anti-HIV Properties Research Articles

Andrographis Paniculata in the Treatment of Upper Respiratory Tract Infections

Andrographis paniculata is a species of Andrographis paniculata (Burm. F) The herbaceous plant Nees, sometimes known as "king of bitters," is a member of the Acanthaceae family. It's commonly used to treat sore throats, flu, and upper respiratory tract infections in China, India, Thailand, and Malaysia. In numerous studies, andrographolide, a significant bioactive chemical ingredient of the plant, has shown anticancer potentialIn experimental models of asthma, stroke, and arthritis, andrographolide and its derivatives show anti-inflammatory properties. Pharmaceutical chemists have recently synthesized a number of andrographolide derivatives with important pharmacological properties such as anti-inflammatory, antibacterial, anticancer, antidiabetic, anti-HIV, antifeedant, and antiviral properties. The summary of the effects of andrographolide on cardiovascular illness, platelet activation, infertility, and NF-B activation in this research is remarkable. In traditional Indian and Chinese medicine, a variety of plant items were frequently recommended as medications. We investigate the potency of four selected phytochemicals from the A. paniculata plant, namely andrographolide (AGP1), 14-deoxy 11,12-didehydro andrographolide (AGP2), neoandrographolide (AGP3), and 14-deoxy andrographolide (AGP4), against four key targets, including three non-structural protein (3 L main protease (3CLpro), Papain like proteinase (PLpro) and RNA-directed RNA polymerase (RdRp)) and a structural protein (spike protein (S)) of the virus which are responsible for replication, transcription and host cell recognition. This paper intended to know the mechanism of A.Panniculata bioactive compounds and its effect to relief the upper respiratory tract infection symptomps.

In-silico modelling of fullerene and fullerene adsorbed by nO2 molecules (n(O2)@Cm with n = 1, 2, 4 and m = 48 and 60) as potential SARS-CoV-2 inhibitors

COVID-19 pandemic started more than a year ago and has infected more than 115 million of people from ~210 countries and >2.5 million of deaths worldwide being reported without any commercial and effective treatment or vaccine being yet released. However, recent studies on nanomaterials such as fullerenes, carbon nanotubes and graphene showed that they possess anti-inflammatory, antiviral, anti-oxidant and anti-HIV properties. Herein, the interactions which established between the fullerenes Cm (m = 48, 60, 70, 80, 84 and 86) and the spike protein (SP) of SARS-CoV-2 and the human ACE2 receptor have been investigated based on the density functional theory (DFT) method with the CAM-B3LYP functional and the 6-31G* basis. The results of this study show that C48 exhibited as potential inhibitor of SARS-CoV-2. Because of the presence of heteroatoms on the surface of fullerenes which systematically reduce energy gaps, which in turn increase their reactivities. The oxygen adsorbed by fullerenes increases the number of non-covalent contacts and involves a large number of hydrogen bonds, while decreasing the binding energies. Thus, the hACE2-SP-4O2@C60 complex is strongly recommended for inhibiting SARS-CoV-2 in the final phase of contamination.Graphic abstractStabilizing interactions between fullerenes and the spike protein of SARS-CoV-2.

A SHORT REVIEW ON HERBAL PRODUCTS ACTING AS ANTI-HIV AGENTS

Over the previous decade, considerable advancement has been made in research on the regular items having hostility to HIV movement. An assortment of optional metabolites got from natural origin demonstrated mild to strong anti-HIV properties. Nature has consistently given a wellspring of medications to different sicknesses. Various therapeutic plants have been accounted for to have against HIV. The investigation of regular items in biomedical exploration is not an advanced idea. vast numbers of the best medicinal therapeutic drugs are extracted from natural products and concentrated in HIV/AIDS. The Biomedical review has a long history of disclosure depending on the screen of medicinal spices and conventional medicines. It is essential to remember the clinical study convention to conclude Therapies based on these herbal products combat the negative view of alternative medicine as therapeutic remedies. This review addressed different herbal products that are having anti-HIV properties.

