading...

Similar Chapters

Loading...

Similar News

Loading...

Similar Articles

Loading...

Similar Article Headings

Loading...

اعلانِ نبوت سے پہلے حضوؐر کا عقیدہ اور ایمان

اعلان نبوت سے پہلے حضورؐ کا عقیدہ اور ایمان
اعتراض نمبر۹۳
ما رگولیس کہتا ہے حضرت خدیجہ ؓ اور آنحضرت ﷺ قبل از نبوت ‘ دونوں سونے سے پہلے ایک بت کی پرستش کر لیا کرتے تھے جس کا نام عزیٰ تھا ۔ ( مارگولیس ۔امہات المو منین ۔۵۹)
۲ ۔انسائیکلو پیڈیا آف اسلام واقعہ غرانیق کے تحت متعدد الزامات تحریر کیے ، اس کے بعد کہا ’’ابتدائی اعتقادات کی جھلک اس طرح بھی نظر آتی ہے کہ عربوں کی طرح انہیں ( محمد ﷺ) بھی جن و شیطان پر عقیدہ تھا ۔ مکہ اپنے حرم کے ساتھ ان کے نزدیک بھی مقدس تھا جن کے تقدس اور رسوم کو انہوں نے اپنے مذہب میں باقی رکھا پھر ایک مرتبہ کفر کی طرف لوٹ جانے کی خواہش نے زور کیا جس پر جلد قابو پا لیا ‘‘۔
جواب: انبیاء اور رسل اعلان نبوت و رسالت سے قبل بھی صفات خداوندی سے آشنا ہوتے ہیں اور ذرا برابر انہیں ان صفات میں شک و شبہ نہیں ہوتا ارشاد ربانی ہے ’’ و لقد الھنا ابراہیم۔۔۔۔۔ عالمین‘‘۔ ’’ترجمہ ‘‘ بے شک ہم نے ابراہیم ؑ کو پہلے ہی سے ان کی شان کے مطابق رشد عطا کیا اور ہم ان کی استعداد کو پہلے سے خوب جانتے تھے ۔‘‘ یہ رشد کیا ہے ؟ سورہ الحجرات میں ہے کہ ’’ رشد قلب میں ایمان و اطاعت خدا وندی کی محبت اور کفر و فسق اور معصیت کی نفرت راسخ ہو جائے اس کا نام رشد ہے ۔ اس سے ظاہر ہے کہ سید نا ابراہیم ؑ ابتدا ہی سے رشد و ہدایت پر تھے یہی حال تمام انبیاء و رسل کا ہے ۔ آپ کا ارشاد ہے ’’ جب میرا نشوو نما شروع ہوا ‘ اس وقت سے بتوں کی شدید نفرت اور عداوت اور اشعار سے سخت...

Practical Depiction of Gender Equality in Fiqh ul Seerah Perspective: An Analytical Assessment

“Gender equality” is certainly not another concept, this approach had been advocated in Islam, based on principles of equity and universal justice. Equality of rights are discussed in detail in sharīʿah (Islamic Law) and Holy Prophet Muhammad (صلى الله عليه وسلم (had implemented them during his sacred era. Because the Qur'an and the Seer’ah of the Holy Prophet Hazrat Muhammad (صلى الله عليه وسلم (is a permanent phenomenon of practice and guidance. According to the sharīʿah men and women without any discrimination are equal before Allah, and women had granted their rights in inheritance and property, social and marriage rights, not aforementioned only, women also have the right to perform civic and administrative duties. From last few decades the concept of gender equality has increased and becoming chicer and trending on the international level. This study emphasizes the equal status between men and women, described in sharīʿah (Islamic Law; based upon Qur’an and Hadith mainly). This concept has often been misunderstood by the majority of society as a direct result of ignorance on how Islam perceives this concept. Not surprisingly, throughout the history of Islam indicates the prominent role has played by Muslim women played every walk of life. Therefore, the present research has discussed the gender equality in fiqh ul seerah perspective and has provided the detailed interpretation in the light of derived Law from actions and decisions taken by the Holy Prophet (صلى الله عليه وسلم, (along this the study also sheds lights upon the implementation of these gender-based rights during most sacred prophetic era and during the period of righteous caliphate as well.