1,8-Naphthyridine Derivatives: An Updated Review on Recent Advancements of Their Myriad Biological Activities

Among all nitrogen-containingheterocycles, the1,8-naphthyridine scaffold has recently gained an immense amount of curiosity from numerous researchers across fields of medicinal chemistry and drug discovery. This new attention can be ascribed to its versatilityof synthesis, its reactivenessand the variety ofbiologicalactivities it has exhibited. Over the past half-decade, numerous diverse biological evaluationshave beenconducted on 1,8-naphthyridine and its derivatives in a quest to unravel novel pharmacological facets to this scaffold. Its potency to treat neurodegenerative and immunomodulatory disorders, along with its anti-HIV, antidepressant and antioxidant properties, has enticed researchers to look beyond its broad-spectrum activities, providing further scope for exploration. This review is a consolidated update of previous works on 1,8-naphthyridines and their analogs, focusing on the past5 years.

Nanomedicine perspective in HIV therapy: biosynthesized gold nanoparticles exhibiting enhanced anti-HIV property

BackgroundGlobally, HIV/AIDS is a major public health issue. Currently, available antiretroviral therapy (ART) has a number of impediments. The need for long-term usage of antiretroviral drugs is associated with the problem of drug resistance, high cost, and other side effects. Hence, there is a constant urge for the development of novel drugs to combat the disease. The synthesis of nanoparticles is of great interest because of their reported application in diverse fields. In contrast to chemical synthesis, green synthesis is inexpensive and enviro-safe.ResultsCalophyllum inophyllum (CI) is a plant that is known to possess anti-HIV activity. Hence, this plant was exploited for the synthesis of gold nanoparticles (AuNPs) in the present study. Two parts of the plant, namely, the fruit and leaves (CIF and CIL) were used for the synthesis of nanocompounds. The two nanocompounds were tested on HIV-1 isolates at different concentrations and the EC50 values were determined. While CIF-AuNP demonstrated very good anti-HIV activity with an EC50 value of 0.09097 ng/ml, CIL-AuNPs did not show significant anti-HIV activity.ConclusionsThe present study is a novel attempt to produce nanocompounds that incorporate the medicinal properties of certain plants that are known to have anti-HIV activity within nanoparticles, such that the compound possesses the attributes of a nanomaterial alongside the phytoactivity. Our results provide evidence to suggest that the CIF-AuNP can be further explored for in vivo activity. In vitro cytotoxicity of the AuNPs was checked in VERO cell lines using the MTT assay. Cytotoxicity was observed to be minimal at all the tested concentrations.

Synthesis of New 1-Substituted-3-(3-(2-Chlorophenyl)-4-Oxo-3,4-Dihydrobenzopyrimidin-2-Ylamino)Isothioureas as Anti-HIV and Antibacterial Agents

In this study, a new benzopyrimidine analog was designed and synthesized by substituting 3-nitrophenyl ring and thiosemicarbazide nucleus at N-3 and C-2 positions of quinazoline ring, respectively. The title compounds, 1-substituted-3-(3-(2-chlorophenyl)-4-oxo-3,4-dihydrobenzopyrimidin-2-ylamino)isothioureas 7A – 7J were obtained via reactions of 2-hydrazino-3-(2-chlorophenyl)quinazolin-4(3H)-one (5) with different alkyl/aryl isothiocyanates followed by methylation with dimethyl sulphate. All synthesized compounds were screened for their antitubercular, anti-HIV, and antibacterial activity against selected Gram-positive and Gram-negative bacteria using agar diffusion method. Amongst, compounds 2-methyl-3-(3-(2-chlorophenyl)-4-oxo-3,4-dihydrobenzopyrimidin-2-ylamino)-1-(3-chloropheny)isothiourea (7I) and 2-methyl-3-(3-(2-chlorophenyl)-4-oxo-3,4-dihydrobenzopyrimidin-2-ylamino)-1-(3-chlorophenyl)isothiourea (7F) showed the most potent activity against P. vulgaris and S. aureus with a MIC of 3 μg/mL. Compound 7I exhibited antitubercular activity at a minimum MIC of 3.125 μg/mL and anti-HIV activity at EC50 of 2.91 μg/mL against HIV1 and HIV2, thus offering probable lead for further development and optimization of new antitubercular and anti-HIV drugs. Results obtained in this study confirm that the synthesized and biologically evaluated benzopyrimidines possess promising antimicrobial, antitubercular, and anti-HIV properties and provide new scaffolds for antimicrobial activity.

Comparative GC-MS Analysis of Methanolic Extracts from Different Parts of Bitter Gourd (<i>Momordica charantia</i> L.) Fruit

Medicinal plants are used in traditional medicine since the prehistoric period. They are considered a rich resource for developing single drugs and formulations due to a wide variety of bioactive phytochemicals present. Bitter gourd (Momordica charantia L.) is an important tropical and subtropical medicinal plant commonly cultivated in Asian and African countries for its health and nutritional properties. The bitter gourd fruits possess antidiabetic, anticancer, anti-obesity, antimicrobial, antioxidant, anti-inflammatory, anti-helminthic, and anti-HIV properties. In this study, we extracted the phytochemicals from the rind, pulp, and seeds of the two botanical varieties of bitter gourd, Momordica charantia var. charantia and Momordica charantia var. muricata in methanol, and subjected them to gas chromatography-mass spectrometry (GC-MS) analysis. Phytochemical analysis revealed several important bioactive compounds such as n-Hexadecanoic acid, Linolenic acid, Vitamin E, Sitosterol, Stigmasterol, and Phytol. Biological activities were reported for some of these compounds. Identification of these compounds validates the medicinal value of bitter gourd. Further studies are to be carried out to isolate, characterize, and study the individual compound's mechanism of action.

On improving the physiological stability of curcuminoids: Curcumininoid-silver nanoparticle complex as a better and efficient therapeutic agent

Curcumin, together with its analogs, namely, demethoxycurcumin and bisdemethoxycurcumin, are phenolic pigments extracted from turmeric. These curcuminoids are considered to be a potent antioxidants possessing a multitude of properties including anti-inflammatory, antitumor, anti-HIV and antimicrobial properties. One of the serious drawbacks of these curcuminoids as therapeutic agent is their fast degradation at physiological pH leading to poor bioavailability in the biological milieu. With a view to address this stability issue we synthesized curcuminoid-silver nanoparticle (CUR-AgNP) complexes, utilizing curcuminoids as reducing agents. The stability of individual curcuminoids in the CUR control and in the CUR-AgNP complex was compared after incubation in phosphate buffer of pH 7.4. Interestingly the initial degradation of curcuminoids at 4 h was only 9.6% in the CUR-AgNP complex when compared to 49.6% degradation observed in the CUR control. Among the three curcumin analogs, bisdemethoxycurcumin showed better pH stability compared to curcumin and demethoxycurcumin whereas all the three curcuminoids exhibited the same degradation pattern in the case of the CUR-AgNP complex. In vitro studies with the CUR-AgNP complex showed excellent antibacterial property against P. aeruginosa. CUR-AgNP complex also exhibited good cytotoxic effect on MDA-MB231 cells. The storage stability of CUR-AgNP complex, kept as a suspension at room temperature (∼28 oC), was tested by measuring its hydrodynamic size and zeta potential. It was found that after 340 days of storage the particle size (Z-average) and zeta potential were 65.5 ± 1.1 nm and -22.9 ± 0.2 mV, respectively, indicating that the nanoparticle suspension was stable The results obtained in the present study are promising and could be extended to improve the therapeutic efficacy of curcuminoids in the biological pH conditions.

Naturally Occurring Calanolides: Occurrence, Biosynthesis, and Pharmacological Properties Including Therapeutic Potential.

Calanolides are tetracyclic 4-substituted dipyranocoumarins. Calanolide A, isolated from the leaves and twigs of Calophyllum lanigerum var. austrocoriaceum (Whitmore) P. F. Stevens, is the first member of this group of compounds with anti-HIV-1 activity mediated by reverse transcriptase inhibition. Calanolides are classified pharmacologically as non-nucleoside reverse transcriptase inhibitors (NNRTI). There are at least 15 naturally occurring calanolides distributed mainly within the genus Calophyllum, but some of them are also present in the genus Clausena. Besides significant anti-HIV properties, which have been exploited towards potential development of new NNRTIs for anti-HIV therapy, calanolides have also been found to possess anticancer, antimicrobial and antiparasitic potential. This review article provides a comprehensive update on all aspects of naturally occurring calanolides, including their chemistry, natural occurrence, biosynthesis, pharmacological and toxicological aspects including mechanism of action and structure activity relationships, pharmacokinetics, therapeutic potentials and available patents.