Assessment of Molecular Diversity in Rice Germ Plasm in Nuclear, Mitochondrial and Chloroplast Genomes

Rice has twenty three species but out of these only two species Oryza sativa L and Oryza glaberrima are being cultivated around the world. Asian cultivated rice (O. sativa L.) grasps an exclusive place among domesticated crop species. It is the first fully sequenced crop genome and a critical staple food. Rice along with its wild relatives is being grown on diverse series of agroecological environments and climates. Pakistan is famous for special Basmati rice varieties mainly grown in the Punjab province. Along with Basmati rice, Indica varieties are also grown throughout Pakistan and being exported to different countries. The comparison of genetic diversity of rice varieties grown in Pakistan along with other countries has been given little attention. Information and genetic characterization of rice accessions would be useful in determining present trends in rice breeding and in assessing alternative for improving cultivars. In the present study microsatellite and SNP markers were used to characterize rice accessions from different countries along with Pakistan to provide information about their genetic diversity, which may help for maintenance or expansion of diversity in future breeding programs and to investigate rice adulteration for export purposes. The first study was carried out to evaluate the genetic diversity within a diverse collection of rice (O. sativa L.) accessions and to determine differences in the patterns of diversity within the aromatic and non-aromatic rice varieties. Forty rice accessions were evaluated by using 24 microsatellite markers distributed over the whole rice genome. A total of 66 alleles were detected at 24 SSR loci and the number of alleles per marker ranged from 2 to 4, with an average of 2.75. Polymorphism Information Content (PIC) value ranged from 0.0476 (RM315) to 0.5993 (RM252), with an average of 0.3785 per marker. The average genetic diversity over all SSR loci for the 40 genotypes was 0.4477, ranging from 0.0488 to 0.6638. Major allele frequency ranged from 0.4250 (RM252) to 0.9750 (RM315), with an average of 0.6472. The dendrogram based on the cluster analysis by microsatellite polymorphism grouped 40 rice cultivars into three groups, effectively differentiating Basmati cultivars from non-basmati cultivars. xiii Understanding genetic diversity and population structure in rice populations are of great importance and a prerequisite for genetic characterization and crop improvement. Ninety five accessions from sixteen countries were characterized by one hundred and fifty nine SSR markers. SSR makers were well distributed on the nuclear, mitochondrial and chloroplast genome. The overall results revealed that Indian rice accessions were more divergent than International Rice Research Institute (IRRI) Philippines and Pakistan. Cluster-analysis based on genetic differences coefficients clearly separated all the genotypes into three major groups but was unable to separate the accessions based on their geographical area. The population structure analyses showed that most accessions exhibit some degree of admixture, with many individuals within a population sharing the same introgressed segment due to artificial selection. The model-based structure analysis revealed the presence of three subpopulations. This was basically consistent with clustering based on genetic distance. SSRs proved to be an efficient tool in assessing the genetic diversity of rice genotypes. The same ninety-five accessions of rice were also analyzed in order to profile SSR variation in mitochondrial and chloroplast genomes as well, by using 62 pairs of SSR primers. Out of 42 microsatellite loci for mitochondria only 12 SSR markers showed polymorphism whereas in case of chloroplast 6 out of 20 were found polymorphic. The average gene diversity for both mitochondrial and chloroplast was 0.32 oscillating between 0.041 to 0.620. The PIC value ranged from 0.040 to 0.543 with an average of 0.282. While allelic richness ranged from 2-4 alleles with an average of 2.779 alleles. Mononucleotide repeats stood first (50% polymorphic) for detecting polymorphism for organelle genome followed by tri- (25%), tetra- (14.29%) and dinucleotide (12.5%). Cluster and population analysis revealed two groups of accessions but principal coordinate analysis disagreed with this grouping pattern. The overall results revealed the monophyletic origin of rice. Single nucleotide polymorphism is the base pair change most frequently present in the eukaryotes and are responsible for major diversity. Multiplex single nucleotide polymorphism has been acknowledged as having great potential to find out genetic xiv diversity and structure of diverse rice accessions. One hundred and five accessions of rice were analyzed by RiceOPA2.1 from diverse environment. Twenty accessions representing all five groups of rice were used as reference. Overall call percentage was 97.7%. A total of 746 alleles were detected in this study. The lowest polymorphism information content (PIC) was 0.0706 for SNP id3002191 as compared to the highest PIC value 0.5222 for SNP ud4000438 with an average of 0.3353. The average genic diversity (H) over all SNPs loci for the 105 genotypes was 0.4196, ranging from 0.0733 to 0.5919. Neighbor Joining and Unweighted Pair Group Method with Arithmetic mean cluster analysis clearly separated all the genotypes in two major clusters. Structure analysis based on admixture model and principal coordinate analysis produced the same results. The results revealed that the Indian accessions are more diverse followed by IRRI and Pakistan. This comprehensive and comparative study based on microsatellites and SNPs provides a clear image of genetic diversity of Pakistani rice accessions in comparison with those of other countries accessions. A narrow genetic base has been reported for rice cultivars in Pakistan as compared to that in other countries. So there is a strong need to introduce diverse material in breeding program keeping in view preference of the farmers’ community. The overall results derived from analyses of genetic diversity could be used for designing effective breeding programs aimed at broadening the genetic bases of commercially grown varieties particularly in Pakistan. These results could also be useful for monitoring purity, genotype identification and for plant variety protection.