Molecular dynamics simulations of sulfone derivatives in complex with DNA topoisomerase IIα ATPase domain

Human topoisomerase II alpha (TopoIIα) is a crucial enzyme involved in maintaining genomic integrity during the process of DNA replication and mitotic division. It is a vital therapeutic target for designing novel anticancer agents in targeted cancer therapy. Sulfones, members of organosulfur compounds, have been reported to possess various biological activities such as antimicrobial, anti-inflammatory, anti-HIV, anticancer, and antimalarial properties. In the present study, a series of sulfones was selected to evaluate their inhibitory activity against TopoIIα using computational approaches. Molecular docking results revealed that several sulfone analogs bind efficiently to the ATPase domain of TopoIIα. Among them, sulfones 18a, 60a, *4 b, *8 b, *3c, and 8c exhibit higher binding affinity than the known TopoII inhibitor, salvicine. Molecular dynamics simulations and free energy calculations based on MM/PB(GB)SA method demonstrated that sulfone *8 b strongly interacts with amino acid residues in the ATP-binding pocket (E87, N91, D94, I125, I141, F142, S149, G161, and A167), driven mainly by an electrostatic attraction and a strong H-bond formation at G161 residue. Altogether, the obtained results predicted that sulfones could have a high potential to be a lead molecule for targeting TopoIIα. Communicated by Ramaswamy H. Sarma

Alkylated benzimidazoles: Design, synthesis, docking, DFT analysis, ADMET property, molecular dynamics and activity against HIV and YFV

A series of alkylated benzimidazole derivatives was synthesized and screened for their anti-HIV, anti-YFV, and broad-spectrum antiviral properties. The physicochemical parameters and drug-like properties of the compounds were assessed first, and then docking studies and MD simulations on HIV-RT allosteric sites were conducted to find the possible mode of their action. DFT analysis was also performed to confirm the nature of the hydrogen bonding interaction of active compounds. The in silico studies indicated that the molecules behaved like possible NNRTIs. The nature – polar or non-polar and position of the substituent present at fifth, sixth, and N-1 positions of the benzimidazole moiety played an important role in determining the antiviral properties of the compounds. Among the various compounds, 2-(5,6-dibromo-2-chloro-1H-benzimidazol-1-yl)ethan-1-ol (3a) showed anti-HIV activity with an appreciably low IC50 value as 0.386 × 10−5μM. Similarly, compound 2b, 3-(2-chloro-5-nitro-1H-benzimidazol-1-yl) propan-1-ol, showed excellent inhibitory property against the yellow fever virus (YFV) with EC50 value as 0.7824 × 10−2μM.

A straightforward synthesis of natural oxygenated ent-kaurenoic acid derivatives

The paper presents the synthesis of some natural diterpenoids of ent-kauranic structure, starting from ent-kaur-16-en-19-oic acid, a natural diterpenoid readily available from the dried wastes of sunflower (Helianthus annuus L.). The reported ent-16α,17-dihydroxykauran-19-oic, ent-16α-hydroxy-17-acetoxykauran-19-oic and ent-16α,17-diacetoxykauran-19-oic acids have been previously isolated from different plant sources and showed diverse biological activities, including anti-HIV, anti-cancer and anti-Alzheimer properties. Their chemical synthesis has not been disclosed so far. Additional cytotoxicity studies of the obtained compounds revealed a remarkable cell proliferative effect of parent ent-kaur-16-en-19-oic acid and two of its synthetic derivatives, which is in line with recent pioneering studies in this area.

Polyethylene glycol (5,000) succinate conjugate of lopinavir and its associated toxicity using Danio rerio as a model organism

Lopinavir (LPV), a well-known drug administered in human immunodeficiency virus (HIV) infection, has shown limitation for pediatric treatment owing to poor aqueous solubility that gives rise to limited oral bioavailability and short plasma half-life (5–6 h). Polymers such as polyethylene glycol (PEG) have been used as drug carriers to improve their solubility. This study reports the preparation of polyethylene glycol (5,000) succinate (PEG–Suc–LPV) conjugate of LPV by the esterification method. The disappearance of the 3,395 cm−1 (O–H stretch of COOH) band for Polyethylene glycol (5,000) succinate (PEG–Suc )confirms the formation ester linkage with the OH group of LPV which is also confirmed by 1H NMR analysis. The XRD for the conjugate showed a broad, amorphous peak while pure PEG, Suc, LPV are crystalline. DSC analysis showed that the conjugate exhibited new broad and diffuse peaks, confirming that they did exist in an amorphous state as multiple complexes. The conjugate showed improved solubility and activity with reduced toxicity compared to pure LPV. The solubility of LPV increased significantly from 80 to 318 ppm. Furthermore, an aquatic toxicity test using Danio rerio showed that the conjugate had a lower LC50 (60.8 ppm) when compared to the pure LPV drug LC50 (6.42 ppm). These results suggest PEG–Suc conjugate of LPV as an efficient carrier for enhanced hydrophilicity and anti-HIV property of LPV.

Betulinic Acid Protects From Bone Loss in Ovariectomized Mice and Suppresses RANKL-Associated Osteoclastogenesis by Inhibiting the MAPK and NFATc1 Pathways.

Osteoclasts with elevated bone resorption are commonly present in postmenopausal osteoporosis, and other osteolytic pathologies. Therefore, suppressing osteoclast generation and function has been the main focus of osteoporosis treatment. Betulinic acid (BA) represents a triterpenoid mainly purified from the bark of Betulaceae. BA shows multiple biological activities, including antitumor and anti-HIV properties, but its effect on osteolytic conditions is unknown. Here, BA suppressed receptor activator of nuclear factor‐κB ligand (RANKL)‐associated osteoclastogenesis and bone resorptive function, as assessed by tartrate‐resistant acid phosphatase (TRAP) staining, fibrous actin ring generation, and hydroxyapatite resorption assays. Mechanistically, BA downregulated the expression of osteoclastic-specific genes. Western blot analysis revealed that BA significantly interrupted ERK, JNK and p38 MAPK activation as well as intracellular reactive oxygen species (ROS) production, thus altering c-Fos and NFATc1 activation. Corroborating the above findings in cell-based assays, BA prevented ovariectomy-associated bone loss in an animal model. In conclusion, these findings suggest that BA can inhibit osteoclast generation and function as well as the RANKL signaling pathway, and might be used for treating osteoclast-related osteoporosis.

Development of a pseudovirus assay and evaluation to screen natural products for inhibition of HIV-1 subtype C reverse transcriptase

Ethnopharmacological relevanceMedicinal plants are used in the management of Human Immunodeficiency Virus and Acquired Immunodeficiency Syndrome (HIV/AIDS) in many developing country settings where HIV-1 subtype C drives the epidemic. Efforts to identify plant derived molecules with anti-HIV properties require reproducible assay systems for routine screening of selected plant compounds. Although a number of standardized HIV-1 pseudoviruses have been generated to assess infectivity, replicability or reproducibility, HIV-1 subtype C (HIV-1-C) pseudoviruses have not been comprehensively characterized to identify inhibitory plant substances. Aim of the studyThe current study aimed at developing an HIV-1-C pseudovirus assay, and evaluate plant substances targeting reverse transcriptase (RT) activity. Materials and methodsHIV-1 subtype C pseudoviruses containing a luciferase reporter gene were generated by transfection of human 293T cells. HIV-1 subtype B (HIV-1-B) wild type pseudoviruses and mutants resistant to nucleoside and non-nucleoside RT inhibitors were also generated and used as controls. Selected plant substances and the RT inhibitors Zidovudine (AZT) and Nevirapine (NVP), were used to evaluate inhibition. Pseudovirus infectivity was determined by luciferase measurement in CF2/CD4+/CCR5 cells, and cytotoxicity was determined using the MTT assay. AZT and NVP inhibited wild type pseudoviruses in a dose dependent manner, with IC50 values in the nanomolar range. ResultsPseudoviruses harbouring RT drug resistance mutations were poorly suppressed by AZT and NVP. Catechin, obtained from Peltophorum africanum inhibited HIV-1-C and HIV-1-B pseudoviruses with selective indices of 6304 μM (IC50: 0.49 μM, CC50: 3089 μM) and 1343 μM (IC50: 2.3 μM, CC50: 3089 μM), respectively; while the methanol root crude extract of Elaeodendron transvaalense gave IC50 values of 11.11 μg/ml and 16.86 μg/ml, respectively. ConclusionThe developed HIV-1-C pseudovirus assay can be used to screen plant substances for RT inhibition, and may have utility in settings with limited access to high level biosafety facilities.

Sulfonate modified Lactoferrin nanoparticles as drug carriers with dual activity against HIV-1

Intriguing properties and structural dynamics of Lactoferrin have been exploited in numerous applications, including its use as self-assembling, pH sensitive nanoparticles to deliver intended cargo at the disease site. In this study, we explore the possibility of surface modification of Lactoferrin nanoparticles to hone its specificity to target HIV-1 infected cells. Existence of free cysteine groups on Lactoferrin nanoparticles available for reaction with external molecules facilitates conjugation on the surface with Sodium 2-mercaptoethanesulfonate (MES). Conjugation with MES is used to edge a negative charge that can mimic CCR5 and Heparan sulfate (initial point of contact of HIV-1 env to host cell surface) electrostatic charge (Sulfate group). A simple sono-chemical irradiation method was employed for self-assembly of Nanoparticles and for surface modification. The nanoparticles serve dual purpose to abrogate extracellular entry and to target viral enzymes, when loaded with ART drugs. The morphology and size distribution of the formed particles were explored using Transmission Electron Microscope (TEM), Scanning Electron Microscope (SEM) and Dynamic Light Scattering. Raman SERS was employed to understand the difference in the protein upon surface modification. The anti-HIV property of the particles was confirmed in-vitro. The modified device demonstrated acceptable nanoparticle properties with controlled release and higher effective concentration in the area of infection.

In vitro anti-HIV-1 activity of ethyl gallate.

In recent years, the exploration for potential inhibitors of HIV has been increased due to the development of drug resistant HIV strains in infected people undergoing antiretroviral agents treatment. In this report, we studied the anti-HIV properties of ethyl gallate (EG) against a panel of HIV-1 strains in in vitro conditions. Different clinical isolates and laboratory strains of HIV-1 were tested for their sensitivity with EG. We found that EG exhibited non-toxic nature over a wide range of cell lines from different tissue origin. Serum proteins have little to no impact on the antiviral activity of EG. In the present study, EG was found to be a promising anti-HIV agent.

Prediction of toxicity of secondary metabolites

Abstract The prediction of toxicological endpoints has gained broad acceptance; it is widely applied in early stages of drug discovery as well as for impurities obtained in the production of generic or equivalent products. In this work, we describe methodologies for the prediction of toxicological endpoints compounds, with a particular focus on secondary metabolites. Case studies include toxicity prediction of natural compound databases with anti-diabetic, anti-malaria and anti-HIV properties.

In vitro inhibition of HIV-1 reverse transcriptase and anti-inflammatory activities of some herbal concoctions sold in the Limpopo Province

HIV-1 is the principal virus that causes acquired immunodeficiency syndrome (AIDS), a condition characterized by extreme immunosuppression and inflammation that leads to life-threatening opportunistic infections. The pitfalls of current anti-retroviral therapies are the lack of medical access in developing countries, adverse side effects and the rise of resistant strains. Natural products used in traditional medicine that can interfere with the replication of the HIV serve as good sources of anti-HIV drugs and anti-inflammation agents. The aim of this study was to validate the anti-HIV and anti-inflammatory properties of some herbal concoctions sold in the Limpopo Province, reported to treat HIV and inflammation related symptoms. The anti-HIV activity was evaluated using the HIV-1 reverse transcriptase (RT) inhibitory bioassay. Anti-inflammatory activity was determined using cyclooxygenase 1 and 2 inhibitory assays. Compared to the controls, Lamivudine, Zidovudine, Lopinavir and Ritonavir, the laboratory concoction showed the highest HIV-reverse transcriptase inhibition (IC50: 2.90 μg/mL), followed by herbal concoction 5 (IC50: 11.74 μg/mL). It is likely the herbal concoctions induced a conformational change on the HIV-RT by binding to its allosteric sites, thus inactivating it. Generally, the herbal concoctions achieved higher percentage inhibitions (≥70%) for COX-2 than for COX-1. The anti-inflammatory activity of the herbal concoctions thus may also assist to alleviate pain in the patients. This research validated the ethnopharmacological use of herbal concoctions towards the treatment of HIV infections. However, more studies are needed to further elucidate the pharmacokinetics and toxicological effects of these medicines.

Quinolone derivatives: Potential anti-HIV agent-development and application.

Acquired immune deficiency syndrome (AIDS)/human immunodeficiency virus (HIV) is one of the largest and most devastating public health pandemics throughout the world. The global pandemic of drug-sensitive HIV and the increasing threat from drug-resistant HIV result in an urgent need to develop more effective anti-HIV candidates. Quinolone represents a significant class of privileged heterocycles, and its derivatives possess promising in vitro and in vivo anti-HIV properties. The 4-quinolone elvitegravir has already been approved for the treatment of HIV; thus, quinolone derivatives might be promising candidates with anti-HIV activity. This review emphasizes quinolone derivatives with potential anti-HIV activity, covering articles published between 1992 and 2019. The structure-activity relationship is also discussed to provide insights for further development of more active quinolone derivatives.